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Explore the world of GPCRs with Dr. GPCR Podcast! Join industry leaders as they share insights, stories, and groundbreaking discoveries, enriching our understanding of GPCRs. Delve into the science behind these vital components shaping our collective knowledge. Welcome to the Dr. GPCR Podcast - The Voice of the Community Conversations with the world’s leading GPCR scientists. Exploring discoveries, careers, and ideas shaping human health. In each episode, we sit down with leading experts to explore their career journeys, groundbreaking discoveries, and the impact of their research on our shared understanding of GPCR biology. Launched at the height of the pandemic, the Dr. GPCR Podcast was created with three goals: Share discoveries – Highlight the latest advances in the GPCR field. Amplify voices – Provide scientists a platform to showcase their work. Inspire the future – Motivate the next generation to pursue GPCR research. At its core, Dr. GPCR’s mission is simple yet ambitious: to bring the GPCR community together - across borders and disciplines - to connect, exchange, and collaborate in order to improve human health through a deeper understanding of GPCR biology. Latest Podcast Episodes More podcast episodes Dr. GPCR Podcast Audience Survey We are currently planning our next season and need your help. This short survey will help us understand your needs to bring you exciting and informative content. We also know that you are busy, which is why we designed this short survey that should take you 5 minutes. Fill out this form Be our Guest In each episode, we chat with an expert about their career trajectory, discoveries, and how their research contributed to the shared pool of knowledge about GPCR biology. We’d love to have you on our podcast. To be a guest, fill out the form below, and we’ll be in touch in 48 hours. Fill out this form What others are saying about this podcast "You made it a very comfortable and engaging experience, and it felt like we were chatting over coffee — Yamina thoughtfully guided our chat throughout." Anita Nivedha I think it's really well done. I'm genuinely interested to see how it evolves and grows over time, as I feel it has the potential to develop into something even more impactful. Anonymous This came at just the most perfect time. I hadn't heard a scientific talk outside my lab since February and was starved to hear someone else talk passionately about GPCRs. I've listened to the episodes multiple times and it's just like being at a conference getting new ideas. I just couldn't be happier y'all created this podcast. Anonymous Great initiative, thanks. Carrier paths, choosing research topics, switching fields, late start, failures and successes. Anonymous I enjoy the breadth of questioning that goes beyond just the science, and reveals a bit about the scientists as individuals/mentors/people. Anonymous Really enjoyable science podcast! Dr. Yamina Berchiche interviews leading GPCR scientists on this vibrant, entertaining podcast. I really appreciate the way the podcast educates and mentors, particularly towards junior scientists but also to the community as a wholen Yamina is a great interviewer, getting insight and personal history from her guests. Am very grateful for Dr GPCR livening up the week in these difficult times! Sam @Pharmamechanic Listen and subscribe where you get your podcasts

Advanced GPCR webinars for pharmacologists and biotech scientists. Live Q&A. Deep mechanistic insight. Reserve your seat. University / Free & Live Webinar Live GPCR Webinars with the World's Leading Experts. Deep-dive sessions focused on real pharmacology, real drug discovery challenges, and real translational insight. Live Q&A with the scientists shaping the field. Live for those who can be there. On demand for everyone else. 👉 Sign Up for Notifications Get the live link before each session Strategic Partners 1,400+ Scientists in the Ecosystem 30+ Countries Represented 60–90 Scientists per Live Session Free Always. No Paywall. No Catch. Use It Tomorrow Practical takeaways, every session. Walk away with something you can apply in your next experiment, assay, or project decision. Together in the Room Scientists from around the world, in the same conversation. The chat, the Q&A, the shared curiosity — the community thinking together in real time. Free and Generous No paywall. No catch. The ecosystem gives this away because GPCR scientists deserve access to high-quality science. Sign up, show up, bring your questions. Direct Access Ask an expert a live question and get a real answer. That direct access doesn't exist at conferences — it exists here. No Borders Live for those who can be there. On demand for everyone else. The GPCR community doesn't stop at borders — and neither do we. Stay Ahead Learn about methods, tools, and approaches before they become widely known. Be ahead of colleagues who aren't in the ecosystem. What Makes These Webinars Different? Not a lecture. A scientific exchange. Built for the GPCR community, by the GPCR community. Every session is designed to move your science forward. Webinars Upcoming Live & On Demand Webinars Recombinant Antibodies for GPCRs: A Challenge to the Community Speakers Dr. Alexander Ball, MD Dr. Alexander Ball of GeneTex joins Dr. GPCR to walk through what the company is doing about it, and the challenge it comes with: A high-throughput recombinant antibody platform built for specificity at scale Prioritized validation: CRISPR KO/KD, endogenous expression, cell fractionation, comparable antibodies, application-specific testing VirDTM-GPCR arrays for cross-reactivity screening when feasible More than 300 recombinant mAbs against almost 200 human GPCRs, and growing Free samples for GPCR researchers who will test the antibodies in their own labs and give structured feedback Register Here 📅 June 25, 2026 at 3:00:00 PM Details Receptor Signaling Bias: A Valuable and Accessible Property of New Drug Candidates Speaker Dr. Terry Kenakin - UNC Chappel Hill | Terry's Pharmacology Corner Topics Covered The biological basis of receptor signaling bias and ligand-dependent conformations How to design functional assay panels that quantify bias rather than infer it Interpretation pitfalls and what assay system choice does to bias estimates Translating pathway-level data into lead selection and optimization decisions Why potency alone is not enough for candidate-level decisions 📅 May 28, 2026 at 3:00:00 PM Details Fluorescent Probes for GLP-1R and GIPR Imaging: From Cell Assays to In Vivo Systems Speakers Dr. Johannes Broichhagen - Junior Group Leader Dr. David Hodson Topics Covered: LUXendin probes for GLP-1R labeling across imaging modalities daLUXendin dual agonists for GLP-1R and GIPR visualization Nanodomain organization in pancreatic islets and neural sites Practical handling: reconstitution, dilution, and storage Applications from live cells to in vivo systems 📅 March 3, 2026 at 3:00:00 PM Details 1 1 ... 1 ... 1 First Dr. GPCR event? Welcome. This is what the community looks like — scientists from around the world, thinking through discovery challenges together. There's no paywall, no catch. Just real science and real exchange. If this is your first session, there's a lot more where this came from. Want to Go Deeper? This Is Just the Beginning If a free webinar is this good, imagine what the full ecosystem looks like. Dr. GPCR University brings you premium Masterclass sessions, 200+ recordings, weekly curated news, and a global community of GPCR scientists — all in one place. Webinar → Weekly News → 14-Day Trial → University Premium 👉 Sign Up for Notifications These sessions are part of a larger mission: building the most trusted home for GPCR scientists worldwide. Frequently Asked Questions Questions about the webinars What are GPCR webinars? GPCR webinars are free, live online scientific sessions focused on G protein-coupled receptor biology, pharmacology, signaling, and drug discovery. Each session explores mechanistic models, translational challenges, and real-world therapeutic implications through presentations and live Q&A. They're designed for scientists who want deep, data-driven discussion rather than surface-level overviews. Who should attend? Any scientist working with GPCRs — pharmacologists, medicinal chemists, cell biologists, translational researchers, discovery teams, postdocs, PIs, and industry scientists. Whether you're deep in receptor biology or evaluating assay tools, these sessions are built for you. Are the webinars free? Yes. Always. No paywall, no catch. Sign up with a free registration and you'll receive the live link before each session. Recordings are also freely available on demand afterward. Are the webinars live or pre-recorded? All webinars are live events with real-time Q&A — that's the point. After the live session, the full recording becomes available on demand so scientists in every time zone can access the same content and depth. How are these different from conference talks or academic seminars? The Q&A is the core, not an afterthought. These sessions are designed for interaction — scientists asking direct questions and getting real answers. There's no travel required, no registration fee, and you're in a room with researchers from dozens of countries who share your focus on GPCRs. What topics are typically covered? GPCR pharmacology, signaling, structural biology, allosteric modulation, biased agonism, assay design, drug discovery workflows, translational challenges, and the science behind emerging tools and methods. Every session is grounded in receptor biology with a focus on what's practical and applicable. Do I need prior knowledge of GPCR pharmacology? A working understanding of GPCR biology helps you get the most from each session. That said, the presenters are skilled at making complex science accessible, and the Q&A often covers foundational questions alongside advanced discussion. Where can I find more advanced GPCR training? If you want to go deeper, Dr. GPCR University offers premium Masterclass sessions with frontier science, unresolved questions, and extended scientific exchange — exclusively with independent scientists. The webinars are the open door; Masterclass is the room you earn access to. You can explore University with a 14-day trial. Be in the Room When the Science Moves Forward Sign up to get notifications about upcoming webinars. Bring your questions. 👉 Sign Up for Notifications

Explore upcoming GPCR Masterclass live sessions featuring expert discussions on GPCR pharmacology, receptor biology, and drug discovery. University / Live Masterclass Sessions In the room with the scientist, not watching from the audience. Live scientific exchanges with leading GPCR experts. Interactive, question-driven, frontier science. This isn't a lecture — it's a conversation with the people shaping GPCR discovery. Masterclass is included inDr. GPCR University Try it for 14 days Upcoming live sessions Your next Live Masterclass Session is waiting Each session focuses on a specific pharmacology or GPCR discovery topic, led by a recognized expert. Live Q&A means your questions get real answers. June 11, 2026 Dr. Jakob Höppner | Harvard University | MGH Subcellular Regulation of PTH1R Signaling Translational Pharmacology & Disease Models Details October 8, 2026 Dr. Marsha Pierce | Midewestern University Introduction to GLP-1 pharmacology Details June 18, 2026 Dr. Dmitry Veprintsev | U. of Nottingham Postponed | Biophysical approaches to study orphan GPCR ligand binding and signalling Details 1 1 ... 1 ... 1 What makes this different? Not a lecture. Not a webinar. A scientific exchange. The Masterclass was created because the most valuable insights in GPCR science aren't captured in papers or conference talks. Scientist-to-scientist discussion Extended Q&A allows deeper exploration than typical presentations. You're engaging directly with the expert — not submitting a question to a moderator. Beyond conference time limits Topics are explored in greater depth than standard conference talks allow. Sessions focus on scientific reasoning, data interpretation, and real discovery problems. Focused audience of specialists Sessions bring together GPCR researchers, pharmacologists, and discovery scientists. The conversation stays at the right level because everyone in the room speaks the same scientific language. Every session recorded Can't make it live? Every Masterclass is recorded and available on demand in the library. Revisit the science anytime — over 200 sessions and growing. On-demand library 200+ expert sessions, available anytime Full recordings of every Masterclass session. Revisit the science at your pace — filter by category, level, or instructor. Andrew Tobin How to Build Breakthrough GPCR Programs Sudarshan Rajagopal The Spatiotemporal Revolution in GPCR Biology Sam Hoare How Signaling Kinetics Shapes GPCR Drug Action Explore all Recorded Masterclasses → The scientists Learn directly from world leaders in GPCR research Andrew Tobin Marsha Pierce Terry Hébert Bryan Roth Matteo Pavan Terry Kenakin Jakob Höppner Samuel Hoare Yamina Berchiche Kenneth Jacobson Sudarshan Rajagopal What scientists say? From the people in the room Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere GPCR researcher Thank you for bringing this course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field GPCR researcher The content had enough depth to satisfy the hunger for theory while being full of practical knowledge GPCR researcher The best pharmacology teacher teaming up with the best GPCR community platform to help train and inspire the next generation of scientists. Also super-valuable for those of us learning how to teach pharmacology GPCR researcher Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him GPCR researcher Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. GPCR researcher The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work GPCR researcher About the GPCR Masterclass What is a GPCR Masterclass? The GPCR Masterclass is a live scientific discussion with a leading expert in GPCR pharmacology, receptor biology, or drug discovery. Sessions focus on research questions, experimental interpretation, and emerging challenges in GPCR science. Are the sessions live or recorded? Masterclass sessions are conducted live with an invited expert. After the event, recordings are added to the Masterclass course library, where Premium Members can access them on demand. Who should join? The Masterclass is designed for GPCR researchers, pharmacologists, and drug discovery scientists working in academia, biotech, and pharmaceutical research. Can I watch sessions later if I miss the live event? Yes. All sessions are recorded and available in the Masterclass course library for Premium Members. Can I watch sessions later if I miss the live event? Yes. All sessions are recorded and available in the Masterclass course library for Premium Members. How do I fit this in my schedule? You can attend the live discussion or watch the recording later. The Masterclass library allows members to revisit sessions at any time. What makes the Masterclass different from reading papers or textbooks? The Masterclass focuses on scientific interpretation and discussion. Experts explain how they think about pharmacological data, experimental design, and discovery challenges—insight that is rarely captured in publications. What happens during the live discussion? Each session begins with a focused presentation from the guest expert, followed by moderated discussion and questions from participants. The format allows deeper exploration of pharmacology concepts than typical conference presentations. Masterclass is included in Dr. GPCR University Live sessions, 200+ on-demand recordings, plus premium intelligence, jobs, events, and a community of GPCR scientists — all in one place. See what it feels like for 14 days. Try University for 14 days — $50 Your professional home in GPCR science. $499/year after trial.

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Advance your GPCR research career with Dr. GPCR University. Access 20+ on-demand GPCR courses, 200+ expert talks, weekly news, and a global scientist network. Join Premium today. Dr. GPCR University Your professional home in GPCR science. University is your professional home in GPCR science — premium intelligence, live Masterclasses, job listings, events, and a community of scientists who have your back. Everything you need, in one place. See what it feels like — $49 for 14 days Already know this is home? Join University — $499/year 1,400+ GPCR scientists reached 200+ Expert talks available $499 Per year — less than $10/week What's inside? The rooms in your professional home University isn't a bundle of features — it's a place where your GPCR professional life is supported. Here's what's waiting for you inside. Live Masterclass Live scientific exchanges with leading GPCR experts. You're in the room with the scientist, asking your question — not watching from the audience. Explore Live Masterclass → Job Listings GPCR-specific job opportunities curated for the community. Your next role is already here — opportunities find you when you're inside the ecosystem. Masterclass On Demand Full recordings of every session, available anytime. Revisit the science at your pace — over 200 expert talks in the library and growing. Explore Masterclass on Demand → GPCR Events A calendar of relevant conferences, meetings, and events in the GPCR field. Your next conference is already here. Premium Weekly News The complete GPCR intelligence — classified publications, industry news, job listings, and events calendar. Know what's coming before it becomes consensus. See Weekly News → Ask the Ecosystem The question you've been sitting on — someone in this ecosystem has the answer. A discussion forum where members share insights and get answers from the community. Live Masterclass In the room with the scientist, not watching from the audience Live scientific exchanges where you engage directly with leading GPCR experts. The question you've been holding — this is where you ask it. Dr. Dmitry Veprintsev | U. of Nottingham Postponed | Biophysical approaches to study orphan GPCR ligand binding and signalling June 18, 2026 Dr. Marsha Pierce | Midewestern University Introduction to GLP-1 pharmacology October 8, 2026 Dr. Jakob Höppner | Harvard University | MGH Subcellular Regulation of PTH1R Signaling Translational Pharmacology & Disease Models June 11, 2026 Explore Live Masterclasses → Who it's for? Whether you're just starting out or 20 years in — this is your place University is designed for GPCR scientists at every career stage who want to stay sharp, connected, and supported. 🎓 Early-career researchers Find your footing in the field. Access the experts, the intelligence, and the community that accelerates your growth. 🔬 Discovery scientists Stay at the frontier. Live Masterclasses and Premium Weekly News keep you ahead of the field — not chasing it. 🏆 Senior investigators Your career stage doesn't matter. Your commitment to the science does. Connect, contribute, and stay current. Explore the Masterclass On Demand Watch Now How to Build Breakthrough GPCR Programs Andrew Tobin Watch Now How Signaling Kinetics Shapes GPCR Drug Action Sam Hoare Watch Now The Spatiotemporal Revolution in GPCR Biology Sudarshan Rajagopal Explore Masterclasses On Demand → The comparison A society membership costs more and gives you less Most GPCR scientists belong to at least one scientific society. Here's how that compares to University. Typical Scientific Society $150 – $500+/year A journal subscription A conference discount A newsletter Occasional networking events Dr. GPCR University $499/year — less than $10 a week Live Masterclasses with leading GPCR scientists 200+ on-demand expert sessions Premium Weekly News intelligence GPCR job board and events calendar Community forum & ecosystem access Intelligence Hub dashboard Grandfather guarantee — your rate never increases "The one membership that has your back." $50 for 14 days - Strat Now What others are saying Scientists inside the ecosystem Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere GPCR researcher The content had enough depth to satisfy the hunger for theory while being full of practical knowledge GPCR researcher Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him GPCR researcher The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work GPCR researcher Thank you for bringing this course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field GPCR researcher The best pharmacology teacher teaming up with the best GPCR community platform to help train and inspire the next generation of scientists. Also super-valuable for those of us learning how to teach pharmacology GPCR researcher Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. GPCR researcher Common questions Thinking it over? Fair enough. Here are the concerns we hear most — and honest answers. "It's too expensive." At less than $10 a week, University gives you live access to leading GPCR scientists, 200+ on-demand talks, premium intelligence, a job board, events calendar, and a global community of peers. One insight, one connection, one 'aha' moment — can save months of research time. "I'm not sure I'll use it often." Even one Masterclass or one new collaboration can make a difference. Members often find value in ways they didn't expect — from expert feedback to career-changing introductions. That's why we offer a 14-day trial, so you can experience it first. "I already get what I need from papers." Papers inform. University helps you understand and apply that knowledge — through expert context, structured scientific exchanges, and real interaction with peers from academia and industry. "Will this really help my career?" Yes. Members grow visibility, confidence, and connections that open doors. It’s not just about learning — it’s about being seen, supported, and part of something bigger . Frequently asked questions What is Dr. GPCR University? Dr. GPCR University is an educational platform that provides in-depth learning and training resources on G protein-coupled receptors (GPCRs). At Dr.GPCR University, you’ll find: Courses: Dive deep into curated educational content designed by experts in GPCR research. Our courses provide comprehensive, on-demand learning to help you expand your knowledge and stay current in the field. Symposia Engage with leading scientists through our symposia, featuring in-depth discussions on cutting-edge research and breakthroughs in GPCR science. Each session brings together a community of experts to share insights and advancements. Summit A global gathering of researchers and professionals showcasing the latest developments in GPCR research. Participate in presentations, networking opportunities, and collaborative sessions. Virtual Café Listen to casual, interactive discussions with experts in the field. How do I register for Dr. GPCR University Masterclasses? To register for any course, you must have a FREE Ecosystem member account. We carefully screen anyone signing up to ensure they are real humans working on GPCRs, so you might not receive confirmation immediately. When signing up for the first time, try to complete as much information as possible about yourself. Who are the Dr. GPCR University Masterclasses designed for? The classes are designed for researchers, students, and professionals in biology, pharmacology, and biochemistry, but anyone interested in GPCR research is welcome to join. What topics are covered in the masterclasses? Masterclasses cover a variety of track including but not limited to pharmacology foundations, agonists, antagonists & core mechanisms , allosteric modulation & kinetics, advanced quantitative approaches and innovation & strategic application Can I register my team for a Dr. GPCR University Masterclasses? To register as a team, one of you must be a Premium Member. This person must email hello@drgpcr.org indicating how many people will register for the course, the names of the participants, and their emails. We will contact each person individually to help them set up a FREE Ecosystem Membership. They will be asked to join a private group to keep updated with the latest announcements about the course. Are the masterclasses on-demand or live? Dr. GPCR University offers both on-demand and live classes led by experts in the field. On-demand classes are only available for Premium Members. Do I need prior knowledge of GPCRs to join the masterclasses? Some classes may require basic knowledge of GPCRs, but many are designed to accommodate beginners as well as advanced learners. What kind of certification will I receive upon completing a masterclass? Participants will receive a certificate of completion from Dr. GPCR University, which can be used to showcase your expertise and enhance your professional credentials. Can I access the course material after completing the course? Yes, if you are a premium member. Move in. Look around. See if it's home. For 14 days, this is what it feels like to have everything in one place — intelligence, learning, community, and opportunities. Your first Masterclass is waiting. See what it feels like Already know this is home? Join University — $499/year Your 14-day trial is $50. If University feels like home, it's $499/year — less than $10 a week. Grandfather guarantee: your rate never increases. No surprise charges.

Advance your GPCR research with expert-led Masterclasses on pharmacology, efficacy, signaling, and drug discovery. Built for serious scientists. University / Masterclass On Demand Every Masterclass session. Anytime. At your pace. The full recording library of GPCR Masterclass sessions — revisit the science, catch what you missed, and explore topics at the depth they deserve. On-demand recordings are included inDr. GPCR University Try it for 14 days Recording library Explore the Masterclass library Full recordings of every Masterclass session. Filter by category, level, or instructor to find exactly what you need. Filter by Category Filter by Level Filter by Instructor Watch Now Andrew Tobin How to Build Breakthrough GPCR Programs Watch Now Terry Hebert GPCR Signaling in iPSC-Derived Cardiac Disease Models Watch Now Terry Kenakin Assessing Bias: The Practical Approach Watch Now Sudarshan Rajagopal The Spatiotemporal Revolution in GPCR Biology Watch Now Bryan Roth GPCR Molecular Glues: Biased Modulation at the Receptor–Transducer Interface Watch Now Terry Kenakin Unconventional GPCR Ligands Watch Now Sam Hoare How Signaling Kinetics Shapes GPCR Drug Action Watch Now Kenneth A. Jacobson, Matteo Pavan Structure-Based Design of Modulators of Purinergic GPCRs Watch Now Terry Kenakin Designing with Time: GPCR Ligand Kinetics 1 2 3 1 ... 1 2 3 ... 3 Topics covered Deep dives across the full scope of GPCR science Sessions span the entire landscape of GPCR pharmacology, from foundational principles to frontier research. Research Strategy Allosteric Modulation Allosteric Modulation & Kinetics Biased Signaling & Allosteric Modulation Structure-Based Drug Design Translational Pharmacology & Disease Models Advanced Quantitative Approaches Translational Pharmacology Innovation & Strategic Application The scientists Learn from world leaders in GPCR research Every session is led by a recognized expert with decades of experience in GPCR pharmacology and drug discovery. Andrew Tobin University of Glasgow Jakob Höppner Endocrine Unit, Massachusetts General Hospital and Harvard Medical School Marsha Pierce Midwestern University Samuel Hoare Pharmechanics LLC Terry Hébert McGill University Yamina Berchiche Dr. GPCR & Yamina's Corner Bryan Roth UNC Chapel Hill Medical School Kenneth Jacobson NIH Matteo Pavan NIH Sudarshan Rajagopal Duke University School of Medicine Terry Kenakin Terry's Corner How it works? Your library. Your pace. 1 Browse or search Filter by scientific category, instructor, or level. Find the session that matches what you're working on right now. 2 Watch at your pace Full recordings with no time limits. Pause, rewind, revisit. The science is here whenever you need it. 3 Go deeper Join the next live Masterclass to ask your questions directly. The recordings are the foundation — the live sessions are where you go further. Want to be in the room live? Live Masterclass sessions run regularly with interactive Q&A. See what's coming up next. See live sessions → What others are saying Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere GPCR researcher Thank you for bringing this course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field GPCR researcher The content had enough depth to satisfy the hunger for theory while being full of practical knowledge GPCR researcher The best pharmacology teacher teaming up with the best GPCR community platform to help train and inspire the next generation of scientists. Also super-valuable for those of us learning how to teach pharmacology GPCR researcher Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him GPCR researcher Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. GPCR researcher About the GPCR Masterclass What is a GPCR Masterclass? The GPCR Masterclass is a live scientific discussion with a leading expert in GPCR pharmacology, receptor biology, or drug discovery. Sessions focus on research questions, experimental interpretation, and emerging challenges in GPCR science. Are the sessions live or recorded? Masterclass sessions are conducted live with an invited expert. After the event, recordings are added to the Masterclass course library, where Premium Members can access them on demand. Who should join? The Masterclass is designed for GPCR researchers, pharmacologists, and drug discovery scientists working in academia, biotech, and pharmaceutical research. Can I watch sessions later if I miss the live event? Yes. All sessions are recorded and available in the Masterclass course library for Premium Members. Can I watch sessions later if I miss the live event? Yes. All sessions are recorded and available in the Masterclass course library for Premium Members. How do I fit this in my schedule? You can attend the live discussion or watch the recording later. The Masterclass library allows members to revisit sessions at any time. What makes the Masterclass different from reading papers or textbooks? The Masterclass focuses on scientific interpretation and discussion. Experts explain how they think about pharmacological data, experimental design, and discovery challenges—insight that is rarely captured in publications. What happens during the live discussion? Each session begins with a focused presentation from the guest expert, followed by moderated discussion and questions from participants. The format allows deeper exploration of pharmacology concepts than typical conference presentations. 200+ sessions are waiting for you inside University The full on-demand library, plus live Masterclasses, premium intelligence, jobs, events, and a community of GPCR scientists — all in one place. See what it feels like... Try University for 14 days — $50

Explore detailed information about our GPCR-focused University Courses. Learn about course content, instructors, and how to advance your expertise in drug discovery. Empower. Connect. Transform. Become part of the Dr. GPCR University Instructor community—where teaching is more than sharing knowledge; it’s about uplifting scientists and advancing GPCR discovery, together. Connecting scientists through knowledge, passion, and purpose. About Dr. GPCR University Dr. GPCR University is a global platform where scientists share their knowledge, inspire discovery, and advance GPCR research together. Our on-demand courses connect experts, students, and industry professionals through authentic, instructor-led learning—built by scientists, for scientists. Each contribution brings new perspectives and tools to advance the field. Instructors are recognized and compensated for their work, ensuring that every shared insight creates impact, visibility, and lasting value across the GPCR community. Course Formats You Can Teach At Dr. GPCR University , every instructor brings a unique voice, style, and rhythm to teaching. Our flexible course formats are designed to fit your time, depth, and teaching goals — whether you’re sharing a focused insight or leading a full exploration of GPCR science. You can also co-lead Full-Length Courses with up to three fellow instructors to share the workload and enrich the learning experience. 🧭 Full-Length Course Structure: 4 × 1-hour sessions Purpose: Deep, multi-session learning experience Best for: Comprehensive topics that require exploration and discussion ⚡ Short Course Structure: 1 session (2–4 hours of content) Purpose: Concise yet thorough coverage of key concepts Best for: Core methods, applied principles, or emerging topics 🔍 Mini Course Structure: 1 short lesson (1–2 hours of content) Purpose: Focused insights into a single theme Best for: Quick takeaways or specialized topics No matter the format, your course helps scientists learn, connect, and keep GPCR science moving forward — one discovery at a time. Instructor Benefits At Dr. GPCR University , we believe those who teach move science forward. As an instructor, you’re not just sharing knowledge — you’re shaping the next generation of GPCR scientists. We make sure your time, expertise, and contribution are recognized and supported every step of the way. 🌟 By teaching with us, you gain: ✔ Premium Membership for you and your team for one year (no credit card required) ✔ A global platform to share your expertise and reach scientists worldwide ✔ Full support with technical setup, editing, and course promotion — so you can focus on teaching We handle logistics so you can focus on what truly matters: delivering meaningful, high-quality education. To ensure lasting impact, each course becomes part of the Dr. GPCR University ecosystem — maintained, updated, and accessible to learners in the long term. Your name and expertise remain at the heart of the course, continuing to inspire scientists long after the sessions end. Together, we’re shaping the future of GPCR education — one course, one scientist, one discovery at a time. What You’ll Need to Provide to Teach a Course Welcome — we’re thrilled to have you join Dr. GPCR University . You bring the expertise; we’ll handle the setup, editing, and promotion. Here’s everything you’ll prepare to bring your course to life: 🧩 Step 1: Email us Start by emailing it us at Hello@DrGPCR.org . We will then have a short call and send you the our Instructor Intake Form — it’s how we build your profile and course page. You’ll be asked for: Instructor info – name, email, affiliation, short bio, photo, and optional social media handles. Course details – title, format (short talk / mini-course / series), audience, main objectives, expected learning outcomes, key topics (≈ 250 words), recommended readings, and any co-instructors. Preferences & agreement – communication style, access to the Premium area, and acknowledgment of the instructor agreement (you’ll receive the full version right after submission). 🧱 Step 2: Plan Your Course Structure Decide how your course will flow — number of modules, duration, and teaching style. (See Course Formats above for ideas.) 🕙 Scheduling note: Courses are typically hosted Thursdays at 10 AM EST — a sweet spot for our global community. We’ll confirm your date together once your proposal is approved. 📝 Step 3: Prepare Your Content Create your teaching materials — slides, visuals, readings, or anything that helps learners grasp your message. Don’t worry — we’ll support you with templates and review tips along the way. 🎥 Step 4: Record a Short Video Chat You’ll have a quick recorded conversation with Dr. Yamina Berchiche about your course — what it covers, why it matters, and what students can expect. It’s relaxed, engaging, and helps introduce you to the community. 💬 Step 5: Join Your Private Course Group Once live, you’ll connect with your students in a private discussion space — perfect for questions, insights, and follow-ups. 💫 Step 6: Teach & Inspire Share your expertise with scientists around the world. Enjoy the experience, the visibility, and the impact — and receive recognition and compensation for your contribution. (See Instructor Benefits for details.) ✨ Your ideas, your voice, and your course will help shape the next chapter of GPCR discovery. Share Your Expertise with the World We’re here to support you from idea to impact. Start your journey as a Dr. GPCR University Instructor and help move GPCR science forward. Email us at Hello@DrGPCR.org Live Masterclass Sessions Previous Instructors Andrew Tobin Marsha Pierce Terry Hébert Bryan Roth Matteo Pavan Terry Kenakin Jakob Höppner Samuel Hoare Yamina Berchiche Kenneth Jacobson Sudarshan Rajagopal Dr. GPCR Courses Reviews Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere GPCR researcher Thank you for bringing this course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field GPCR researcher The content had enough depth to satisfy the hunger for theory while being full of practical knowledge GPCR researcher The best pharmacology teacher teaming up with the best GPCR community platform to help train and inspire the next generation of scientists. Also super-valuable for those of us learning how to teach pharmacology GPCR researcher Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him GPCR researcher Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. GPCR researcher The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work GPCR researcher Contact Contact us First name* Last name Email* Write a message Submit

Strategic approaches to building GPCR research programs that translate fundamental discoveries into clinical impact and drug development. < Back How to Build Breakthrough GPCR Programs June 4, 2026 10 AM - 11:30 AM EST 🔒 Watch Recordings - Join Premium Access the full library of recorded Masterclass sessions. Get Live Updates Be notified when new live Masterclasses are scheduled. Introduction Building GPCR research programs that achieve both fundamental discovery and clinical translation requires strategic thinking from day one. This session addresses the structural and strategic decisions that determine whether breakthrough science reaches patients: securing funding aligned with translational potential, defining research directions that balance risk and impact, identifying discoveries worth pursuing to clinical endpoints, and navigating the pathway from academic research to drug development and spin-out companies. Andrew Tobin draws from his experience leading translational GPCR programs and co-founding Keltic Pharma to illustrate each strategic element. Intended for GPCR scientists, postdocs, and research leaders planning translational research programs. Instructor Andrew Tobin directs translational GPCR research focused on generating new medicines for brain disorders, severe asthma, and inflammatory gut disease. As co-founder and CEO of Keltic Pharma Therapeutics, he leads a biotechnology company developing a novel drug-discovery platform and working toward a radical cure for malaria. He also serves as Director of the Advanced Research Centre at the University of Glasgow, a £130M collaborative initiative housing over 550 researchers designed to redefine interdisciplinary research. His recent work on muscarinic acetylcholine receptor modulation and structure-guided design of M1 receptor agonists exemplifies the strategic approach to translational GPCR science that defines this Masterclass session. Upcoming Live Sessions

Beatriz Blanco-Redondo on characterizing unknown adhesion GPCRs in Drosophila - receptor discovery, nocifensive behavior, and human disease links. << Back to podcast list Strategic Partner(s) Beatriz Blanco-Redondo: Adhesion GPCR Discovery in Drosophila Adhesion GPCRs are among the least characterized receptor families in the human genome - and in Drosophila melanogaster, three of the five known adhesion GPCRs had no documented function, expression pattern, or signaling profile when Beatriz Blanco-Redondo's group began working on them. The receptors were named after condiments - ketchup, mayo, and remulate - not out of irreverence, but because no functional data yet existed to guide any other kind of nomenclature. Blanco-Redondo, group leader at the University of Leipzig, uses CRISPR engineering, epitope tagging, and in vivo behavioral assays to build the first systematic characterization of these receptors from the ground up. Her primary focus is remulate - a neuronal adhesion GPCR with a human ortholog linked to vascular malformations and blood-brain barrier dysfunction in vertebrate models. The fly system makes it tractable: new lines in weeks, knockouts in months, and behavioral readouts that connect receptor loss to nocifensive phenotypes in larvae. For Blanco-Redondo, the pull toward this work is not abstract. Remulate is the receptor she secured funding to study, the one her first PhD student built an entire project around, and the one that still does not have a complete localization map. This conversation covers what it looks like to do receptor biology when you are writing the first chapter - with no antibodies, no prior literature, and no established toolkit to fall back on. About the Guest Beatriz Blanco-Redondo is a group leader in the Department of Biochemistry at the University of Leipzig, where she studies adhesion GPCRs in Drosophila melanogaster. Her research focuses on characterizing the localization, signaling, and in vivo function of previously unknown adhesion receptors in the fly nervous system and gut. She trained in protein biochemistry and neuroscience, completing her PhD in Germany and her postdoctoral work at Columbia University, where she worked on ALS models using mouse systems. Since returning to Europe, her research has centered on receptor biology at the intersection of basic discovery and translational relevance. Scientific Themes of the Conversation First-contact receptor characterization - what it means to study a GPCR with no prior functional data Genetic tools for adhesion GPCR research in Drosophila - CRISPR, epitope tagging, and knockout strategies The logic of model organism selection - speed, genetic tractability, and translational value Nocifensive behavior as a readout for neuronal receptor function in larvae Human ortholog connections - from fly adhesion GPCRs to vertebrate vascular and neurological disease Career decisions in academic science - uncertainty, reentry, and the conditions that keep scientists in the lab Key Insights from the Conversation 1. Three adhesion GPCRs in Drosophila were functionally unknown until recently When Blanco-Redondo's group began this work, five adhesion GPCRs were known in the fly - but only two had any functional characterization. The other three had no documented expression pattern, signaling data, or phenotype. The approach was systematic: generate knockouts, introduce epitope tags, observe what breaks, and build the picture from scratch. There was no shortcut available because there was no prior literature to build on. 2. Naming receptors after condiments signals where the field actually stands Ketchup, mayo, and remulate were named in the absence of functional data that would normally guide nomenclature. It is a small detail, but it marks something real about the state of adhesion GPCR biology in insects: these receptors exist in a space where the biology precedes the vocabulary. The playfulness of the naming reflects the honesty of the situation. 3. Remulate connects fly neuroscience to human vascular and neurological pathology In the peripheral nervous system of Drosophila larvae, loss of remulate disrupts nocifensive behavior - the animal's response to aversive stimuli. The human ortholog has been associated with vascular malformations and blood-brain barrier dysfunction in vertebrate models. That thread, from a behavioral assay in a fly larva to a clinical phenotype in mice, is what gives the model system its translational justification. 4. Antibody limitations drive the methodological design Because the antibody landscape for adhesion GPCRs is sparse - and largely underdeveloped for fly receptors - Blanco-Redondo's group relies on CRISPR-introduced epitope tags to track receptor localization in vivo. This is not a workaround. It is a deliberate strategy that delivers spatial resolution that antibody-based approaches cannot offer for these targets at this stage of the field. 5. Drosophila generations close the experimental feedback loop A new fly line is ready in one to two weeks. A knockout can be generated and validated in two to three months. For receptor biology that requires iterative genetic manipulation - knocking out, tagging, rescuing, observing - this compression of experimental time changes which questions are tractable within a single grant period. It is not incidental to the science; it is part of the scientific logic. 6. Reconsidering a career is not the same as leaving science Blanco-Redondo describes a period after returning from New York when she was genuinely uncertain about continuing in the lab. The decision to stay came from a specific opportunity, a specific mentor, and a specific set of questions she hadn't yet answered. It did not resolve into a clean narrative. It was uncertain, and she says so plainly. 7. Negative results need infrastructure, not just tolerance Blanco-Redondo and Yamina discuss the cost of unpublished negative data - particularly for PhD students working within three-year funding windows. The argument is not sentimental. If a failed approach were citable, it would shorten the path for the next researcher attempting the same thing. Some journals are beginning to accept negative data, and both agree this matters structurally. Episode Timeline Timestamps are AI-generated from the transcript and may not reflect the final edited episode precisely. Verify against the published video before use. 00:00 - Sponsor intro: GeneTex and Eurofins DiscoverX 00:29 - Introduction of Beatriz Blanco-Redondo; icebreaker 01:15 - Career path: from Spain to Germany, and the decision to go further 05:57 - Dr. GPCR University mid-roll 06:17 - Life in New York; comparing research cultures across continents 08:30 - How adhesion GPCRs entered the picture, and the shift toward receptor biology 11:49 - Research program in Leipzig: three unknown adhesion GPCRs in Drosophila 13:57 - Naming remulate, ketchup, and mayo; why remulate became the primary focus 15:47 - Lab methods: CRISPR, epitope tagging, colony generation timelines 17:29 - Behavioral and phenotypic readouts; nocifensive responses in larvae 18:48 - The human ortholog of remulate and connections to vascular and neurological disease 22:58 - What first-contact receptor characterization actually looks like 26:02 - Career turning points; uncertainty on returning from the US 33:25 - Advice for scientists working on adhesion GPCRs and difficult model systems 35:26 - The case for publishing negative results; pressure on PhD timelines 40:54 - Upcoming GPCR conferences in Leipzig and Dusseldorf Selected Quotes "It's like there's nothing known at all about this receptor. And then you come into play and piece by piece you try to put the pieces together - it's like a puzzle. And then at the end, you can discover what a receptor that was there in the fly - nobody ever checked what it's doing." "When I moved back from the US, I was not sure I wanted to continue in science. Thanks to Toby, that gave me a position here, and I could stay. Yeah, I'm still here - so it means that I enjoy it." "You come from disease and then you're working on a receptor and you want to study what happens there. But then to see all the possibilities that this offers - that was also great." "Don't give up, because it's your passion, it's your job. We love what we do. And we have a lot of friends who don't like what they are doing. And this is very important." Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

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Dr. Paul Insel explains how unbiased GPCR expression profiling uncovered overlooked receptors in cancer — and why the field may need to rethink which GPCRs matter most. << Back to podcast list Strategic Partner(s) Paul Insel: Unbiased Discovery and the GPCRs We've Been Missing The GPCR field has produced thousands of studies on a small number of well-characterized receptors. But what if the ones that matter most in human disease are the ones we haven't prioritized? Dr. Paul Insel's lab at UC San Diego has pursued this question using unbiased expression profiling — GPCR arrays, RNA-seq, and single-cell analysis — to catalog which receptors are actually highly expressed across human tissues and disease states. In pancreatic cancer, proton-sensing GPCRs such as GPR68 are dramatically upregulated in cancer-associated fibroblasts, creating feedback loops between the tumor microenvironment and stroma that may drive disease progression. Across 45 cancer types, numerous GPCRs show elevated expression without corresponding mutations — a pattern the mutation-centric oncology paradigm has largely missed. For Dr. Insel, this shift began with a single dataset — a postdoc's unbiased expression profile showing the most abundant receptor in a normal human cell type had almost no literature behind it. Listeners will gain perspective on how asking broader questions about receptor biology can reshape drug discovery priorities. About the Guest Dr. Paul Insel is Distinguished Professor of Pharmacology and Medicine at the University of California, San Diego. His research spans four decades of GPCR signaling, from cyclic AMP and adrenergic receptor biology to purinergic receptors and, most recently, proton-sensing GPCRs in the tumor microenvironment. His lab combines bioinformatic analysis of GPCR expression across human cancers with wet-lab validation in animal models, particularly in pancreatic cancer. Dr. Insel also directs UCSD's MD-PhD Medical Scientist Training Program, a role he has held for over 30 years. Scientific Themes of the Conversation Unbiased receptor discovery — Why hypothesis-free expression profiling reveals GPCRs that decades of targeted research missed GPCRs in the tumor microenvironment — Proton-sensing receptors, cancer-associated fibroblasts, and the role of low pH in tumor signaling Drug repurposing through receptor mapping — Identifying already-approved drugs that target overexpressed GPCRs in cancer Reductionism vs. native cell biology — The limits of studying purified components and the case for understanding receptors in intact cellular environments Biased signaling in practice — Why the promise of biased agonism is more complicated than the field hoped Breadth as a scientific strategy — How reading across disciplines and resisting premature narrowing drives discovery Key Insights from the Conversation 1. The biggest discoveries came from asking what was being overlooked Dr. Insel's late-career pivot began with a deceptively simple question: are we studying the right GPCRs? When his lab ran unbiased expression profiles on normal human cells, the most highly expressed receptor — PAR1 — had almost no functional literature behind it. Nature had placed it at the top; science had barely looked. 2. Proton-sensing GPCRs create a feedback loop in pancreatic cancer GPR68 is dramatically upregulated in cancer-associated fibroblasts — not the cancer cells themselves. The tumor signals fibroblasts to raise GPR68 expression, and the low pH of the tumor microenvironment then activates that receptor, which signals back to promote cancer survival. It is a positive feedback loop that exploits the acidic environment tumors naturally create. 3. GPCRs are overexpressed across dozens of cancers — without mutations A large bioinformatic study from Dr. Insel's lab examined GPCR expression across 45 human cancer types and found widespread over expression without corresponding increases in copy number or mutation frequency. This challenges the mutation-centric framework that dominates oncology and suggests GPCRs may contribute to pathophysiology through expression changes alone. 4. The field's reductionism may be hiding how receptors actually work Dr. Insel has long argued that purifying receptors, depleting GTP, and stabilizing conformations through mutations teaches us about components — not about how cells actually use them. He compares the biochemist's approach to smashing a television with a wrecking ball and trying to reassemble the pieces to understand how it works. 5. Biased signaling is real but harder to exploit than expected GPR68 couples to both Gq and Gs, and the functional effects in cancer-associated fibroblasts appear to run primarily through Gs. In principle, biased antagonists could selectively block the disease-relevant pathway. But Dr. Insel is cautious — signaling bias operates on a conformational continuum, and clinical translation has not yet matched the elegance of the concept. 6. A career redirected by a dinner and an empty schedule In 1975, Dr. Insel was the only unmarried scientist at a dinner with Al Gilman. The group needed someone to visit Gilman's lab to learn radioligand binding — and he was the one with nothing else to do. That accidental assignment launched a career in GPCR signaling that has now spanned over four decades. 7. The "unknown unknowns" should change how we fund and train scientists Dr. Insel believes the training system pushes young researchers to narrow too early, at the cost of the cross-disciplinary thinking that leads to real discoveries. His own career has been shaped by reading broadly and importing ideas from other fields — a strategy he sees as increasingly essential as GPCR biology intersects with cancer, immunology, and systems biology. Episode Timeline 00:00 Introduction and context 01:08 Dr. Insel's path from medicine to molecular pharmacology 05:15 The origin story — dinner with Al Gilman and the start of a GPCR career 09:06 Evolving receptor loves: from adrenergic to purinergic to proton-sensing GPCRs 13:19 Proton-sensing GPCRs: what they are and why they matter 16:18 GPR68 and the feedback loop in pancreatic cancer 19:46 Challenges of targeting GPCRs in oncology — funding, skepticism, and the mutation paradigm 25:05 AI, in silico screening, and the limits of computational drug discovery without structures 31:33 Biased signaling: promise, complexity, and caution 35:00 The case against reductionism — why native cell biology matters 38:05 Advice for young scientists: think broadly, resist narrowing too fast 42:14 Aha moments — the data that changed the direction of a lab 47:30 The future of the GPCR superfamily and the work still to be done Selected Quotes "I said, which receptors are the highest expressed? And the answer was PAR1, the thrombin receptor. So I did what anyone would do — I looked up what's known about it. And the answer was nothing." "We don't know what we don't know. And I think that's been a real driver for how I've approached the last several years of my scientific effort." "If you ask a biochemist how does a television work, he would probably take a wrecking ball to it and then try to piece all the little parts back together." "Nature decided, for reasons that none of us will ever probably know for sure, that GPCRs should be the largest receptor membrane family. And there's still a lot to be learned." About this episode In 1975, Dr. Paul Insel was at the FASEB experimental biology meeting in Atlantic City. During dinner with colleagues and Alfred Gillman , co-recipient of the 1994 Nobel Prize in Physiology or Medicine for their discovery of G-proteins and their role in signal transduction in cells, Paul was designated to go to Gillman’s lab . That summer, he used radioligand binding methods to dissect receptor function from the adenylyl cyclase activated by ligands, including adrenaline. From that point on, Paul was hooked and has since studied receptor function in human physiology, receptor molecular pharmacology in cells, and animal models, and as he puts it has now he’s "gone full circle" back to studying GPCRs important in human pathophysiology. Today, Paul and his team focus on previously unrecognized receptors with the hopes to use these as novel drug targets. Dr. Paul Insel on the web Insel Laboratory Institute of Engineering in Medicine UC San Diego UCSD Profiles Google PubMed Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Vaithish Velazhahan About Vaithish Velazhahan Vaithish obtained dual bachelor’s degrees with honors in Medical Biochemistry and Microbiology from Kansas State University, USA. His undergraduate thesis work on studying the biochemical mechanisms of flavonoids in cancer using nuclear magnetic resonance spectroscopy (NMR) led to a Barry M. Goldwater Scholarship. He then received a prestigious Gates Cambridge Scholarship to study for a Ph.D. at the MRC Laboratory of Molecular Biology and the University of Cambridge, where he is currently a final year Ph.D. candidate. His Ph.D. work has been focused on understanding the structure and activation of Class D fungal GPCRs. He has developed novel tools and methodologies to study fungal GPCRs which allowed the determination of the first structures of the prototypical fungal GPCR Ste2. This work has led to two first-authored manuscripts published in the journal Nature. Vaithish has been recognized with the MRC LMB's Max Perutz Prize for outstanding Ph.D. work and has been elected a Research Fellow at Gonville and Caius College, which is one of the most prestigious positions at the University of Cambridge. Vaithish Velazhahan on the web Twitter GatesCambridge PubMed Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. John Janetzko About Dr. John Janetzko "I received my Honors BSc in Chemistry from the University of Toronto in 2011, with a focus on synthetic organic and inorganic chemistry. Following this, I pursued graduate studies in Chemistry at Harvard University. At Harvard, I worked in the labs of Drs. Daniel Kahne and Suzanne Walker studying the structure and function of the essential human enzyme, O-GlcNAc transferase (OGT). My Ph.D. work focused on understanding the mechanism of an enigmatic moonlighting function of OGT that had been described only a year earlier. Over the course of my graduate work, I gained experience with structural mass spectrometry and protein crystallography, which shaped my interest in understanding how protein dynamics are linked to function. To further develop these ideas, I joined the lab of Dr. Brian Kobilka at Stanford University at the end of 2017 for postdoctoral work. There, I’ve been working towards understanding the molecular basis of G protein-coupled receptor desensitization and trafficking. My postdoc work has made use of several techniques including various mass spectrometry approaches, single particle cryo-EM and single-molecule fluorescence spectroscopy. In July 2024 I will join the University of Colorado, Anschutz Medical Campus, as an Assistant Professor in the Department of Biochemistry and Molecular Genetics. Besides research, I am passionate about teaching, science communication and making research more inclusive and welcoming. Outside of the lab, I am an avid bike racer, an occasional cycling coach, and I enjoy spending time with my wife, son, and Bernedoodle." Dr. John Janetzko on the web Stanford University Stanford Medicine Google Scholar Personal Website ResearchGate LinkedIn Twitter Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick recap In their conversation, Yamina and John discussed crafting social media posts for John's scientific content. They also shared their respective backgrounds and future plans, with John planning to start his own lab at the University of Colorado School of Medicine. John shared his journey into science, from his interest in creative fields to his involvement in the Chemistry Olympiad and subsequent academic pursuits. The conversation also touched on the challenges of applying for academic positions in the US, the importance of adaptability in one's career, and the potential benefits of networking and mentorship. Next steps • Yamina will share ideas on supporting John's new academic position after the recording stops. • John will prioritize getting feedback from people outside his lab to structure his job seminars. Summary Social Media Post Crafting for GPCRs Yamina and John discussed crafting social media posts for John's scientific content. Yamina emphasized that the content should be kept in a PG-13 context and be scientifically related to GPCRs. John expressed his comfort in sharing his stories and agreed to follow Yamina's guidelines. They also discussed their respective backgrounds and John's future plans to start his own lab at the University of Colorado School of Medicine. John shared his journey into science and his initial interest in creative fields. John's Chemistry Olympiad Journey John shared his experiences in high school, where he developed a keen interest in advanced physics and math curriculum. He participated in various academic competitions, including math, physics, and chemistry contests. John explained that he was drawn to chemistry because it allowed him to build things in his mind and design them. He discovered the National Chemistry Olympiad and was selected to attend a provincial training camp at the University of Toronto. This led to his participation in the National Training Program in Quebec City and his selection to represent Canada at the Chemistry Olympiad in Moscow, Russia. John also mentioned his university application process, which was less stressful than the US system. Yamina shared her own experiences with applying to universities in Canada and the US. John's Chemistry Olympiad and GPCR Journey John shared his experience with the Chemistry Olympiad program, highlighting its rigorousness and advanced content that exceeds typical high school curriculums. He also reflected on his journey from his early involvement in a university chemistry lab to his current interest in graduate school, inspired by the innovative approach of using chemistry to understand and build tools for biology. Yamina sought clarification on John's involvement with GPCRs, but the transcript ended before he could respond. John's Scientific Journey and Lab Collaboration John discussed his scientific journey, starting with a project in Suzanne Walker's lab focusing on the essential mammalian protein O-GlcNAc transferase. He then moved to Dan's lab where he met Suzanne and her project. Towards the end of his PhD, John became interested in understanding how proteins operate as large macromolecular machines and decided to work on memory proteins. He chose Brian's lab due to his interest in studying conformational changes. John shared his experience of reaching out to and securing a position in Brian's lab. He detailed his initial email contact, the subsequent Skype meeting, and the in-person visit that led to his acceptance of the position. John also discussed the potential complications that arose when his then-girlfriend, now wife, was applying for residencies. Ultimately, John did join the lab after his girlfriend successfully matched at Stanford. John explained the collaborative culture in Brian's lab, where individuals are encouraged to pursue projects aligned with their interests. He shared his experience working on a project involving receptor kinases and collaborating with other postdocs in the lab to develop assays and improve the biochemistry of certain targets. The conversation emphasized the importance of diverse backgrounds and skill sets in tackling complex challenges and finding solutions. Academia vs. Industry: Career Progression Discussion Yamina and John had a detailed discussion about the prospects of staying in academia versus transitioning to biotech or industry. John shared his thoughts about the great science happening in other sectors and how the decision largely depended on the opportunities presented. Yamina agreed and sought advice from John on career progression in academia. John suggested building milestones and landmarks into a postdoc, such as applying for funding opportunities, and getting diverse feedback to effectively present work. The conversation ended with Yamina asking when a postdoc should start considering their next steps in their career. Academic Position Applications and Transition Preparation John and Yamina discussed the extensive process of applying for academic positions in the US. John suggested starting preparations a year to two years ahead due to the time needed to develop ideas, write proposals, and get feedback. They also highlighted the need for mentorship and networking in finding job opportunities. Yamina questioned whether universities adequately prepare postdocs for the transition to industry or academia, suggesting a detailed manual or guide might be helpful. Both agreed on the importance of adaptability, as unexpected situations like the Covid-19 pandemic can affect the job searching process. John shared his experiences, stating that he submitted approximately 35 to 40 applications and that the interview process is time-consuming. Career Choices and Support in Academia John shared his positive experiences from job interviews and forming friendships with colleagues at various institutions. He also discussed the challenges of choosing between job offers, including considering his wife's career, her family's location in Denver, and other factors like monetary package and colleagues. John emphasized that negotiating salary is often not possible due to strict regulations. Yamina suggested having round tables to discuss these topics. John then reflected on his career, sharing key moments of realization in his scientific work and his upcoming transition out of his lab. The conversation concluded with both John and Yamina expressing a desire to support the academic community in various ways. Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Neil Grimsey About Dr. Neil Grimsey " During my postdoctoral studies at USCD, I discovered a novel GPCR-dependent atypical kinase activation mechanism that drives vascular edema and inflammation. These studies shaped my future goals as an Assistant Professor in the College of Pharmacy at the University of Georgia Athens. My group studies the spatiotemporal dynamics of atypical inflammation and the control of disease progression. We have developed an array of fluorescent biosensors to map kinase activity in living cells and are exploring innovative techniques to delineate the molecular dynamics of atypical p38 and suppress kinase activation. To further define the role of atypical p38 signaling responses we are studying how atypical p38 controls the onset and pathogenesis of acute lung injury, retinal vasculopathies, and infections. " Dr. Neil Grimsey on the web LinkedIn University of Georgia Google Scholar X (Twitter) Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Sudarshan Rajagopal About Dr. Sudarshan Rajagopal Dr. Sudarshan Rajagopal obtained his B.S. in Chemistry from The University of Chicago in 1998. He subsequently enrolled in the Medical Scientist Training Program at The University of Chicago. During his doctoral work in the lab of Prof. Keith Moffat, he studied the structural mechanisms of bacterial photoreceptors using time-resolved Laue crystallography. He was awarded his Ph.D. in 2004 and his MD in 2006. He then joined the Internal Medicine Residency training program at Duke University Medical Center. During his Cardiology fellowship, he trained in the lab of Dr. Robert J. Lefkowitz , where his research focused on biased agonism, with the development of approaches to quantify ligand bias and the identification of beta-arrestin-biased receptors. After completing his training in clinical cardiology, he started as an Assistant Professor of Medicine at Duke University School of Medicine. The main focus of his lab’s research is on the mechanisms underlying biased agonism at chemokine receptors and how that contributes to inflammation. The chemokine system is relatively unique in having multiple receptors and multiple ligands that display considerable promiscuity for one another. His group and others have shown that many of these ligands act as biased agonists for the same receptor. His lab is also interested in identifying novel signal transduction mechanisms of GPCRs, such as the formation of complexes between G proteins and beta-arrestins. His clinical focus is on pulmonary arterial hypertension, a disease of the pulmonary arterioles that causes right heart failure, and he serves as co-director of the Duke Pulmonary Vascular Disease Center. Dr. Sudarshan Rajagopal on the web LinkedIn Website Google Scholar LinkedIn Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Steve McCloskey About Steve McCloskey Steve McCloskey is an Alumni from the first class of Nanoengineering at the University of California, San Diego. Steve’s work is focused on emerging technologies applied to Science, Technology, Engineering, and Mathematics (STEM). During his time at UC San Diego Steve worked directly with the founding Chair of the Nanoengineering Department, Ken Vecchio helping set the foundation for the Nanoengineering Materials Research Center and developing thermodynamic processing methods for Iron-based Superelastic alloys. After graduating from UCSD he founded Nanome Inc to build Virtual Reality solutions for Scientists and Engineers working at the nanoscale, specifically protein engineering and small molecule drug development. Steve McCloskey on the web Website LinkedIn Twitter ResearchGate Medium Orchid Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Sudha Shenoy About Dr. Sudha Shenoy Dr. Sudha Shenoy is currently an Associate Professor in Medicine & Cell Biology in the Division of Cardiovascular Medicine, Duke University Medical Center. She received her Ph.D. from Oklahoma State University and completed her postdoctoral training with Dr. Robert J. Lefkowitz (Nobel Laureate, 2012) at Duke University. Dr. Shenoy’s postdoctoral research discovered that ubiquitination of mammalian G protein-coupled receptors is a tag for lysosomal degradation, whereas ubiquitination of the adaptor protein, β-arrestin, is a tag for receptor internalization and formation of signaling endosomes. Her laboratory has continued to work on identifying the molecular mechanisms that ascribe ubiquitin code on GPCRs and β-arrestins. Current efforts aim to understand the regulation of GPCR and beta-arrestin signaling in the heart and vascular endothelium by the deubiquitinating enzymes USP20 and USP33. Dr. Sudha Shenoy on the web Duke University Personal Reflections and Words of Wisdom: Story From Dr. Sudha Shenoy LinkedIn Pubmed Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Gloriam on orphan GPCR biology, GPCRDB, biased signaling, and how the data analysis bottleneck is reshaping receptor pharmacology and drug discovery. << Back to podcast list Strategic Partner(s) David Gloriam: Orphan Receptors, GPCRDB, and the Data Revolution in GPCR Pharmacology GPCRs represent the largest and most pharmacologically important family of membrane receptors, yet a significant portion remain orphans - proteins whose endogenous ligands and physiological roles are still unknown. This conversation explores the intersection of computational biology, cheminformatics, and structural pharmacology through the work of David Gloriam, whose career spans the identification of 26 novel human GPCRs from genome sequence data to the development of GPCRDB, a community resource used by more than 4,400 researchers monthly. Gloriam's research addresses a central challenge in the field: how to move from a bare protein sequence to a pharmacologically characterized receptor with identified ligands, a determined structure, and a plausible role in physiology. The conversation covers the de-orphanization of GPR139 and GPR55, the unresolved promise of biased agonism as a strategy for safer drug development, and the concept of data-accelerated receptor evolution as a framework for engineering receptor-ligand interactions at the residue level. For Gloriam, this work began with a grandmother's cancer diagnosis and an early determination to develop drugs - a goal that led him through the human genome and into a decades-long pursuit of receptors whose functions remain to be written. ABOUT THE GUEST David Gloriam is a professor at the University of Copenhagen's Department of Drug Design and Pharmacology, where he leads a multidisciplinary research group working across data science, computational drug design, pharmacology, and structural biology. His primary research focus is orphan GPCR biology, with particular emphasis on identifying endogenous ligands and physiological roles for receptors discovered during the human genome sequencing era. He maintains and develops GPCRDB, a continuously updated database and tool platform that integrates structural, functional, and ligand data for the entire GPCR superfamily. His group contributed to the de-orphanization of GPR139 and GPR55, including the identification of sub-nanomolar peptide ligand candidates, and has published widely on computational approaches to GPCR drug discovery and receptor classification. SCIENTIFIC THEMES OF THE CONVERSATION Orphan GPCR biology - the challenge of connecting a protein sequence to a physiological function GPCRDB as community infrastructure for integrating and accelerating GPCR research The interdisciplinary de-orphanization pipeline: from bioinformatics to pharmacology to structure The data interpretation bottleneck - how the field's rate-limiting step has fundamentally shifted Biased agonism: from theoretical framework to the challenge of pathway-specific drug design Data-accelerated receptor evolution: engineering GPCR function at the single residue level KEY INSIGHTS FROM THE CONVERSATION The Human Genome as a Discovery Platform When Gloriam joined a bioinformatics group during his master's studies, the first human genome sequence had just become available. Working within that resource, his group identified 26 previously unknown GPCRs in the span of a few years - a pace of discovery that would have been impossible through classical biochemical approaches. The experience established his conviction that computational analysis could function as a genuine primary discovery tool, not merely as support for bench science. De-Orphanization Is a Full-Discipline Effort The process of characterizing an orphan receptor from protein sequence to identified ligand to determined structure cannot be completed within a single lab or a single methodology. Gloriam described the journey of GPR139 as spanning sequence-based phylogeny, database mining for tissue expression, virtual screening, pharmacological assay development, machine learning-guided ligand identification, and finally structural collaboration with external groups. The full arc took more than a decade and required sustained coordination across disciplines that rarely share a lab bench. Taking Over GPCRDB Without a Safety Net When the original GPCRDB team approached retirement, Gloriam chose to carry the resource forward despite holding no tenure and working under a two-year contract. He described it as one of the major single decisions of his career - a bet that the community would respond and the opportunity would justify the risk. The response exceeded his expectations: within years, researchers he had never met were greeting him at conferences by name because of the database. The Bottleneck Has Flipped For most of the history of pharmacological research, generating reliable data was the rate-limiting step. Gloriam argued that this has fundamentally changed: the volume and diversity of available data now far outpaces the field's capacity to analyze and interpret it. This shift places data scientists and computational biologists in a newly central role - not as support for experimentalists, but as the primary constraint to overcome in advancing receptor biology. Biased Agonism Still Needs Its Proof of Concept A drug designed around biased agonism principles received regulatory approval, but its actual functional selectivity has since been questioned - with some researchers arguing it may be a partial agonist rather than a genuinely biased compound. Gloriam identified this ambiguity as symptomatic of a deeper challenge: the field has not yet fully characterized which signaling pathways produce therapeutic benefit and which produce side effects across the GPCR targets most relevant to disease. Until that pathway-level map is built, designing genuinely biased drugs remains a hypothesis in search of its first clean demonstration. Leadership Is a Learnable Skill - If You Seek the Training Gloriam took formal research leadership training before his group was large enough to require it - acting on advice from mentors who recognized that funding panels wanted evidence of leadership readiness alongside scientific merit. He described coaching sessions, national leadership courses, and the deliberate selection of mentors who had recently navigated the specific challenges he was facing. The result was a structured group management model built around four specialized subgroups, each with a senior researcher as daily supervisor - a design that reduced bottlenecks and allowed the science to scale beyond what one group leader could hold. Open Science as the Next Infrastructure Problem Gloriam articulated a vision for GPCRDB as more than a data repository - a shared scientific workspace where researchers could surface big unsolved problems, correspond across institutions, design experiments collectively, and deposit results in a structured format accessible to the entire community. He described the complete characterization of biased signaling pathways across all GPCRs as one such challenge: too large for any single group, and structurally dependent on coordinated community effort that currently has no home. EPISODE TIMELINE Timestamps are AI-generated estimates based on the transcript and may not align exactly with the final edited episode. Verify against the published audio before use. 00:00 Welcome and introduction of David Gloriam 02:23 Career origins - from childhood medicine ambitions to pharmaceutical sciences and bioinformatics 05:34 The human genome treasure hunt - discovering 26 new GPCRs from sequence data 11:55 Orphan GPCRs - years spent chasing receptors with no known function or ligand 13:31 De-orphanizing GPR55 and GPR139 - the full pipeline from sequence to structure 17:21 GPCRDB - origin story, the career-defining decision to take it over, and its growth 23:21 Two frontiers: residue-level receptor function and the unresolved challenge of biased agonism 30:29 Managing a multidisciplinary group of 15 - subgroups, leadership training, and delegation 40:41 What excites Gloriam today - open science models and the long-term vision for GPCRDB 50:01 Career-defining moments, work-life balance, and advice for junior scientists SELECTED QUOTES "Whereas data generation used to be the limiting factor, today it's the analysis and the interpretation and understanding of the data - because we have so much data now, and it's actually our ability to understand it." "The day I stop learning, I might as well die. For me, the actual development - that's the thing. And that's the fun part." "I walked in there and I did the best performance ever. And I walked out and I felt - I think I did it. I did it, yes." "When I come into work and I have a group member that does something better than I do - that's actually what makes me the most proud." About this episode David Gloriam is a Professor in Computational Receptor Biology at the University of Copenhagen where he leads a research cluster for GPCR function and drug discovery and a Pharmaceutical Data Science unit. His group runs the GPCRdb database where ~4,000 researchers each month retrieve reference data and access online tools for analysis, visualization, and experiment design. David obtained his Ph.D. from Uppsala University in Sweden where he worked on the bioinformatic identification of 24 novel human G protein-coupled receptors. He later identified physiological hormones of such under characterized ‘orphan’ receptors and functional probes for a range of receptors. He completed two postdocs in the UK at the EMBL-European Bioinformatics Institute and GlaxoSmithKline . In 2018 he joined the University of Copenhagen, where he has received an ERC Starting Grant, Lundbeck Foundation Fellowship, and Novo Nordisk Foundation Ascending Investigator awards. Dr. Gloriam is a corresponding member of the Nomenclature Committee of the International Union of Pharmacology (IUPHAR). He is one of the coordinators of recommendations to describe ligand bias towards signaling probes and safer drugs. His group recently developed an online resource of biased ligands and pathway effects to advance the biased signaling field. Join me a learn more about David’s work, his career trajectory, and GPCRdb. Dr. David E. Gloriam on the web LinkedIn ResearchGate Twitter Google Scholar Computation Receptor Biology- Gloriam Group GPCRdb Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Dr. Terry Hebert on why challenge trials weren't ready, what it takes to hold a GPCR signaling lab together during a pandemic, and the BRET-based beta-1 adrenergic paper that landed in lockdown. << Back to podcast list Strategic Partner(s) Terry Hébert This resilience conversation with Dr. Terry Hebert was recorded in spring 2020, when Montreal was the national epicenter of the COVID-19 pandemic and every non-essential bench in the country was shut. The discussion moves across three scientific registers: the practical mechanics of holding a GPCR signaling lab together remotely; the continuity of receptor pharmacology work already in the pipeline before the shutdown, including a newly accepted BRET-based platform for beta-1 adrenergic receptor signaling built with the Bouvier lab; and a pharmacologist's reasoning about the then-unresolved question of whether human challenge trials were an ethical shortcut to a SARS-CoV-2 vaccine. Dr. Hebert's argument — that challenge trials depend on a reliable therapeutic the field did not yet have — sits at the intersection of drug discovery logic and public health ethics, and illustrates how GPCR scientists reason about pharmacology problems well outside their primary receptor. For Dr. Hebert, the conversation is also about what he had to let go of: the assumption that a lab, once built, runs on its own inertia. About the Guest Dr. Terry Hebert is a professor at McGill University in Montreal, where his lab studies G protein-coupled receptor signaling. His research spans BRET-based assay platforms for characterizing signaling downstream of specific GPCRs, the transcriptional regulation of signaling components as an underappreciated axis of pharmacological modulation, and long-running collaborations on beta-adrenergic receptor biology with the Bouvier lab and others. His work is grounded in careful assay development and a conviction that the signaling space around a receptor is richer than single-pathway readouts suggest. Scientific Themes of the Conversation Lab continuity during institutional shutdown — What it takes to maintain scientific output when the physical lab is closed and every operation has to happen remotely. BRET platforms for GPCR signaling — The role of resonance-energy-transfer-based assays in capturing signaling downstream of specific receptors, with the beta-1 adrenergic receptor as a worked example. Challenge trials and the therapeutic floor — Why the ethics of accelerating vaccine trials depend on having an adequate treatment for the disease under study. Vaccine development at scale — How to read a landscape of 90+ parallel vaccine candidates without confusing breadth of effort for probability of success. Mentorship under isolation — The practical and emotional work of keeping graduate students — especially international students far from their families — connected to a lab that has gone quiet. Pandemic preparedness as a scientific failure — The gap between what infectious disease researchers had been warning about and what institutions were actually ready to do. Key Insights from the Conversation Challenge trials don't work without a reliable drug. Dr. Hebert's core pharmacology argument is that proposing a challenge trial — where volunteers receive placebo or active virus — is ethically unworkable without a therapeutic that can rescue the ones who get sick. His position is that the drug problem has to be solved, or at least bounded, before the vaccine trial design can responsibly change. 90 vaccine candidates is a number about effort, not probability. The conversation pushes against the comfort of large numbers. A field running 90 parallel vaccine trials is a field hedging under uncertainty, not a field with 90 independent chances of success. Dr. Hebert is hopeful but careful about the distinction. BRET platforms carry work forward when the lab can't. The beta-1 adrenergic receptor paper — a BRET-based platform for capturing downstream signaling, built with the Bouvier lab — illustrates how assay-development projects remain productive when benchwork stops. The experimental data was in hand before the shutdown; the intellectual work of writing, reviewing, and revising kept going regardless. A lab is a social infrastructure, not just a physical one. Weekly Monday lab meetings, Friday journal clubs, daily Slack and Zoom contact, a faculty-vs-student trivia night — the lab's continuity came from translating routines, not suspending them. The most fragile link in the system was the isolation of international students away from their families. Reopening is a puzzle about labs, not benches. The hardest logistical problem isn't social distancing within a single lab — it's social distancing between labs sharing a floor, shared equipment, and a public transit system that funnels everyone through the same bottleneck. The warnings were there. Dr. Hebert's reflection on preparedness is quiet but pointed: the scientific community had been warning about this for years. The failure wasn't epistemic — it was institutional. And that failure is what will cost the most, borne hardest by the people least cushioned against it. The next one is coming. The most forward-looking moment in the conversation is also the most sober. This disease, for all its damage, is survivable for most people. The next one might not be. The open question is whether the system will have learned anything by then. Episode Timeline Timestamps were generated using AI for readability. 00:00 Welcome and Dr. GPCR Summit 2020 announcement 01:49 Check-in with Dr. Hebert — shutdown, reopening plans, and Montreal as epicenter 03:06 Paper acceptances, thesis writing, and 30 hours of Zoom teaching in one month 04:29 The beta-1 adrenergic BRET paper and a review on transcriptional regulation as a drug target 05:22 Lab meetings, journal clubs, and the Slack/Zoom scaffolding 06:12 Student wellbeing and the puzzle of reopening a shared floor 07:16 Why challenge trials aren't ready — and the remdesivir question underneath them 08:52 When pandemic infrastructure breaks down at national scale 10:16 Lessons for the next one, and the shape of the new normal Selected Quotes "So we made a decision a month and a half ago to kind of stop going to the lab. Montreal being the epicenter of the disease in this country — we don't regret that decision now." "I don't think [challenge trials] are a good idea because we don't really have good drugs to deal with the disease when people get sick. If we have a way to control the disease and keep people from getting really sick, I think we can go to challenge trials more rapidly." "Honestly it could be worse, right? This disease, most people survive. When the next one comes, let's hope we learn something from this one." "Those are the people we have to protect, not big corporations who, you know, are probably in a sense part of the cause. Globalization is not something that is without its consequences here." About this episode Dr. Terry Hébert is a Professor within the Department of Pharmacology & Therapeutics at McGill University. Much of his work is based on GPCR signaling in the context to cardiovascular diseases. In this special episode of the Dr.GPCR podcast , we re-connected with Dr. Terry Hebert to chat about how he and his team has been adapting to the new reality of working remotely. Terry tells us about the importance of adapting, communicating, and being mindful of those around us. Dr. Terry Hébert on the web Terry Hébert | Institute of Health Sciences Education Hébert Lab LinkedIn Hébert Lab The GPCR Consortium PubMed Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Dr. Alexander Ball of GeneTex on the recombinant platform and validation strategy behind a challenge to GPCR researchers. Free live webinar, June 25. < Back to Webinars 📅 Thursday, June 25, 2026 at 3:00:00 PM UTC Register Here 🤝 Webinar in collaboration with: GeneTex Recombinant Antibodies for GPCRs: A Challenge to the Community Test them in your lab. Tell GeneTex what works and what doesn't. A reagent gap that holds back the biology GPCR activity is targeted by one-third of all FDA-approved drugs. Yet much remains to be learned about how these 800-plus receptors are expressed and how they function in living systems. Part of the gap is biology. Multipass transmembrane proteins are genuinely difficult targets. Part of the gap is the reagents. Reliable antibodies for human GPCRs are scarce, and without them, basic questions about expression and physiological function stay out of reach. Producing specific antibodies for human GPCRs is a formidable job. Expression levels in common cell lines are often low. Identifying an immunoreactive antigen sequence that is specific for a single receptor and detectable across applications is difficult on its own. The literature often disagrees on which antibodies actually work. Proving specificity for the intended GPCR is rarely straightforward. GeneTex is tackling that problem with a high-throughput recombinant antibody platform paired with enhanced validation strategies. The approach has already generated more than 300 recombinant monoclonal antibodies against almost 200 human GPCRs, and the catalog keeps growing. Inside the platform The production workflow is built to detect promising clones early and to hold specificity, scalability, and consistency steady once those clones are selected. Dr. Ball will walk through how the recombinant platform was built, what it takes to produce specific antibodies against multipass transmembrane targets including GPCRs at scale, and how the workflow handles the realities of low endogenous expression and tight specificity requirements. Validation that earns the catalog its place Every antibody is characterized through a prioritized validation set: CRISPR-based knockout and knockdown protocols, endogenous expression detection, cell fractionation, comparable antibody testing, and application-specific testing. When feasible, GeneTex uses VirDTM-GPCR arrays (CDI Labs, Mayagüez, PR), which present a nearly comprehensive library of human non-olfactory GPCRs individually expressed on herpes simplex virion envelopes for cross-reactivity screening. Dr. Ball will walk through each, explain why KO/KD testing is prioritized, and show how the validation data is shared with researchers. The challenge: test them in your lab This is the goal of the Dr. GPCR x GeneTex partnership. GeneTex is offering free samples of the recombinant antibodies to GPCR researchers in exchange for structured feedback, positive or negative. As Dr. Ball puts it in his own words, the primary goal is to get these reagents tested and evaluated by GPCR researchers. That is how a catalog earns the trust of the community, and how the community ends up with reagents it can actually rely on. Dr. Ball will explain how the challenge works, who it is for, and how to request samples. Speaker Dr. Alexander Ball , MD, Senior Scientist, GeneTex, Inc. Dr. Ball has been with GeneTex since 2012 and leads the company's enhanced antibody validation initiative. He earned an M.D. from the University of Southern California School of Medicine and completed internal medicine training at California Pacific Medical Center in San Francisco. He transitioned from clinical medicine to academic research at UC Irvine, where he worked on protein complexes mediating chromosome dynamics. At GeneTex, that background shapes how he thinks about reagent quality. Antibodies are tools scientists depend on, and validation is not optional. Organizers GeneTex GeneTex is a multinational antibody manufacturer founded in San Antonio, Texas in 1997. Since 2020, its recombinant monoclonal antibody facility has produced reagents paired with enhanced validation protocols and a strong emphasis on KO/KD testing. The company's GPCR program is building a comprehensive catalog of recombinant monoclonal antibodies for the human nonsensory and orphan GPCRs. More than 300 recombinant monoclonal antibodies against almost 200 human GPCRs, and growing Prioritized validation: CRISPR KO/KD, endogenous expression, cell fractionation, comparable antibodies, application-specific testing VirDTM-GPCR arrays for specificity screening when feasible Free samples available to GPCR researchers willing to give structured feedback Yearly Glow Strategic Partner in the Dr. GPCR ecosystem Dr. GPCR Dr. GPCR is a nonprofit ecosystem dedicated to advancing GPCR-targeted drug discovery. Through curated intelligence, community engagement, podcasts, webinars, and editorial content, Dr. GPCR connects scientists, tools, and decision-makers across academia and industry, all year round. Previous Webinar Next Webinar Don’t Miss the Next Live Session Dr. GPCR membership gives you access to all upcoming live, interactive webinars. Free. Takes less than a minute to join. Cancel anytime. Sign Up for Free

<< Back to podcast list Strategic Partner(s) Dr. GPCR Team About Dr. Yamina Berchiche Dr. Yamina A. Berchiche is the founder of Dr. GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors (GPCRs) that control virtually everything in the body as drug targets. The mission of Dr. GPCR is to accelerate GPCR drug discovery by sharing the latest research and technology advances in the field and providing exposure to scientists through the Dr. GPCR podcast. Dr. Berchiche obtained her Master’s and Ph.D. in Biochemistry at the University of Montreal in Canada before training at Rockefeller University in New York and the National Institutes of Health in Bethesda, Maryland. She developed expertise over the past two decades studying structure/function relationships of GPCRs using live-cell bioluminescence resonance energy transfer (BRET). Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the body. Dr. Yamina Berchiche on the web Website LinkedIn Facebook Twitter ResearchGate PubMed Google Scholar Dr. GPCR About Dr. Shivani Sachdev Dr. Sachdev is an early career researcher in the National Institute of Diabetes and Digestive and Kidney Diseases at the National Institutes of Health. Her research centers on developing nanobody-ligand conjugates to target GPCRs, with a focus on receptors relevant for treating osteoporosis, diabetes, and pain. She received her undergraduate degree in Biotechnology from KIIT University in India. She subsequently joined Professor Mark Connor's laboratory at Macquarie University in Australia. Dr. Sachdev pursued Ph.D. in the same lab where she investigated the molecular pharmacology of cannabinoid receptors. She is also very active within the pharmacology community and currently serves on the editorial board of the British Journal of Pharmacology. Given her expertise in GPCR pharmacology and scientific communication, she is poised to make valuable contributions to the field and expand our understanding of GPCR signaling. Dr. Shivani Sachdev on the web NIDDK ReseachGate Google Scholar LinkedIn Twitter Dr. GPCR About Dr. Inês Pinheiro PharmD by training and Ph.D. candidate in Hartley's lab at the University of Geneva. As a young researcher fascinated by chemokine receptors, molecular pharmacology, drug discovery, and immuno-oncology. Dr. Inês Pinheiro on the web LinkedIn University of Geneva Twitter Dr. GPCR About Dr. Monserrat Avila Zozaya I did a PhD in cell biology at CINVESTAV, Mexico. During that time, I investigated the effect of lung cancer-related mutations in the GAIN domain of the Latrophilin 3 receptor. My long-term interest is focused on understanding the mechanisms mediated by GPCRs at the cellular communication level. Dr. Monserrat Avila Zozaya on the web LinkedIn Antony Boucard Lab Dr. GPCR About John Azietaku John Teye Azietaku,PhD is a trained pharmacist, holding a Ph.D. in Drug Discovery Biology and Pharmacology from Monash University. Currently serving as a Post Doctoral research fellow at Monash University, John plays a pivotal role in the pharmacological screening of compounds for a commercial drug discovery program. With prior industry experience as a Clinical Research Associate at IQVIA and regulatory officer at the Food and Drug Authority (FDA) in Ghana, John has a proven track record of ensuring compliance with protocols and regulatory standards. Driven by a passion for advancing drug development, John is committed to leveraging his expertise to enhance healthcare outcomes and contribute to the growth of the pharmaceutical and biotech industry. John Azietaku on the web LinkedIn Dr. GPCR About Ya-Tzu Li Ya-Tzu is a Master's student at the University of South Florida, utilizing large-scale virtual drug screening to identify agonists and antagonists targeting Class A GPCRs. Since beginning her undergraduate studies, she has used computational methods like molecular dynamics simulations and free energy landscape analysis to understand the signaling pathways and activation mechanisms of the Dopamine D3 receptor and the CXCR4-CXCL12 complex. In August, Ya-Tzu will continue her academic and research pursuits by beginning her PhD training in Medical Science at USF, aiming to further contribute to the field of medical pharmacology. Ya-Tzu Li on the web LinkedIn Dr. GPCR About Cam Sinh Lu Cam Sinh Lu is a PhD student at Monash Institute of Pharmaceutical Sciences, Monash University, with a deep interest in understanding drug-receptor interactions. With an immense passion for molecular pharmacology, his research focuses on elucidating the molecular basis of membrane protein signalling using quantitative assays and molecular modelling. Further down the track, he aims to apply this knowledge to develop novel chemical treatments for neuronal and cardiovascular diseases. Cam Sinh Lu on the web LinkedIn Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Dr. Eric Trinquet discusses the science and story behind pH Sense, Revvity’s innovative GPCR internalization assay, and his journey in GPCR product R&D. << Back to podcast list Strategic Partner(s) From Rare Earth Probes to Internalization Assays: The pHSense Story with Dr. Eric Trinquet What does it take to design a breakthrough GPCR assay—from idea to industrial impact? In this special episode, Dr. Eric Trinquet shares the inside story behind the development of pH Sense, Revvity’s latest innovation for tracking GPCR internalization. With a career spanning two decades at the intersection of fluorescence chemistry, functional assays, and product development, Eric takes us through the highs, failures, and scientific “aha” moments that shaped tools like the IP-One kit, Tag-lite, and now, pH Sense. If you’ve ever used HTRF or wondered what goes into making a product worthy of your next experiment, this is your backstage pass. You’ll hear what truly makes a reagent successful—and why academic–industry collaborations are essential for advancing GPCR research. Inside This Episode How Eric and his team reimagined rare earth complexes to develop pH-sensitive probes with tunable brightness and lifetime. Why pH Sense enables high-throughput, no-wash tracking of GPCR internalization—even at endogenous expression levels. What shifted the team’s strategy from traditional calcium assays to IP1 accumulation—and why it mattered for Gq-coupled receptors. How collaborations with David Parker and Jean-Philippe Pin accelerated both probe chemistry and biological validation. What it felt like to see the first dose-response curves in native beta cells—and why that moment changed the trajectory of the project. Why the commercialization of a reagent is not the end, but the beginning of a feedback-driven innovation cycle. Why It Might Hit Home If you’ve ever: Wrestled with unreliable endpoint assays or cumbersome radioactive protocols, Pushed for more physiologically relevant systems and hit the “overexpression ceiling,” Balanced scientific rigor with the unpredictability of product development, Or felt the thrill of seeing a tool you built drive real biological insight… …this episode will resonate. About the Guest Dr. Eric Trinquet is Head of R&D for Life Sciences Reagents at Revvity, where he leads innovation in biochemical and cell-based assay platforms. With a foundational career at Cisbio Bioassays—later acquired by Revvity—Eric played a pivotal role in bringing technologies like HTRF, the IP-One kit, and the Tag-lite platform into widespread use. Originally trained as a physicist with a strong interest in photophysics and fluorescence chemistry, Eric transitioned into the GPCR field through hands-on assay development. His passion lies in turning cutting-edge probe chemistry into robust, scalable tools for drug discovery and basic research. What drives him? A mix of scientific curiosity, a tolerance for failure, and a commitment to delivering real-world impact—one product at a time. More about Revvity pHSense Reagents GPCR Reagents Revvity on Dr. GPCR Dr. GPCR X Revvity Collaboration Want more like this? Join the Dr. GPCR Premium Ecosystem for behind-the-scenes access to GPCR innovators, exclusive deep-dives, and practical tools to accelerate your research or career. 👥 Build connections. 🧪 Get insights. 🎧 Stay ahead. 👉 Join now Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Dr. Michelle Halls reveals how organized GPCR signaling drives assay innovation and new therapeutic insights. << Back to podcast list Strategic Partner(s) Leadership, Impact, and GPCR Signaling with Dr. Michelle Halls In this episode Dr. Michelle Halls shares how dissecting the spatial organization of GPCR signaling opens new doors in drug discovery. From early discoveries in cyclic AMP signaling to uncovering ultrasensitive receptor responses at femtomolar ligand concentrations, her work highlights why receptor localization and protein complex assembly matter for therapeutic targeting. This conversation is especially valuable for scientists developing functional assays, fluorescence-based tools, and high-throughput GPCR screens. Inside This Episode How ultrasensitive GPCR signaling emerges from pre-assembled receptor–effector complexes at the plasma membrane. Why receptor localization and scaffolding dramatically shift functional readouts in disease models. What early cyclic AMP assays revealed about spatial signaling long before high-content technologies existed. The moment when femtomolar ligand concentrations uncovered unexpected receptor sensitivity. How an integrated training and lab structure at Monash Institute of Pharmaceutical Sciences fosters innovation in functional assay development and GPCR research. Why It Might Hit Home If you’ve ever: Faced unexpected assay behavior at ultra-low ligand concentrations, Balanced innovation with robust validation under real experimental constraints, Tried to map signaling heterogeneity in disease-relevant models, Built assays that need to work in real biology—not just on paper, …this episode will resonate. About the Guest Michelle Halls is an Associate Professor at Monash University and Deputy Theme Leader of Drug Discovery Biology at Monash Institute of Pharmaceutical Sciences. She leads the Spatial Organisation of Signalling Laboratory, where her team investigates how GPCRs orchestrate localized signaling events, how these mechanisms are hijacked in disease, and how they can be leveraged for therapeutic innovation. Michelle earned her PhD in Molecular Pharmacology at Monash University, then trained in single-cell biology as an NHMRC CJ Martin Fellow at University of Cambridge. She established her lab in 2011, and today she is a Viertel Senior Medical Research Fellow. Her recognitions include the 2024 ASCEPT Achievement Award, the 2023 BPS Geoffrey Burnstock Prize, and the 2019 Faculty Future Research Leader Award. More about Michelle Halls Monash Institute of Pharmaceutical Sciences Bluesky LinkedIn Articles about this Podcast Episode How GPCR Spatial Signaling Sparked a Scientific Journey From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Collaboration Built an Innovation Engine 🎓 Want more like this? Get behind-the-scenes conversations, advanced assay development strategies, and practical GPCR tools inside Dr. GPCR Premium . Join a global GPCR community of scientists and biotech leaders. 👉 Join now Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Arthur Christopoulos About Dr. Arthur Christopoulos " Arthur Christopoulos is the Professor of Analytical Pharmacology and the Dean of the Faculty of Pharmacy & Pharmaceutical Sciences, Monash University, Australia. His research focuses on novel paradigms of drug action at GPCRs, particularly allosteric modulation and biased agonism, and incorporates computational and mathematical modelling, structural and chemical biology, molecular and cellular pharmacology, medicinal chemistry, and preclinical models of behaviour and disease. His work has been applied to studies encompassing neurological and psychiatric disorders, cardiovascular disease, obesity, diabetes, chronic pain and addiction. He has received substantial, long-term support from international and national competitive, charitable and commercial sources, as well as being academic co-founder of three GPCR-focussed biotechnology companies. Professor Christopoulos has over 360 publications, including in leading international journals such as Nature,Science and Cell, and has delivered over 180 invited presentations. He has served on the Editorial Board of 8 international journals and was a Councillor of the International Union of Basic and Clinical Pharmacology (IUPHAR). He has also been the recipient of multiple awards, including the John J. Abel Award and the Goodman and Gilman Award from the American Society for Pharmacology and Experimental Therapeutics; the Rand Medal from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists; the British Pharmacological Society’s Gaddum Memorial Award; the IUPHAR Sir James Black Analytical Pharmacology Lecturer; the GSK Award for Research Excellence and a Doctor of Laws (Honoris Causa) from the University of Athens. Since 2014, Clarivate Analytics have annually named him a Highly Cited Researcher in ‘Pharmacology & Toxicology’, and in 2021 also named him a Highly Cited Researcher in the additional category of ‘Biology & Biochemistry’. In 2017, he was elected a Fellow of the Australian Academy of Health and Medical Sciences, in 2018 as a Fellow of the British Pharmacological Society, and in 2021 he was elected a Fellow of the Australian Academy of Science for his seminal contributions to drug discovery. In 2023, he was elected a Fellow of the Pharmaceutical Society of Australia. " Dr. Arthur Christopoulos on the web Monash University Wikipedia Google Scholar LinkedIn Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick recap Yamina and Arthur from Monash University discussed Arthur's career journey, the importance of hard work, failure, and differentiation in academic and personal lives, and the value of international conferences. They also explored the significance of translating fundamental discoveries into clinical applications, the potential of new drugs, and the unique challenges within universities. Additionally, they discussed the importance of hiring based on differentiation, impact, and interest, the need for workforce development, and the potential of involving junior scientists and postdocs in their podcast. Lastly, they touched upon the global challenges of healthcare workforce growth, climate change, and emerging psychiatric disorders, as well as the importance of recording lectures and making pre-lesson materials available to students. Next steps - Yamina will share notes about PRISM and presentability with Arthur. - Arthur will share the story of PRISM's development and its impact on the field with Yamina. - Yamina will send an invite for a follow-up meeting with Arthur next Saturday at 9 PM. - Arthur and Yamina will prepare for the next meeting, focusing on the concept of biased agonism and discussing Dr. GPCR and the charity status. - Yamina will attempt to book Denise for a future podcast episode. Summary Arthur's Career Journey and Transition to Dean Yamina introduced Arthur to her team and discussed the use of a particular tool for meeting summaries. Arthur shared his career journey from pharmacy to becoming a professor, highlighting the influence of his mentors and the importance of his postdoctoral experience. They discussed the value of hard work, failure, and the significance of differentiation in their personal and academic lives. Towards the end, they focused on Arthur's transition to become Dean and his decision to move from Australia to the United States for a postdoctoral position. Postdoctoral Position, Scientific Dynamics, and New Drug Targets Arthur shared his decision to undertake a postdoctoral position with Nigel Bird's lab in the UK and his experiences of meeting influential figures during his time in the US. He and Yamina discussed the importance of preserving original work, the value of international conferences, and the dynamics between junior and senior scientists in a research environment. They also shared their admiration for the work of a mutual friend and discussed the history of muscarinic receptors, specifically focusing on the role of a compound that Arthur received from Fred. Lastly, they discussed the progress of new drugs targeting specific receptors for various diseases, with Arthur sharing insights on Eli Lilly's compound, Xanomeline, and the potential of M4 PAM for psychosis. Collaborative Research and Translational Approach Arthur and Yamina from Monash University discussed their collaborative approach to scientific research, emphasizing the benefits of combining their complementary skills and interests. They shared their unconventional approaches to research, including the creation of a critical mass of GPCR researchers in Australia and the initiation of a successful series of conferences. They also discussed the relocation of some university labs to facilitate collaboration and overcome the siloed department structure. Additionally, they explored the unique culture and structure of their Institute, highlighting its translational approach to research and its capacity to translate research into therapeutic commercialization. Lastly, Arthur shared three significant moments that shaped his career, including the evolution and impact of analytical pharmacology, particularly highlighting the role of Prism, a data analysis tool. Podcast Format, Team Culture, and Science Yamina and Arthur concluded their discussion and decided to take a short break. They talked about the format and length of their podcast, their professional interests, and their recent successful bid to bring Moderna to their university. They also explored the idea of starting a similar talk show format to 'Between Two Ferns', the importance of maintaining team culture, and the potential health issues among well-known scientists. Lastly, they discussed the growth and development of the Monash Institute of Pharmaceutical Sciences, the importance of knowing when to let go in scientific experiments, and the idea of a panel for building and incubating companies. Arthur's Pandemic Journey and Global Challenges Yamina and Arthur discussed Arthur's experiences during the Covid-19 pandemic, his journey as a research fellow in Australia, and his transition to the role of Dean. Arthur shared his insights into the unique grant funding system in Australia, the importance of impact in research, and the challenges of balancing administrative responsibilities with scientific pursuits. He also reflected on his personal health struggles, the growth of his university, and the faculty's successful response to the Covid crisis. The conversation also touched upon Arthur's career decisions, his scientific achievements, and the importance of learning from mistakes and self-confidence. Lastly, they discussed the global challenges of healthcare workforce growth, climate change, and emerging psychiatric disorders, as well as the importance of recording lectures and having pre-lesson materials available to students. Translating Discovery Into Clinical Application Arthur and Yamina discussed the importance of translating fundamental discoveries into clinical applications in their research, highlighting the unique opportunities presented by their location and partnerships with other institutions. They stressed the necessity of making their research goals clearer, avoiding replication, and adopting a more assertive approach in grant applications. They also emphasized the significance of fundamental discoveries, the role of biotech, and the need for efficiency and process development in university systems. The conversation highlighted ongoing challenges within universities, including resistance to change and the need to communicate expectations and protect established cultures. Hiring Process, Collaboration, and Education-Focused Initiatives Arthur emphasized the importance of differentiation, impact, and interest in their hiring process and fostering a culture of collaboration. He shared his vision of breaking down barriers and promoting education-focused initiatives, encouraging his team to be innovative and apply their skills to education. Yamina expressed a desire to learn from successful leaders and the importance of recognizing talent and matching it with the needs of a particular project. They also discussed the disruption within the pharmaceutical sector, the importance of workforce development, and the need for maintaining a healthy work-life balance. Lastly, they deliberated on involving junior scientists and postdocs in their podcast and the possibility of writing a book about their experiences in academia. Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Demet Araç About Dr. Demet Araç "Demet was an undergraduate at Bilkent University in Turkey, where she majored in Molecular Biology and Genetics. She moved to the University of Texas Southwestern Medical Center at Dallas in 2000 to work with Dr. Jose Rizo-Rey as a graduate student to elucidate the mechanisms of neurotransmitter release. After finishing her graduate training, she joined Dr. Axel Brunger’s lab at Stanford University to study the structure and function of cell-adhesion proteins at the synapse. In 2013, Demet began her independent research career at the University of Chicago within the Department of Biochemistry and Molecular Biology." Dr. Demet Araç on the web University of Chicago Araç Laboratory Google Scholar Twitter Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick recap Yamina and Demet discussed their personal backgrounds, academic backgrounds, and career paths, with a focus on their experiences in the field of GPCR (G protein-coupled receptor). Demet shared his journey of studying adhesion GPCRs, the challenges he faced, and the progress made in understanding their structure and function. They also discussed the ongoing developments in the GPCR field, the upcoming adhesion GPCR consortium meeting, and the naming conventions of proteins in the field. Lastly, they shared their views on pursuing one's passions and not being afraid of the unknown, and Demet expressed his satisfaction with his first podcast experience. Next steps • Yamina will send an email to Demet, encouraging him to distribute information about the Doctor GPCR Symposium to his team, including students, postdocs, and PhD students, and will share the recording of the podcast with Demet for the same purpose. • Demet will distribute information about the Doctor GPCR Symposium to his team and encourage his students, postdocs, and PhD students to contact Yamina for potential speaking opportunities at the symposium or other events. Summary Personal Backgrounds and GPCR Interest Yamina and Demet had a discussion about their personal backgrounds, interests, and experiences. Yamina shared her experiences of living in different countries and the adaptability skills it required. Demet, who had studied various subjects including chemistry, physics, biology, and math, shared his interest in science and physics. He also opened up about his childhood experiences of living in a place with limited pedestrian infrastructure. Yamina inquired about Demet's interest in studying GPCRs, and he explained his motivation stemmed from his experiences as an international student. They also acknowledged the cultural differences between Demet's home country, Turkey, and Yamina's, Canada. Academic Backgrounds and Career Paths Discussion Demet and Yamina discussed their academic backgrounds and career paths, with a focus on their experiences in academia. Demet shared that his interest in science led him to study biology, genetics, and molecular biophysics in Turkey and the United States, eventually becoming a professor at UT Southwestern Medical Center in Dallas. Yamina asked about Demet's career aspirations, to which he responded that he pursued science because he enjoyed it. They also discussed their scientific journeys, focusing on their work on adhesion GPCRs, a field that was largely neglected at the time. Demet's research on the gain domain of adhesion GPCRs started during his postdoctoral studies and continued into his faculty position, despite initial challenges in securing funding. Demet's Journey in Studying Adhesion GPCRs Demet discussed his journey in studying adhesion GPCRs, outlining his collaborations, challenges, and the progress made in understanding their structure and function. He explained that initially, the field lacked adequate tools, and his lab had to develop new techniques to work with these complex proteins. Over the years, Demet's team expanded their collaborations and improved their understanding of the GPCRs through various approaches, including structural biology and signaling assays. Yamina expressed her appreciation for Demet's work and asked about the development of the GPCR field over time. Demet explained that since the year 2000, the field has seen significant growth, with important discoveries such as the transmembrane region structures mediated by agonists. GPCR Field and Naming Convention Discussion Demet and Yamina discussed the ongoing developments in the GPCR field and the upcoming adhesion GPCR consortium meeting, which Anthony will be organizing in Mexico in October. They also addressed the naming conventions of proteins in the field, with Yamina expressing concern about the potential confusion caused by changes in nomenclature. Lastly, they shared their preferences for GPCRs, with Demet expressing a particular fondness for certain adhesion GPCRs. GPCR Field Progress and Advice for Junior Scientists Demet and Yamina discussed the progress of their research in the GPCR (G protein-coupled receptor) field, specifically focusing on adhesion GPCRs. Demet shared that they have been working on the Latrophilin project since 2013, screening about 20 adhesion GPCRs, with the Latrophilin 3 construct proving most successful. They also discussed the importance of the extracellular region of these receptors and its potential as a drug target. Demet highlighted a series of realizations over the years about the importance of the GPCR field and its applications, emphasizing that it's not just about one "Aha!" moment. Yamina expressed her love for the GPCR field and asked for advice for junior scientists interested in the same. Embracing Passions and Embracing Unknowns Demet and Yamina discussed the importance of pursuing one's passions and not being afraid of the unknown in their chosen fields. Demet shared his belief that he was driven by a biological need to tackle more challenging tasks. Both agreed that one should find work exciting and interesting, as life is too short to spend doing things one doesn't enjoy. Yamina posed the question of what advice Demet would give his younger self, but Demet responded that he wouldn't change his past actions, as he believed they led him to his current fulfilling path. Podcast Experience and Upcoming Collaboration Demet expressed satisfaction about his first podcast experience and showed interest in sharing his insights in future episodes. Yamina shared her plans for an upcoming Doctor GPCR Symposium in June, for which Demet is the first confirmed speaker, and discussed potential challenges and solutions. The conversation ended with an agreement to collaborate in the future, with Yamina expressing her intention to reach out to Demet's students and postdocs for potential podcast participation. Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Developing new tools to uncover GPCR signaling patterns with Remi Janicot About Remi Janicot I was born in Paris (France) and grew up in Europe until I was 18. After graduating high school, I moved to America to pursue my passion for basketball while continuing high level studies. I played collegiate basketball and earned my bachelor’s at Ursinus College, a small school around Philadelphia where I graduated from in 2018. After that, I worked at Johns Hopkins in Baltimore as a research assistant investigating mechanisms and treatments for pediatric epilepsy. With my background in neuroscience, the lab of Dr. Mikel Garcia-Marcos seemed like a good fit as GPCRs are integral to the functioning of the nervous system (and much more). My particular projects revolve around developing new tools to study GPCR activity in ways that were not previously possible. This research has led to a first-author Cell article on the development of a new biosensor platform called ONE-GO biosensors. Overall, the lab works on diverse models and diseases, and has developed a wide array of tools to dissect GPCR/G protein signaling which I would be happy to discuss. Remi Janicot on the web Chobanian & Avedisian School of Medicine Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Gunnar Schulte of Karolinska Institute makes the case that frizzled receptors are GPCRs — through G-protein coupling maps, conformational biosensors, and the first small molecule shown to activate frizzled 6. << Back to podcast list Strategic Partner(s) Gunnar Schulte: Frizzled Receptors and the GPCR Identity Question Frizzled receptors are a family of 10 cell surface proteins that mediate Wnt signaling — one of the most fundamental pathways in vertebrate development, stem cell renewal, and tumor biology. Despite decades of study, the field remains divided on a foundational question: are frizzled receptors GPCRs? They carry the characteristic seven-transmembrane topology, but their ligands are large, lipid-modified proteins that require carrier molecules for transport, their canonical Wnt–beta-catenin signaling appears G-protein-independent, and almost no small molecule pharmacology exists for this subfamily. Gunnar Schulte's lab at Karolinska Institute has spent years assembling the evidence on the other side — demonstrating G-protein coupling specificity across individual frizzled subtypes, detecting ligand-induced conformational changes through biosensor approaches that mirror what is seen in classical GPCRs, and showing that G-protein-dependent pathways downstream of frizzled activation are physiologically relevant. For Schulte, the scarcity of pharmacological tools is not just a technical inconvenience — it is the central obstacle that has shaped every decision his lab has made since his first postdoc. The question of whether frizzled receptors are GPCRs is, in his view, inseparable from the question of whether they can ever be drugged. About the Guest Gunnar Schulte is a professor at the Department of Physiology and Pharmacology at Karolinska Institute in Stockholm, where he leads research on Wnt–frizzled receptor signaling. His lab investigates the molecular mechanisms of frizzled receptor activation, including G-protein coupling specificity across all 10 human frizzled subtypes, receptor conformational dynamics, and biosensor platforms for quantifying signaling selectivity. Schulte's work helped establish that individual frizzled receptors are not interchangeable — each couples to distinct G-protein families in ways that challenge the field's conventional focus on the beta-catenin pathway alone. He began his scientific career studying adenosine receptor signaling during a PhD with Bertil Fredholm at Karolinska, and pivoted to frizzled receptors during a postdoctoral fellowship with Ernest Arenas, staying at the same institution ever since. Scientific Themes of the Conversation The GPCR identity question — what it takes to make the case, and why the field is still divided G-protein coupling specificity across the 10 frizzled subtypes — each receptor is its own pharmacological entity The Wnt ligand problem — lipid modifications, carrier proteins, and what makes these ligands so difficult to work with Conformational dynamics as functional evidence — how biosensors are being used to argue for GPCR-like activation in frizzled Pathway selectivity — how the receptor may choose between disheveled and G-protein signaling through conformational selection The pharmacology gap — small molecules, repurposed Smoothened compounds, and what a druggable frizzled might eventually look like Key Insights from the Conversation 1. Each frizzled receptor is its own pharmacological entity The frizzled family is commonly discussed as a single target class, but Schulte's G-protein coupling data reveal that individual subtypes are functionally distinct. Frizzled 5 couples to Gq, frizzled 7 to Gs, frizzled 10 to G13 — and the pattern continues across the family without a simple organizing rule. Treating "frizzled" as a unified target, Schulte argues, is one reason the field has been slow to build pharmacology. 2. The Wnt ligand problem may be the field's deepest bottleneck Wnt ligands are approximately 35–40 kDa, carry a lipid modification that prevents them from diffusing freely in aqueous medium, and require carrier proteins to reach their receptors. Fewer than one in 19 Wnt ligands is currently available in a biologically active, tagged form suitable for binding assays. Schulte describes spending a substantial portion of his lab budget on recombinant Wnts while still unable to run the systematic interaction mapping the field needs. 3. Conformational change is Schulte's strongest argument for GPCR identity Using cpGFP-based conformational sensors inserted into frizzled receptors, Schulte's lab has shown that Wnt stimulation produces detectable conformational changes that parallel what is observed in classical GPCRs. For Schulte, this is not secondary evidence — it is the clearest demonstration that frizzled receptors operate by the same fundamental activation mechanism, and the clearest challenge to those who believe otherwise. 4. A Smoothened compound became the first pharmacological handle on frizzled SAG1.3, a small molecule agonist originally developed for the related receptor Smoothened, was shown by Schulte's lab to act as a weak partial agonist at frizzled 6. Every chemical modification so far has converted it into an antagonist rather than a stronger agonist. But the result was the first demonstration that frizzled receptors have a pharmacologically accessible binding pocket — a conclusion that was not obvious from the initial frizzled 4 crystal structure, which suggested the pocket was too small for small molecule targeting. 5. The class F CRISPR knockout cell line changed what questions could be asked Working in cells that endogenously express multiple frizzled subtypes makes it nearly impossible to attribute a signaling event to a single receptor. The development of a HEK cell line with all class F receptors knocked out — generated by Benoît Vanhollebeke's lab in Belgium and shared with the field — gave Schulte's group the clean background needed to study individual frizzled subtypes in isolation. Combined with porcupine inhibitors to suppress endogenous Wnt secretion, this system has become what Schulte describes as one of the most important practical advances the field has seen in years. 6. Disheveled may regulate access to both G-protein and beta-catenin pathways through conformational selection Disheveled (DVL), the scaffolding protein downstream of frizzled, is not simply a beta-catenin pathway component. Schulte's lab has preliminary evidence that disheveled undergoes conformational selection at the receptor — analogous to the way G proteins adopt receptor-stabilized conformations before activating. This would mean the receptor itself determines whether a signal flows through disheveled or through a G protein depending on its conformational state, a form of pathway selectivity that remains to be fully mapped in the frizzled system. 7. A PhD lesson in pharmacological humility that lasted 25 years During his thesis seminar, Schulte presented data attributing an unexpected signaling connection to a kinase pathway he had dissected with pharmacological inhibitors. His supervisor, Bertil Fredholm, asked a single question: had he checked whether those inhibitors were also antagonists at the adenosine receptors under study? Several were — the signal Schulte had mapped was an off-target receptor effect, not the kinase pathway he had concluded. He describes the experience as formative, and the lesson as one that has quietly shaped his approach to chemical probes ever since. Episode Timeline Timestamps are AI-generated from the transcript and may not reflect the final edited video exactly. 00:00 Introduction 00:48 From Berlin to Stockholm — a career redirected by armed robbery 08:30 The adenosine receptor talk that pulled Schulte into GPCRs 11:14 From adenosine to frizzled: the postdoc decision that defined the lab 17:43 Frizzled receptors: 10 subtypes, 19 ligands, almost no drugs 20:22 When Wnt–frizzled signaling goes wrong — cancer, fibrosis, nail dysplasia 28:23 G-protein coupling specificity across the frizzled family 34:55 SAG1.3: repurposing a Smoothened compound to activate frizzled 6 40:51 Where beta-arrestin and disheveled fit in Wnt signaling 47:01 The class F CRISPR knockout cell line that changed everything 53:43 Conformational change as the strongest argument for GPCR identity 01:03:11 Career advice: explore widely, then commit to a niche Selected Quotes "The frizzles look like GPCRs, but the field is somehow split in people who believe they are and other people who don't believe they are. The biggest question is how we don't understand how the ligand interacts with the receptor, how the receptor really gets activated and how signaling is initiated and specified." "I think that is one of the interesting advances — we understand that a frizzled in a signaling system is not necessarily only the abbreviation FZD. It's also a number, because the individuals of the family are different. And I think that is not really particularly appreciated in the field, because we didn't know so far." "We clearly see that Wnt stimulation changes the conformation of the frizzles that we have looked at in the same way, or a similar way, as the GPCR acts. That is my strongest argument for the GPCR nature of these receptors." "It's not like in the good old adenosine receptor times, that we have the small molecule available and get crystal clear tenfold increase of a kinase phosphorylation or something." About Dr. Gunnar Schulte Gunnar Schulte is a Professor in receptor pharmacology and research group leader for the section Receptor Biology and Signaling at the Department of Physiology and Pharmacology. He has a background in biochemistry from the Free University in Berlin/Germany and a Ph.D. in molecular pharmacology (supervisor: Bertil B Fredholm; 1998-2002) from Karolinska Institutet. As a postdoc, he trained first with Ernest Arenas (Karolinska Institutet, Molecular Neurobiology; 2003-2005) and later with Roger J Summers (Monash University, Melbourne Australia, GPCR pharmacology; 2006) before starting his independent research team "Receptor Biology & Signalling" in 2008. Gunnar Schulte is also the scientific secretary of the Swedish Society for Medical Research (SSMF) and a member of the editorial board/editorial advisory board of Molecular Pharmacology, British Journal of Pharmacology, Pharmacological Reviews, and The Journal of Biological Chemistry. General Research Interest: The focus in the Schulte lab is on Frizzled signaling and pharmacology aiming to understand the role of WNT/Frizzled signaling in biology, physiology, and disease. Most importantly my research team tries to understand underlying mechanisms of WNT-receptor interaction, the relevance of receptor dynamics, and receptor complex composition for signal initiation and specification. The ultimate aim is to use the new knowledge to find, create and optimize Frizzled-targeting small molecule drugs to improve future therapies of human disease. Dr. Gunnar Schulte on the web Schulte Lab LinkedIn Google Scholar Orcid YouTube Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. David Sykes About Dr. David Sykes " David Andrew Sykes, BSc Hons Pharmacology, MSc Molecular Biology and Biochemistry, PhD in Molecular Pharmacology & Drug Discovery. David has over 20+ years of experience working in a drug discovery environment mainly in a specialist assay development role and most recently with Novartis. In 2014 David joined the University of Nottingham and began a part-time PhD in Molecular Pharmacology and Drug Discovery that he was awarded in 2020. During this period David has made a significant contribution to the understanding of agonist/ antagonist GPCR kinetic determinants in an area of growing scientific interest. His current interests include the development of HTS fluorescence-based kinetic binding assays specifically designed to assess the kinetics of unlabelled compounds (and chemical fragments) and the use of purified receptor/ effector proteins as tools for drug discovery. " Dr. David Sykes on the web Veprintsev Lab ResearchGate LinkedIn Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Pfleger on NanoBRET live-cell assays, receptor complex pharmacology, and what it took to move GPCR biology from HEK cells to phase 2 clinical trials. << Back to podcast list Strategic Partner(s) Pfleger: NanoBRET, Receptor Complexes, and the Translation of GPCR Pharmacology GPCR pharmacology has long depended on recombinant systems in which receptors are expressed and studied as isolated proteins. But in living tissue, GPCRs do not operate alone - they form dynamic complexes with other receptors, scaffold proteins, and cytoskeletal components, and those interactions reshape conformation, ligand binding, and signaling output in ways that isolated assays cannot detect. Kevin Pfleger's research at the University of Western Australia sits at the intersection of assay technology, receptor pharmacology, and translational medicine. His group developed BRET and NanoBRET-based live-cell platforms that capture protein-protein interactions and signaling dynamics in real time, preserving the kinetic information that endpoint assays routinely discard. Those platforms have been applied across arrestin biology, receptor complex pharmacology, and the angiotensin and chemokine receptor systems, including CCR2. The conversation also covers what it means when cell biology reaches the clinic. Pfleger co-founded a biotech company that completed phase 2 clinical trials in focal segmental glomerulosclerosis and diabetic kidney disease - and watching protein levels fall in patients' urine is, for him, the reason most scientists enter medical research in the first place. About the Guest Kevin Pfleger is Professor, Director of Biomedical Innovation, and Head of Molecular Endocrinology and Pharmacology at the University of Western Australia and the Harry Perkins Institute of Medical Research. His research centers on GPCR functional interactions, with a focus on arrestin signaling, receptor complex pharmacology, and the angiotensin and chemokine receptor systems. He developed BRET and NanoBRET-based live-cell assay platforms now widely adopted across the GPCR field, and serves as Deputy Director of the Australian Research Council Centre for Personalised Therapeutics Technologies. Pfleger co-founded a publicly listed biotech company that has completed phase 2 clinical trials in focal segmental glomerulosclerosis and diabetic kidney disease, and holds leadership roles across Australian biomedical innovation and entrepreneurship. Scientific Themes of the Conversation Real-time vs. endpoint assays - why kinetics change the pharmacological picture GPCR receptor complexes and the limits of isolated receptor screens Bias signaling as a kinetic and time-dependent phenomenon NanoBRET and the evolution of live-cell assay design for GPCR biology Academic entrepreneurship and the path from bench to phase 2 clinical trials Funding diversification and the transferable skills embedded in PhD training Key Insights from the Conversation 1. Endpoint Assays Can Miss the Biology Entirely A single measurement at a fixed time point collapses all the kinetic information in a signaling event into one number. Pfleger describes profiles where the peak of a response occurs early and then subsides - and where an endpoint assay taken after that peak would return a flat or misleading result. The problem is not the assay format itself; it is the assumption that one time point is enough. 2. Bias Signaling Is a Kinetic Problem, Not Just a Pathway Problem Spider plots comparing signaling bias across multiple pathways are a standard output in GPCR pharmacology. Pfleger challenges a silent assumption embedded in most of them: that the time point chosen for each measurement is irrelevant. If bias has a kinetic component - and the evidence suggests it often does - then what gets called "biased" may be an artifact of when you looked, not what the receptor is actually doing. 3. Receptors in Complexes Behave Differently Than Receptors in Isolation Standard drug screens present a receptor as a discrete, isolated target. In the body, that receptor is complexing with other receptors, scaffold proteins, and cytoskeletal elements - and those interactions alter its conformation and drug-binding properties. Pfleger argues this is not a theoretical complication; it is a pharmacological reality that current screening approaches largely bypass. Understanding receptor complexes is where the next layer of selectivity and specificity in drug discovery lives. 4. BRET Went From a Handful of Labs to the Go-To Platform When Pfleger began working with bioluminescence resonance energy transfer in GPCR research, it was a niche technology used by a small number of groups worldwide. That has changed. The development of NanoBRET - including live-cell ligand binding assays built on CRISPR-expressed receptors - contributed to an adoption curve that now spans most GPCR pharmacology labs. For Pfleger, the reach of the technology is not a source of pride as much as a signal that the field recognized what real-time, live-cell measurement offers that nothing else does. 5. The Long Road From HEK Cells to a Patient's Urine Pfleger describes a particular moment from the phase 2 clinical trial his spin-out company ran in kidney disease: seeing urinary protein levels fall in patients on the compound. He had spent years characterizing arrestin interactions with angiotensin and CCR2 receptors in cell-based systems, working through the logic of functional selectivity in disease-relevant pathways. That cell biology eventually became a clinical hypothesis, then a compound, then a trial result. What made it humbling, he notes, were the calls from patients' families asking to get into the trial. 6. The PhD Trains You for Far More Than the Bench The skills built during doctoral training - managing time, coordinating teams, working within resource constraints, communicating under uncertainty - map directly onto the skills required in industry, entrepreneurship, and scientific leadership. Pfleger made this case from personal experience: spending years pitching to rooms of executives taught him that the win-win logic he needed there was not foreign to scientific collaboration. It was the same logic, applied to different stakeholders. The analytical discipline of the PhD, he argues, is not a niche credential. It is a transferable toolkit most PhD students do not realize they have built. Episode Timeline Timestamps are AI-generated from the transcript and may require minor adjustment after final audio editing. 00:00 Introduction 01:36 Pfleger's philosophy: science as a team sport 03:54 From Cambridge to Edinburgh - an accidental PhD and the origin of a career 06:10 Working on biosignaling before the field had a name for it 09:12 Postdoc pivot: from GnRH receptors to arrestin interactions in Australia 12:47 The spin-out - how a discovery became a phase 2 clinical trial in kidney disease 16:56 Why grant-only funding is becoming unsustainable and what to do instead 22:21 What a PhD actually trains you for 25:42 NanoBRET, live-cell assay design, and the CRISPR ligand binding platform 27:54 Why endpoint assays miss the peak - the case for real-time kinetics 29:44 Bias signaling as a time-dependent measurement 32:26 Screening receptors in complexes, not in isolation 40:03 When cell biology reached the patient Selected Quotes "The number of times we see very interesting profiles and if you were to do an endpoint assay, you would completely miss the point because you've missed the peak. A lot of the time you get a signature, and you can compare those signatures and see a lot of nuance." "Traditionally screening has happened with receptors in isolation, but in reality, in the body, these receptors are complexing. They're interacting with the cytoskeleton, with other proteins, with other receptors, and that will change their conformation. That will change their ability to bind." "We were actually seeing the protein levels in the urine going down in the patients. That is really why I think most people get into medical research. It's very humbling." "A PhD is not just a training in working at a bench and writing a thesis. It's so many other things - whether it's about time management, people management, managing a budget. These are all business skills. And these are all skills that can be transferred." About this episode Dr. Pfleger trained as a pharmacologist and obtained his Ph.D. at the University of Edinburgh. I sat down with Kevin to chat about GPCRs, pharmacology, and his contributions to the field in both the academic and biotech worlds. Professor Pfleger has developed extensive expertise in profiling receptor binding and function at the molecular and cellular levels over the last 20 years, particularly involving GPCRs. He also has globally-recognized expertise in bioluminescence resonance energy transfer (BRET) technology, including his patented Receptor-Heteromer Investigation Technology (Receptor-HIT) for studying heteromers. Kevin is also Director, Biomedical Innovation at The University of Western Australia (UWA) and the MTPConnect Western Australian Life Sciences Innovation Hub. He is Head of Molecular Endocrinology and Pharmacology at the UWA Centre for Medical Research and Harry Perkins Institute of Medical Research, Deputy Director of the Australian Research Council Centre for Personalised Therapeutics Technologies, Chief Scientific Advisor to Dimerix, and co-founder of RAGE Biotech . He currently serves on the Board of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists and is a member of the British Pharmacological Society International Advisory Group. Join me and learn more about Kevin’s work and how he manages all his responsibilities. Dr. Kevin Pfleger on the web LinkedIn ResearchGate Pubmed Google Scholar University of Western Australia Harry Perkins Institute of Medical Research Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Inês Pinheiro, Monserrat Avila Zozaya & Yamina Berchiche About Inês Pinheiro PharmD by training and Ph.D. candidate in Hartley's lab at the University of Geneva. As a young researcher fascinated by chemokine receptors, molecular pharmacology, drug discovery, and immuno-oncology. Inês Pinheiro on the web LinkedIn University of Geneva Twitter Dr. GPCR Ecosystem About Monserrat Avila Zozaya I am a cell biologist interested in studying GPCRs, especially adhesion GPCRs. Motivated by my scientific passion, I recently started a postdoctoral fellowship to study the role of GPCRs in the mechanisms of pain and its comorbidities. Monserrat Avila Zozaya on the web Antony Boucard Lab Dr. GPCR Ecosystem About Yamina Berchiche Dr. Yamina A. Berchiche is the founder of Dr. GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors (GPCRs), that control virtually everything in the body, as drug targets. The mission of Dr. GPCR is to accelerate GPCR drug discovery by sharing the latest research and technology advances in the field and providing exposure to scientists through the Dr. GPCR podcast. Dr. Berchiche obtained her Master’s and Ph.D. in Biochemistry at the University of Montreal in Canada before training at The Rockefeller University in New York and the National Institutes of Health in Bethesda, Maryland. She developed expertise over the past two decades studying structure/function relationships of GPCRs using live-cell bioluminescence resonance energy transfer (BRET). Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the body. Yamina Berchiche on the web Website LinkedIn Facebook Twitter ResearchGate PubMed Google Scholar Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>