A conversation with Dr. Silvio Gutkind on keeping a cancer research lab running at 10% occupancy, why rotation students act like a sorting hat, and why breakthroughs come from working hypotheses that fail. << Back to podcast list Strategic Partner(s) Silvio Gutkind: Building a Lab That Doesn't Shut Down Conversations that happen when a research community faces a shared constraint reveal as much about scientific practice as any experiment. Dr. Silvio Gutkind joins this resilience conversation from the UCSD Moores Cancer Center, where cancer patients cannot wait for normalcy to return. For Dr. Gutkind — carrying a personal loss in New York and leading a cancer center building that operated at 93% capacity during the early pandemic — the question was not abstract. He had to decide, week by week, what could pause and what couldn't, and whose careers would bear the cost of getting it wrong. He walks through the structure his team built: staggered schedules at 10–15% occupancy, written contracts with every lab member, a Zoom-based communication cadence, and an internal directive to read, think, plan, and write. The constraint did not slow the science; it redirected it. Bioinformatics projects flourished. Collaborations that would have waited for conferences started immediately. A harder question surfaces underneath: how much of what we call a lab is its physical walls, and how much is the community, the plan, and the willingness to let a failed hypothesis open a new direction? About the Guest Dr. Silvio Gutkind is Professor and Associate Director for Basic Science at the UCSD Moores Cancer Center. His research spans GPCR signaling in cancer biology, head and neck squamous cell carcinoma, and the molecular circuitry that drives tumor progression. Before moving to La Jolla, he spent decades at the NIH, where he led a branch at NIDCR. That dual lineage — extramural academic and intramural NIH — shapes how he thinks about research infrastructure, student training, and scientific community. Scientific Themes of the Conversation Institutional resilience and the architecture of a research lab under constraint The contract between scientific leadership and trainees during crisis Communication infrastructure as a substitute for physical proximity Chance and opportunity as drivers of a scientific career Rotation students as cross-pollinators between labs Why breakthroughs tend to come from working hypotheses that fail Key Insights from the Conversation Cancer centers don't get to pause. Dr. Gutkind describes operating his cancer research building at 93–94% capacity during the early pandemic because cancer patients couldn't wait for normalcy. The question was never whether to stay open — it was how to stay open safely, and how to absorb the stress that came with that responsibility. The NIH shutdown playbook made UCSD ready. Years at the NIH, where federal shutdowns were routine, gave Dr. Gutkind a pre-built mental model for what to freeze, what to protect, and what to let continue. When the pandemic hit, he reached for an infrastructure he already had. Every lab member needed a contract. Rather than making ad hoc decisions about who would come in and when, the team wrote down expectations — hours, distancing, critical versus deferrable work, and an explicit clause that no one should feel pressured to be on-site. The contract wasn't bureaucracy; it was protection, especially for students. The bioinformatics arm called it "heaven." Computational scientists suddenly had uninterrupted time at home with full data access and far fewer meetings. Dr. Gutkind reports that five years' worth of ideas accumulated in that stretch — more than the lab can realistically work through. "Physical distancing," not "social distancing." A small language correction with structural weight. Dr. Gutkind argues the scientific community grew closer during the pandemic, not further apart — the physical space contracted, but the community expanded through Zoom, shared drives, and unhurried collaboration conversations. Rotation students function like the sorting hat. Because trainees rotate through multiple labs, they carry science from one bench to another. Dr. Gutkind credits several of his most valuable collaborations to a rotation student recognizing a fit that no PI would have spotted from across campus. Breakthroughs come from working hypotheses that fail. Dr. Gutkind reflects that the most significant advances in his career didn't come from confirming a premise — they came from digging into why the premise broke. The discipline is not in being right, but in being willing to let go of the framework you built when the data refuses to fit it. Episode Timeline Timestamps were generated using AI for readability. 00:00 Welcome and introduction 01:46 Navigating research during the pandemic 03:30 Why cancer research couldn't stop 04:30 The NIH shutdown playbook 05:20 Writing the contract: occupancy, staggering, communication 06:50 The productivity paradox — "it's like heaven" 07:55 What will change after the pandemic 09:20 "Physical distancing, not social distancing" 11:31 Chance versus scientific knowledge in a career 12:20 Rotation students as the sorting hat 13:20 When the working hypothesis fails 14:30 Closing Selected Quotes "We have many more ideas than we can handle for at least the next five years." "I wouldn't call it social distancing — I would call physical distancing… as a community, we are even stronger." "These rotation students are like cross-pollination… almost like the sorting hat in Harry Potter." "Quite often, our breakthroughs are more often from when the working hypothesis did not work. The breakthrough came from getting deeper into why." About this episode Dr. J. Silvio Gutkind sheds light on his work and life since the beginning of COVID restrictions. A large component of his work is centered around dysregulated signaling in cancer and the development of novel mechanism-based cancer therapies. In this episode, Dr. J. Silvio Gutkind highlights how his past experience proves useful in current COVID times and potential benefits the changes in work environments can do for future collaborations. Dr. J. Silvio Gutkind on the web Gutkind Lab – UC San Diego Moores Cancer Center Gutkind Lab publications More Publications from the Gutkind Lab on Pubmed Dr. J Silvio Gutkind on LinkedIn Gutkind Lab on Twitter UCSD Moores Cancer Center Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Get ready to connect, collaborate, and innovate at the Dr. GPCR Retreat — an immersive event uniting scientists, biotech leaders, and innovators in GPCR research. Dr. GPCR Retreat - Coming Soon - Please tell us your thoughts about scientific gatherings by filling out this short survey

Join the Dr. GPCR Affiliate Program and earn commissions by helping connect the global GPCR community. Share our ecosystem, courses, and events to advance drug discovery together. Dr. GPCR Affiliate Program Earn by Empowering the GPCR Ecosystem Help us connect scientists, founders, and innovators while earning commissions for every member, partner, or course you bring into the Dr. GPCR community. Become our Brand Ambassador Our vision is to build the best platform for the GPCR community and help you the scientists and business owners to share their experiences with others, get help, and find the perfect tools, colleagues, build their strategy and advance our field. As an ambassador, with the Affiliate Program, you'll earn a commission whenever your referral link is used and a qualified purchase has been made by your friends, colleagues, or followers who are also part of the GPCR field. Become our Brand Ambassador About Dr. GPCR Ecosystem We aspire to provide opportunities to connect, grow, and thrive together as a dynamic group. The goal is to better understand and exploit the druggability of GPCRs, together. The Dr. GPCR Ecosystem members have the opportunity to solve problems, find answers to their questions, identify the perfect service provider, and, most importantly, boost their GPCR project with just a few clicks. The Ecosystem is designed for all GPCR professionals to have an affordable and highly effective way to showcase their knowledge, connect, and advance the field, together. About the Dr. GPCR brand ambassador affiliate program Who can be a Dr. GPCR ambassador? Scientists and trainees with a strong GPCR background who like and want to create content by writing articles about their favorite GPCR topics and sharing these on social media platforms such as LinkedIn and other options listed at the end of this page. Who is eligible for the Dr. GPCR affiliate program? A GPCR background is mandatory independent of your current position and industry. You also must be an individual Dr. GPCR Ecosystem membership holder. For full details on eligibility, please read our Affiliate Policy . How do I apply for the affiliate program? To become an affiliate, you must create an account here . How does the Dr. GPCR affiliate program work? After becoming a member of the affiliate program, you'll get your personalized link where you can send your potential clients. After every qualified sale, you will earn a commission of $50. How does the commission work? Each qualifying sale earns a commission (excluding sale cancellations). Does it cost me anything to become an affiliate? The program is free to join; there are no monthly charges and no minimum sales requirements. However, the number of ambassador members is limited. Dr. GPCR reserves the right to remove the least active members from the program. Can I invite someone to participate? Yes! You can invite anyone to participate, and we welcome anyone if they are qualified. Do I need to sign a contract? There's no contract to sign when joining our program. You will be required to agree to our Terms and Conditions and our Affiliates Policy when you sign up on Ecosystem.DrGPCR.com. You can leave the program at any time by contacting us. Dr. GPCR may also remove affiliates from the program at any time. Is there an exclusivity agreement when joining? There's no exclusivity agreement. You can take part in other affiliate programs as well as be part of ours. Are affiliates outside of the U.S. eligible for the Affiliate Program? Yes, you may join the affiliate program as long as you have a verified PayPal account. What type of channels, tools, and techniques can I use to promote Dr. GPCR Ecosystem? OK to use: - Writing, blogging, guest blogging, - Podcast, video, vlog - Social media sharing, - YouTube & TikTok channels, - Business Page and website, - Informational and fan sharing, - Presentations and meetups. Not OK to use: Advertising Spam Anything misleading or annoying Social media bios Paying or offering intensives for the use of your link How do I track my earning? We use a third-party provider, GoAffPro.com , where you'll create your own account and through your dashboard, you can track all your activities. When will I receive my affiliate commissions? Affiliate payments are processed and sent directly to your PayPal in 7 to 30 days. We could hold payments up to 30 days to allow for processing, chargebacks, etc. Good Faith We introduce programs such as the Dr. GPCR Ambassador, in good faith and expect the same good faith in return. Please note that we may withhold awards where we believe customers are acting in bad faith or otherwise acting contrary to the intent of this program. To be clear, commercializing, advertising, publishing, mass distributing, selling, or paying for the use of referral links is not appropriate, and we will not honor such links. We cannot cover every nefarious scenario, nor will we attempt to, but we do promise to be fair and reasonable. Closure We are so excited about the Dr. GPCR Ambassador program. It will be a remarkable journey and fun to build together the "next-generation" platform for the B2B industry. With your help, we can create a world where the living experience is joyful and worry-free. Are you ready? Sign up , explore, and connect with us. Become our Brand Ambassador

Discover our transparent and fair affiliate policy, supporting Dr. GPCR Ecosystem. Join us to make a positive impact while earning commissions. << Back Affiliate Policy Dr. GPCR Ambassador Program Dr. GPCR, Corp., (“Dr. GPCR”) provides its Service to you through our websites referred to as Dr. GPCR, Ecosystem.DrGPCR.com , DrGPCR.com . Dr. GPCR Affiliate Program ( DrGPCR.com , Ecosystem.DrGPCR.com ) offers eligible affiliates, including blogs and other third-party websites (“Affiliates”), the opportunity to earn commissions on qualifying sales that originate from links to the Ecosystem.DrGPCR.com website on an Affiliate’s site. This Affiliates Policy explains your rights and responsibilities when participating in the Dr. GPCR Affiliates Program. This policy is a part of our Terms of Use . By participating in the Dr. GPCR Affiliates Program, you agree to this policy and all legal documents. 1. Eligibility and Enrollment in Dr. GPCR Affiliates Program Prospective eligible affiliates must apply and be approved by Dr. GPCR to gain access to the Affiliate Program. The Affiliate program is only available to individual members who have paid their yearly membership fees in full. Group membership holders are excluded from the Affiliate Program. Prospective eligible affiliates are evaluated based on criteria such as type of site, site quality, site content, variety of site content, social media content, and, most importantly, scientific knowledge. During the application process, prospective eligible affiliates may be asked to provide additional information to support any listed criteria. The following types of websites are prohibited from participating in the Affiliates Program: “Cash-back” or voucher sites (websites that offer rewards for buying goods through referral links); Price comparison sites; Sites using “pop-ups” or “pop-unders” (websites that launch “pop-up” or hidden windows on users’ browsers); Sites that violate the Dr. GPCR Trademark Policy ; Sites that exist solely to promote Dr. GPCR & Dr. GPCR Ecosystem; Sites with content related to sexual, religious, political, or other sensitive matters. Prospective eligible affiliates must apply, and approved affiliates must enroll directly through Ecosystem.DrGPCR.com . Signing up to the program via a sub-network is not permitted. Affiliates may leave the Affiliate Program and terminate this agreement at any time by sending an email to Hello@DrGPCR.com . Dr. GPCR reserves the right to remove Affiliates from the Affiliate Program and refuse service to anyone, for any reason, at any time. Participation in the Affiliate Program may be limited to affiliates located in certain countries and is void where prohibited by law. Dr. GPCR reserves the right to approve or reject any application to join the Affiliate Program for any reason. Depending on where an affiliate is located, they may be subject to varying regulations regarding endorsements and testimonials. For example, in the United States, the Federal Trade Commission outlines specific requirements regarding disclosure. The affiliate's responsibility is to be aware of and comply with any applicable regulations that pertain to their site. Dr. GPCR cannot provide legal advice; we urge you to consult a legal expert if you believe these or other regulations may apply to you. 2. Commission Rates, Qualifying Sales, and Payment As an affiliate, you can receive commissions for qualifying sales. Commission rates are determined on a case-by-case basis and may vary based on various factors such as the type of site and content. Commissions may increase during limited-time special promotions. The current commission rate is: $100 (January 2022) Qualifying sales are sales made on the Ecosystem.DrGPCR.com or DrGPCR.com websites by users who arrived on the Dr.GPCR sites by clicking an approved link on an Affiliate’s site (an “Affiliate Link”). Affiliate links will be sent to you after approval, including URLs, banners, or other creative assets. The affiliate may not alter any text links or creative assets made available through the Affiliates Program platform to receive payment. Affiliates are also requested not to hardcode Affiliate Links into their sites. The Affiliate Program uses unique links to verify qualifying sales. Commissions are paid on qualifying sales made through the affiliate's unique links. This means that an Affiliate can receive a commission for a qualifying sale if the deal was created. Commissions are not paid on sales that are canceled. Commissions are subject to review and other limitations for fraudulent activity. Dr. GPCR reserves the right to withhold commissions if fraudulent activity is found. Dr. GPCR pays affiliates via a PayPal account, provided to us when a member joins. If the PayPal email address changes, it is the affiliate's responsibility to notify the Affiliate Program of the changes to ensure proper commission payments. The affiliate is responsible for the entire amount of PayPal's processing fees when payments are made. Dr. GPCR will be solely responsible for processing every order placed by a customer via affiliate links. Affiliates are not authorized to collect payments or sell Dr. GPCR membership or products from other websites as a “reseller,” and no “resale” rights are granted in ANY way. Affiliates are not authorized to sell any of these products on auction sites. Affiliates are not permitted to give away copies of any of these products. Dr. GPCR will also be solely responsible for all customer service inquiries. All affiliates understand and acknowledge that no physical products will be shipped. 3. Program Restrictions Affiliates that violate any of the following program restrictions may be suspended or removed from the Dr. GPCR websites and may not receive any commissions. Paid Search Dr. GPCR maintains a strict policy on paid search activity. Affiliates must comply with the following conditions on any ad platform, including, but not limited to, search engines, content networks, and social networking sites: Affiliates are not permitted to bid or appear on searches that include the term “Dr. GPCR”, "DrGPCR", "Doctor GPCR", "Ecosystem Dr. GPCR", "EcosystemDrGPCR". Dr. GPCR Ecosystem", DrGPCREcosystem";- Affiliates are not permitted to bid or appear on extended or hybrid searches that include the terms “Dr. GPCR”, "DrGPCR", "Doctor GPCR", "Ecosystem Dr. GPCR", "EcosystemDrGPCR". Dr. GPCR Ecosystem", DrGPCREcosystem"; Affiliates are not permitted to bid or appear on misspellings or variations of searches that include the terms “Dr. GPCR”, "DrGPCR", "Doctor GPCR", "Ecosystem Dr. GPCR", "EcosystemDrGPCR". Dr. GPCR Ecosystem", DrGPCREcosystem"; Affiliates are not permitted to use Dr. GPCR trademarks in any paid search activity, including ad text, ad copy, or display URLs; Affiliates are not permitted to direct link PPC activity to the Dr. GPCR sites; this includes using the DrGPCR.com or Ecosystem.DrGPCR.com website as a display URL; Affiliates are not permitted to send traffic through automatic redirects on a website page;- Affiliates are not permitted to use the Dr. GPCR name (including misspells and variations) as a sub-domain or sub-folder. Responsibility for Your Site You are solely responsible for your website, including its development, operation, maintenance, and all materials that appear on or within it. Dr. GPCR disclaims all liability for your site, social media, and other content, and any of your users’ claims relating to your site, and you agree to defend, indemnify, and hold Dr. GPCR harmless from and against all claims relating to your site. 4. Modification Dr. GPCR may modify any of the terms and conditions within the Affiliate Agreement at any time, at its sole discretion. These modifications may include, but are not limited to, changes in the scope of available referral fees, fee schedules, payment procedures, and Affiliate Program rules. If any modifications are UNACCEPTABLE TO YOU, your only recourse is to terminate this Agreement. If you CONTINUE PARTICIPATION IN THE PROGRAM following the changes in the new agreement, it will be considered your acceptance of the change. Are you ready? Sign up, explore, and get in touch with us. Become our Brand Ambassador Please read carefully our Legal Policies and Disclaimers to understand how Dr. GPCR conducts business Affiliate Policy Content and Conduct Policy Content Guidance Privacy Policy Terms and Conditions Trademark Policy

<< Back to podcast list Strategic Partner(s) Dr. Nyla Naim, Dr. Michael Lemieux & Dr. Jason Nasse About Dr. Nyla Naim Nyla is a Senior Scientist on the Scientific Support Team at Addgene . She received her Ph.D. at the University of Pittsburgh and continued her postdoctoral research at the University of Vermont studying cellular signaling, biosensors, and optogenetics. Nyla supports biomedical research by connecting researchers with resources and promoting reproducible science. Dr. Nyla Naim on the web LinkedIn Dr. GPCR Ecosystem About Dr. Michael Lemieux ''My name is Michael (Mike) Lemieux and I am a Connecticut native. I completed my Ph.D. in molecular and cell biology at UConn and then joined Addgene as a Quality Control Scientist in 2015. Since then I transitioned into a Scientific Support role to leverage my passion for helping people! Beyond my interest in science, I am a strong advocate for graduate education reform and I love to write.'' Dr. Michael Lemieux on the web Addgene Blog Dr. GPCR Ecosystem About Dr. Jason Nasse Dr. Jason Nasse is a senior scientist at Addgene specializing in the use of AAV viral vectors. He obtained his Ph.D. in Neuroscience from Ohio State University focusing on synaptic plasticity and adrenergic receptor modulation of both pre-and postsynaptic properties. By taking a very non-traditional path to obtain a Ph.D. Dr. Nasse has had the opportunity to experience how science is performed across different sectors and around the country. Prior to his role at Addgene, Jason held roles in academia, big pharma, and non-profit research organizations. Dr. Jason Nasse on the web LinkedIn Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Five scientists audit what AI can and can't do for GPCR drug discovery — from orphan receptors and biased signaling to the true-negatives problem nobody writes into grant proposals. Recorded at the 3rd EARNEST meeting. << Back to podcast list Strategic Partner(s) EARNEST Panel: Can AI Accelerate GPCR Drug Discovery? In October 2020, five scientists gathered virtually at the 3rd EARNEST meeting to debate a question that has only grown more urgent: can artificial intelligence actually accelerate GPCR drug discovery, or is it mostly a rebranding of methods the field has used for decades? Panelists from InterAx Biotech, Rockefeller University, and the University of New Mexico — computational chemists, systems biologists, structural biologists, and drug-discovery veterans — drew on their combined experience to separate what machine learning can credibly do for GPCR research from what still depends on pharmacological judgment. The conversation moves from definitional clarity (AI is not machine learning, and neither is simple computational modeling) to the practical realities of building usable datasets, deorphanizing receptors, handling generative models, and confronting the true-negatives problem that quietly breaks so many published models. For any scientist whose grant proposal now contains the phrase "machine learning" whether they fully believe in it or not, this panel is an honest audit of what the technology can deliver today and where it still falls short. About the Panelists Dr. Maria Waldhoer is Chief Scientific Officer at InterAx Biotech in Switzerland. A pharmacologist by training, she spent more than six years in early R&D at Novo Nordisk before turning to systems biology approaches for connecting in vitro signaling data to in vivo drug behavior. Dr. Aurélien Rizk is Chief Technology Officer at InterAx Biotech. Trained as a mathematician and computer scientist, his doctoral work focused on developing new methods for modeling GPCR signaling pathways. Dr. Yaroslav Nikolaev is a scientist at InterAx Biotech with a dual background in biology and computation. His research combines biomolecular NMR, structural biology, and machine learning to study how GPCRs function dynamically. Dr. Thomas Sakmar has run a laboratory at Rockefeller University for roughly thirty years. His group contributed to the early cloning of GPCRs in the mid-1980s and has since pushed the boundaries of GPCR biochemistry — including early homology modeling, coarse-grained molecular dynamics, and genetic code expansion for site-specific chemistry on receptors. Dr. Tudor Oprea is Principal Investigator at the University of New Mexico and coordinator of the Illuminating the Druggable Genome Knowledge Management Center. An MD-PhD who has practiced machine learning since 1989, he built Pharos, the public-facing data platform for the IDG program, and co-developed G1, the first agonist for GPR30, which reached an IND for melanoma. Scientific Themes of the Conversation The definitional boundary between AI, machine learning, and computational modeling Data quality as the rate-limiting step for machine learning in GPCR pharmacology Orphan receptor deorphanization and the limits of learning from known peptides Generative models, scoring functions, and the role of molecular dynamics in ligand design The true-negatives problem and how it distorts biological models The hybrid future: chemical intuition, experimental judgment, and where computation still falls short Key Insights from the Conversation AI and machine learning are not the same thing, and the difference matters. Machine learning finds patterns in defined datasets; AI aims to substitute for human reasoning more broadly. Using the terms interchangeably blurs what each approach can realistically deliver in a pharmacology workflow. The barrier isn't messy data — it's missing metadata. Most pharmacology datasets aren't useless for ML; they're incomplete. Buffers, incubation temperatures, time points, co-expression conditions, the specific Emax reference — these are the details that determine whether a dataset can be pooled with others or must stand alone. Deorphanization via AI is possible, but constrained by what we already know. Random-forest classifiers trained on known peptide ligands can find new orphan-receptor pairings. But the remaining orphans may be orphans precisely because they don't resemble anything we've characterized — which caps what this class of model can find. The bottleneck in structure-guided ML isn't the algorithm. The panel agreed that the real limits are the availability of high-resolution GPCR structures and the computational cost of molecular dynamics simulations needed to capture the dynamic conformations behind signaling. True negatives quietly wreck biological models. Most published models rely on inferred negatives — genes or molecules assumed inactive by convenience. When one panelist replaced inferred negatives in an autophagy model with CRISPR-validated true negatives, the model's predictions changed radically. Chemical intuition has no AI equivalent yet — and won't soon. The experience of a seasoned medicinal chemist mentally docking a molecule from a 2D structure is not a skill current models replicate. The panel expects a hybrid future, not a replacement one, for the next five to ten years. Olfactory GPCRs remain a trillion-dollar opportunity the field has largely ignored. GPCR-targeting drugs represent roughly 0.9 trillion dollars in global sales across 75 countries. Olfactory GPCRs — which account for a large fraction of the receptor class — have been systematically sidestepped for lack of tractable in vitro screening methods. Episode Timeline 00:00 Welcome from Yamina Berchiche 01:36 Panelist introductions 11:41 AI vs machine learning — the definitions that matter 15:21 The undrugged majority: 400 non-olfactory GPCRs, only 160 drugged 20:12 What makes a pharmacology dataset usable for machine learning 24:41 Advice for small academic labs entering the field 30:34 Can AI help deorphanize understudied receptors? 37:01 Reading GPCR signaling dynamics with computational models 39:53 Generative models, scoring functions, and molecular dynamics 50:32 The true-negatives problem and the limits of inferred datasets 52:30 Hype vs reality in AI drug discovery 55:05 Where the GPCR field goes in the next five years Timestamps were generated using AI for readability. Selected Quotes "My computational team told me, 'this receptor is not using arrestin to internalize. There has to be an arrestin-independent thing there.' And I'm like, that's rubbish. Never picked it up. Complete rubbish. And then a year later or so, I get a call from a colleague who said, 'oh, we've tested this compound as a negative control because we thought it doesn't need arrestin to internalize. And now we put it in this CRISPR knockout cell and — it does.'" — Dr. Maria Waldhoer "In 1989, as a med student in Romania, I used BASIC to model the variation in heart rate and blood pressure for 11 patients. I wrote an 11 polynomial that fit everything, so I thought I had solved the problem with drug discovery. I have learned a lot since." — Dr. Tudor Oprea "Dan Rich worked on HIV protease inhibitors. He would look at the 2D structure and basically mentally do a docking and tell you whether that's a good protease inhibitor or not. I think there are people who have worked in the GPCR field that can do a similar exercise." — Dr. Tudor Oprea "If you only make big enough numbers, big enough networks, big enough algorithms, suddenly intelligence pops out on the other side. [Roger Penrose] said, well, it's simply because they cannot think of anything else to do yet." — Dr. Maria Waldhoer About this episode Listen to this fantastic round table discussion that I had the privilege to moderate with Alexander Hauser . Our guests were Maria Waldhoer , Tudor I. Oprea , Thomas Sakmar , Aurelien Rizk & Yaroslav Nikolaev . The explosion of biomedical data such as in genomics, structural biology, and pharmacology can provide new opportunities to improve our understanding of human physiology and disease. In recent years, machine learning (ML) and artificial intelligence (AI) methods have received a significant boost in attention. ML/AI can be powerful for identifying abstract patterns within large data where traditional methods would be oblivious to. This comes without the need for manual feature engineering as systems can learn through implicit rules from the data provided. G protein-coupled receptors (GPCRs) mediate a vast variety of critical biological processes and provide an ideal case study for quantitative, and multi‐scale integration of these amounts of data to gain novel insights into receptor biology. How can we best leverage these exciting new techniques in areas such as protein structure prediction, bioactive ligand discovery, in-vivo translation ability, or in our understanding of signaling determinants? Here, we would like to discuss the opportunities, weaknesses, and advantages of these new technologies, which may contribute to probe our favorite targets at all scales. For more information on the ERNEST network, visit https://ernest-gpcr.eu/ . Dr. Yamina Berchiche on the web Website LinkedIn Publications Twitter Facebook Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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. Stephen Ferguson The History of the Great Lakes GPCR Retreat with Dr. Stephen Ferguson About Dr. Stephen Ferguson Dr. Stephen Ferguson is a Professor in the Department of Cellular and Molecular Medicine at the University of Ottawa. He did B.Sc. in biology at McGill University and received his Ph.D. under the mentorship of Dr. Brian Collier in the Department of Pharmacology and Therapeutics at McGill University (1994). He did his postdoctoral training with Dr. Marc G. Caron at Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking, and signaling. He has held four Canada Research Chairs since 2001 and was previously a Heart and Stroke Foundation of Canada MacDonald Scholar (1998-2003) and Heart and Stroke Foundation of Ontario Career Investigator (2003-2016). He was a recipient of Canada's Top 40 under 40 award in 2004 and received Queen Elizabeth II, Diamond Jubilee Medal, in 2012. He has also received both Junior (2001) and Senior (2005) investigator awards from the Pharmacological Society of Canada. Most recently, in 2021, he was elected as a Fellow of the Canadian Academy of Health Science (FCAHS). His research career has focused on the investigation of the regulation of G protein-coupled receptors signaling mechanisms in health and disease. He currently holds multiple research grants from the Canadian Institutes of Health Research (CIHR) for his research investigating the role of metabotropic glutamate receptor signaling in Huntington’s and Alzheimer’s disease. Dr. Stephen Ferguson on the web Carlton University Canada Research Chairs Twitter ResearchGate LinkedIn Dr. GPCR Ecosystem Great Lakes GPCR Retreat on the web 21st Great Lakes GPCR Retreat More about previous GPCR Retreat meetings Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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. Kathleen Caron About Kathleen M. Caron Kathleen M. Caron, Ph.D. is the Frederik L. Eldridge Distinguished Professor and Chair of the Department of Cell Biology & Physiology at The University of North Carolina at Chapel Hill—a large, interdisciplinary basic science department currently ranked 1st in the Nation in NIH funding. Dr. Caron received a BS in Biology and BA in Philosophy at Emory University and a PhD at Duke University while training with Dr. Keith Parker to elucidate the role of steroidogenesis in regulating sexual determination and adrenal and gonadal development using genetic mouse models. She pursued postdoctoral training with Nobel Laureate Dr. Oliver Smithies at UNC-CH, where she was the first to discover the essential role of adrenomedullin peptide for embryonic survival. With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular biology, the Caron laboratory has gained valuable insights into the genetic basis and pathophysiology of lymphatic vascular disease, preeclampsia and sex-dependent cardiovascular disease. Dr. Caron has received numerous awards including a Burroughs Wellcome Fund Career Award in the Biomedical Sciences, an Established Investigator Award and an Innovator Award from the American Heart Association, a Jefferson Pilot Award in Biomedical Sciences and a UNC-CH Mentoring Award. She currently serves as Associate Editor of Physiological Reviews; the #1 ranked journal in Physiology (IF 46.5). Dr. Caron is also past Associate Editor at JCI and served as the inaugural Associate Editor at ACS-Pharmacology and Translational Science. Dr. Caron currently holds multiple scientific advisory roles in academia, industry and the National Institutes of Health. Kathleen M. Caron on the web Lab Website Twitter Pubmed Google Scholar Orcid Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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) The Scientist's Compass: From Academia to Entrepreneurship with Dr. Dmitry Veprintsev In this episode, Yamina sits down with Prof. Dmitry Veprintsev , a molecular pharmacologist at the University of Nottingham, to discuss his scientific journey, GPCR research, and the intersection of academia and entrepreneurship. Key Takeaways: From Protein Folding to GPCRs – How Dmitry transitioned from biophysics and protein folding to cannabinoid receptor research, guided by key mentors like Michel Bouvier. Why GPCRs? – The challenge and excitement of working with notoriously difficult-to-study membrane proteins. The Power of Asking the Right Question – Dmitry emphasizes that mastering a technique isn’t enough—true scientific breakthroughs come from formulating the right biological questions. Building Z7 Biotech – The unexpected journey into biotech entrepreneurship, providing GPCR profiling services to pharma and biotech companies. Interdisciplinary Research & Future Directions – Exploring combinatorial drug actions, receptor interactions, and novel profiling approaches. Networking & Career Growth – Overcoming introversion, the importance of talking to people, and how networking (or just genuine curiosity) opens doors in science. 💡 Big Takeaway? Whether in academia or industry, success comes from curiosity, persistence, and knowing your values. Tune in to hear how Dmitry navigated his career, the challenges of studying GPCRs, and why talking to others will always lead to answers! Summary made with AI About Dmitry Veprintsev Dmitry is Professor of Molecular and Cellular Pharmacology at the Centre of Membrane Proteins and Receptors (COMPARE), University of Nottingham, where he provides leadership in structural and biophysical pharmacology of G protein coupled receptors. He is author of over 100 papers, including several in Nature, Science and Cell. Dmitry studied biophysics at the Moscow State University, followed by a PhD (1998) in protein folding at the Russian Academy of Sciences and at the Ohio State University, USA. He joined the MRC Centre for Protein Engineering and later at the MRC Laboratory of Molecular Biology in Cambridge, UK as a postdoctoral fellow and later as a staff scientist, focusing on the biophysical studies of the tumour suppressor p53. In 2010 he became a group leader at the Paul Scherrer Institute and ETH Zürich in Switzerland, changing his attention to structural pharmacology of G protein-coupled receptors (GPCRs). In 2017 Dmitry became a full professor at the Centre of Membrane Proteins and Receptors, COMPARE, a joined venture between the University of Birmingham and the University of Nottingham. In 2021 he co-founded Z7 Biotech, developing and providing innovative GPCR drug screening and precision pharmacology services. Dmitry Veprintsev on the web LinkedIn Veprintsev Lab Z7 Biotech University of Nottingham Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Access expert CRO advisory services through the Dr. GPCR Ecosystem. Get guidance, strategies, and insights to optimize your GPCR research and drug discovery projects. Home About Services News Get in Touch Welcome CRO & Vendor Advisory Your Science Is Strong. Your Process Should Be, Too. I help CRO teams bring structure to collaboration—so your data gets acted on, not overlooked. When biotech partners trust your process, they come back again and again. You deliver high-quality data. But when timelines shift, expectations blur, or feedback loops break down, even the best work can lose momentum. Let’s turn your scientific rigor into results that move programs—and people—forward. Power My Discovery Biotech Clients Want Results - Not Confusion Every CRO I work with has great science—but clients still struggle to understand the value. Here's what I hear from biotech teams: “We’re not sure what we’re getting—or when we’re getting it.” “The science is solid, but the communication is scattered.” “The data looks fine, but it doesn’t help us make decisions.” Great science isn’t enough if clients don’t feel aligned, informed, and in control. That’s where I come in. How I Help CROs Deliver High-Impact Science That Biotech Teams Trust Biotech Clients Stay in Sync With Your Team I work to strengthen communication & collaboration: • Facilitate smoother communication between technical teams and biotech clients • Set clear expectations and deliverables to build trust and reduce delays • Align teams across roles—from assay execution to client updates Data Turns Into Decisions—Not Delays I help turn great science into clear deliverables • Define program objectives and guide assay plans that support partner decisions • Translate discovery data into clear, actionable formats biotech teams can use • Streamline deliverables to reduce review cycles and accelerate go/no-go calls & shorten timelines Your Science Stays Focused on What Matters We work together to position your CRO for growth • Refine your offering to match what biotech teams actually need • Position your services to shorten sales cycles and increase repeat business • Turn client feedback into improvements that boost trust and outcomes Here's What CROs Are Saying "Before working with Yamina, we were generating high-quality data across biotech programs but often navigating evolving expectations and goals from different stakeholders. After partnering with her, communication became clearer, deliverables were better defined, and collaboration across teams ran more smoothly. She helped streamline complex projects and made the CRO–client relationship more effective and productive." - Anne Marie Quinn, CEO Montana Molecular Frequently Asked Questions 01 What kinds of CROs do you work with? Any CRO focused on GPCRs, pharmacology, discovery biology, or antibody discovery—regardless of size or location. 02 What happens when I reach out? We'll start with a focused conversation about your programs and current challenges. You'll leave with clarity—even if we don't end up working together. 03 Can you help on an ongoing basis? Yes. I offer both short-term consulting and ongoing partnerships depending on your needs. Power My Discovery Send me a message First name* Last name Company name* Email* How Can I Help?* Send Message or Book My Call Menu Home Services About Ready to collaborate? Let’s talk about how I support GPCR discovery, pharmacology strategy, and cross-functional execution across biotech, VC, and CRO teams. Get in touch Connect LinkedIn Podcast Dr. GPCR Calendly ©2023-2025 All rights reserved by FindYooour, LLC & Dr. GPCR Corp Proudly created with Wix.com

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 Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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. Foord reflects on discovering RAMPs, deorphanizing GPCRs, and navigating industrial GPCR pharmacology, target validation, and drug discovery strategy. << Back to podcast list Strategic Partner(s) Foord: Serendipity, RAMPs, And Industrial GPCR Pharmacology Scientific Abstract This conversation traces how GPCR pharmacology, receptor signaling, and drug discovery evolved inside one of the world’s largest pharmaceutical organizations. Dr. Foord reflects on his path from academic neuroendocrinology to introducing molecular biology and molecular pharmacology into Glaxo’s GPCR programs, and on the combination of rigor, bioinformatics, and serendipity that led to several influential discoveries. He describes the purification and cloning of the CGRP receptor, the identification of receptor activity-modifying proteins (RAMPs), and the realization that CGRP signaling required receptor complexes rather than a single seven-transmembrane protein, reshaping thinking about peptide receptor activation and ligand binding. Dr. Foord also discusses work on angiotensin, GABA B, free fatty acid, nicotinic acid, and prostaglandin EP4 receptors, showing how orphan receptors were deorphanized using expression systems, electrophysiology in Xenopus oocytes, and early bioinformatics. The discussion highlights the gap between identifying a target and delivering a drug, the challenges of target validation, and the realities of industrial decision-making around receptor selectivity, safety, and market focus. Along the way, Dr. Foord reflects on the limits and promise of human genetics, the underexploited potential of GPCR antibodies, and the importance of team composition, negative data, and scientific community in navigating complex receptor biology. About the Guest Dr. Foord is a physiologist and pharmacologist who spent more than two decades at Glaxo, Glaxo Wellcome, and GlaxoSmithKline working on GPCR pharmacology and drug discovery. Trained in neuroendocrinology, he helped bring molecular biology into traditionally pharmacology-driven GPCR programs and worked across migraine, cardiovascular, pain, and inflammation projects. His work contributed to the identification of RAMPs in the CGRP receptor system, deorphanization of several GPCRs including GABA B and carboxylic acid receptors, and discovery of a prostaglandin EP4 modulator that advanced as a drug candidate. Later in his career, Dr. Foord led bioinformatics for neuroscience and played a central role in GSK’s early large-scale genetics initiative, integrating GPCR targets, ion channels, transporters, and ligands into association studies. His experience spans receptor cloning, expression systems such as Xenopus oocytes, electrophysiology, molecular pharmacology, and the use of informatics to mine sequence, structural, and genetic data for new receptor targets. Key Insights from the Conversation RAMPs Reframed Peptide GPCR Pharmacology . Dr. Foord explains how attempts to clone the CGRP receptor from SK-N-MC cells, combined with highly sensitive cAMP readouts in Xenopus oocytes, unexpectedly pulled out RAMP1 rather than a conventional seven-transmembrane receptor. The realization that RAMPs co-assemble with CRLR to form CGRP and related receptors forced a reconceptualization of peptide receptor activation and made clear that receptor complexes, not single proteins, could underlie pharmacological specificity. Serendipity Depends on Experimental Design and System Choice . The discovery of RAMPs was only possible because the assay tied receptor signaling to a highly amplified electrophysiological readout, revealing dramatic effects that might have been lost in noisier systems. Similarly, placental tissue became the source for CGRP receptor purification simply because binding studies showed it combined high receptor density with practical availability, illustrating how pragmatic choices in model systems can open unexpected paths in GPCR pharmacology. Deorphanizing Receptors Blends Bioinformatics and Bench Work . Dr. Foord describes a period where his group repeatedly identified ligands for orphan receptors: the second GABA B subunit via yeast two-hybrid, a carboxylic acid receptor when the solvent turned out to be the real agonist, and a nicotinic acid receptor by intersecting tissue expression data with orphan GPCRs. These stories show how careful pharmacology, informed sequence analysis, and attention to apparent artifacts can reveal new receptor signaling pathways relevant for metabolism and cardiovascular disease. Target Validation Is Harder Than Cloning a Receptor . From the non-existent second AT1 angiotensin receptor to the MAS oncogene as a poor angiotensin responder, Dr. Foord emphasizes how easy it is to be misled by overexpressed systems and noisy orphan receptor data. Southern blotting, cross-hybridization, and later genetic analyses ultimately showed that some hypothesized subtypes were artifacts, underscoring that robust target validation is a distinct and often more challenging problem than receptor cloning or initial ligand binding assays. Drug Discovery Is Constrained by Selectivity, Safety, and Strategy . The CGRP story illustrates how structural biology and pharmacology intersect with corporate decisions: once it became clear that the CRLR binding pocket is shared across CGRP, amylin, and adrenomedullin receptors, small-molecule selectivity looked problematic. Later hepatotoxicity concerns and the success of antibody therapeutics further shifted strategy. Similar strategic considerations shaped the fate of the EP4 partial agonist that ultimately found a niche in veterinary medicine rather than human rheumatoid arthritis. Genetics and Informatics Offer Power but Not Simple Answers . As Head of Bioinformatics for Neuroscience, Dr. Foord participated in GSK’s early large-scale association genetics effort, feeding GPCRs, ion channels, and transporters into case–control studies. Apart from APOE4 in Alzheimer’s disease, most signals failed to reach robustness with available cohort sizes, tempering expectations that genetics alone would deliver pipelines of GPCR targets. He argues that integrating structural biology, computational pharmacology, and genetics may still be key to understanding receptor activation in patients, but requires realistic views of effect sizes and trial design. Scientific Careers Depend on Teams, Mentors, and Community . Reflecting on his path from physiology to molecular pharmacology to bioinformatics, Dr. Foord highlights how good mentors, diverse teams, and open sharing of reagents and ideas enabled progress. He stresses the value of lab “optimists and cynics,” the importance of talking about negative results, and the role of informal networks in preventing wasted effort. For younger scientists, his advice centers on doing work you genuinely enjoy, finding supervisors who connect you to the broader GPCR community, and being willing to pivot as new methods and questions emerge. Episode Timeline 00:00 — Early academic work in neuroendocrinology, self-experimentation with TRH and somatostatin, and first encounters with hormones and GPCRs. 02:00 — Move to Roger Craig’s lab, purification of the CGRP receptor from human placenta, and practical considerations in choosing receptor-rich tissues. 05:00 — Transition from academia to Glaxo, early HIV TAT work in Xenopus oocytes, and the emergence of molecular pharmacology within a pharmacology-led organization. 10:30 — Expression cloning of the CGRP system, discovery of RAMP1, and how oocyte electrophysiology revealed a massive potentiation of endogenous CRLR signaling. 18:00 — Industrial migraine programs, small-molecule CGRP antagonists, challenges with selectivity and liver toxicity, and the later success of CGRP antibodies. 20:00 — Angiotensin receptor work, using Southern blots to hunt for a non-existent AT1 subtype, and the MAS oncogene as a cautionary tale in receptor signaling artifacts. 30:00 — Discovery of the prostaglandin EP4 receptor while searching for angiotensin-related sequences, development of an EP4 partial agonist, and its path into veterinary medicine. 34:00 — GABA B receptor complex, identification of the second subunit via yeast two-hybrid, and closing the chapter on proposed additional GABA B subtypes. 39:00 — Large-scale genetics and bioinformatics at GSK, expectations for GPCR target discovery from association studies, and reflections on why many signals remained elusive. 52:00 — Career advice on doing work you enjoy, the importance of mentors and connectedness, and how team composition and negative data shape GPCR research and drug discovery. Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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. Stuart Maudsley About Dr. Stuart Maudsley Stuart graduated from the University of Leeds in the U.K. with a First Class Honors degree in Pharmacology. At the end of his studies, he was awarded the Pfizer Prize for undergraduate research. He then completed his Ph.D. at Leeds as well as the University’s Ackroyd, Brotherton, and Brown Scholar. Following his Ph.D., Dr. Maudsley was awarded a Howard Hughes Medical Institute Fellowship to train with Professor Robert Lefkowitz at Duke University. Following this tremendous experience, he was recruited to be the Principal Investigator of the Receptor Biology Section at the Medical Research Council (MRC) -Human Reproductive Sciences Unit within the University of Edinburgh. At the MRC he developed novel prostate cancer therapeutics based upon his research into GPCR pluridimensional signaling. To broaden his biomedical skill-set Stuart next accepted the position of Head of the Receptor Pharmacology Unit at the National Institutes of Health – National Institute on Aging at the Johns Hopkins University Medical Center. At the NIH he was the recipient of the coveted NIH ‘Bench-to-Bedside’ Translational Research Grant Award, one of the few awards available within the intramural NIH program. Upon starting a new family, and returning to Europe, Dr. Maudsley continued his scientific journey with the award of the highly-valued Odysseus Program Type I Program Grant to work as both the Adjunct Director of the VIB Center for Molecular Neurology and also Vice-Chair of the Department of Biomedical Sciences at the University of Antwerp. Stuart’s current research, in the Receptor Biology Lab, focuses on the development of novel GPCR-based therapeutics that interdict diseases based on their gerontological underpinnings. This research stream is now forming the basis of a new technology-based start-up company, HeptOME , to help screen and develop novel longevity/disease-regulating compounds with multidimensional disease efficacy profiles. Dr. Stuart Maudsley on the web Maudsley Lab LinkedIn Google Scholar ResearchGate Maudsley Lab on Facebook Receptor Biology Lab Facebook Group Twitter Semantic Scholar Instagram Neurotree Dimensions Reddit Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Your One-Stop-Shop for GPCR Drug Discovery and Development Researchers developing GPCR-targeted therapeutics need a reliable, comprehensive partner that spans discovery, optimization, and regulatory submission. Eurofins DiscoverX leads GPCR research innovation with 25+ years of expertise and provides you with product solutions including cell-based assays for basic research through therapeutic discovery and development. The assays are validated and accepted by industry and the scientific community, with thousands of peer-reviewed publications and billions of data points screened. These industry-standard assays, designed for regulatory submissions, are backed by partnerships with leading pharma and biotech companies worldwide. GPCR Product Solutions Determine rank-order hits, evaluate ligand bias or allostery, study multiple targets and signaling pathways, investigate target species variations, deorphanize receptors, and more Perform target identification and validation, high-throughput screening (HTS), lead optimization, safety assessment, and regulatory potency testing for commercial release Access a complete toolkit for GPCR solutions: cell line assay kits, cell lines, ready-to-use assays, detection kits, custom products, and more Comprehensive Coverage >1500 Human GPCRs products, including: 90% Target coverage Orphan receptors Ortholog variants Multiple cell line backgrounds Multiple Mechanisms of Actions (MOA) cAMP accumulation β-Arrestin recruitment Receptor internalization Ligand binding Calcium flux Pharmaco Chaperone discovery Numerous Product Types Cell line assay kits Cell lines Qualified bioassays eXpress assay kits Membrane preps Detection kits Custom products Services Flexible Formats for Every Research Need Eurofins DiscoverX understands that different research stages require different tools. This comprehensive portfolio offers multiple product formats to match your exact needs, whether you're conducting exploratory screens or regulatory-compliant potency testing. Assay Principle of Eurofins DiscoverX Cell-based Assays Whether you are developing small-molecule or biologic therapeutic drugs, Eurofins DiscoverX provides you with a variety of drug discovery and development products with multiple assay types and applications to meet your specific GPCR research needs. Access Product Solutions and Key Resources GPCR Functional Cell-Based Assays - Assessing Biased Signaling of Agonist Access White Paper Discover Your GPCR Solution - Find The Assay for Your Target of Interest Find Your Solutions The Human GPCRome - Obtain Your FREE Wall Poster for Your Laboratory Obtain Wall Poster Access GPCR Cell Line Assays, Ready-to-Use Kits, Mem Preps, & More Shop Products Supporting GPCR-focused Obesity and Diabetes Research Eurofins DiscoverX supports the ongoing obesity/diabetes revolution with the most comprehensive, validated portfolio for obesity and diabetes GPCR targets, including GLP-1, GIP, GCG, MC4, PYY, AMY receptors, and more. Browse products related to your obesity/diabetes target of interest: CALCRL and RAMP (AMs) GIPR GLP-1R GLP-2R GCGR GPR75 MC4R NPY2R (PYY) SSTR5 Activins CALCR and RAMPs (AMYs) Apelin (APJ/AGTRL1) View representative data: GLP-1R multi-MOA profiling Eurofins DiscoverX's GLP-1 receptor (GLP-1R) assay portfolio illustrates a comprehensive approach to obesity research, with complete MOA coverage for a single target: GLP-1. These assays enable complete pharmacological profiling across cAMP, β-arrestin, and internalization. GLP-1R representative assay results (dose-response curves) for exendin-4, tirzepatide, and retatrutide. A. cAMP dose–response; B. β-arrestin recruitment showing ligand bias; and C. Internalization profiles distinguishing highly versus weakly internalizing agonists. Together, these datasets exemplify the depth of pharmacological insight enabled by Eurofins DiscoverX platforms. This multi-dimensional characterization extends across our full obesity and diabetes product portfolio, including GIPR, GCGR, AMY receptors, MC4R, and beyond. Access GPCR Obesity and Diabetes Solutions and Key Resources Discover GPCR Obesity and Diabetes Product Solutions Find Your Solution Review GIP Product Solutions to Support Obesity/Diabetes View GIP Solutions Explore GLP-1 Product Solutions to Support Obesity/Diabetes See GLP-1 Solutions Accelerating Obesity Therapeutics Development Download App Note Beyond Eurofins DiscoverX Products: The Full Power of Eurofins Discovery Eurofins DiscoverX cell lines, assays, kits, and custom product solutions represent the foundation of tools for GPCR research and drug discovery and development. When these product solutions are combined with Calixar GPCR membrane proteins and Eurofins Discovery GPCR services, the benefits from integration provide the most comprehensive GPCR research and drug discovery platform spanning the entire discovery and development continuum. Eurofins Discovery GPCR services provides the industry's most extensive collection of validated GPCR assays with hundreds of binding and functional assays, available individually or in panels. These assays use the same platform as the Eurofins DiscoverX assays and beyond. Calixar GPCR membrane proteins , as a service, provides a wide array of GPCRs from various species, purified to the highest standards to ensure purity, integrity, and biological activity. These GPCRs are excellent for use in functional, structural, or identification assays. Let us Help You Get Started! Contact us Visit GPCR Product Solutions

<< Back to podcast list Strategic Partner(s) Dr. Shivani Sachdev 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 Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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. JoAnn Trejo About Dr. JoAnn Trejo Dr. JoAnn Trejo earned her Ph.D. at UC San Diego. She completed her postdoctoral fellowship at UC San Francisco under the guidance of Professor Shaun Coughlin where she worked on the newly discovered protease-activated GPCRs. Dr. Trejo joined the faculty in the Department of Pharmacology at the University of North Carolina in 2000 and then moved to UC San Diego School Medicine, Department of Pharmacology in 2008, where she quickly rose through the ranks to tenured professor in 2012. In 2014, she was appointed Vice-Chair of the Department of Pharmacology. The long-term goal of Dr. Trejo’s research program is to gain a thorough and mechanistic understanding of processes that control cell signaling by protease-activated receptors (PARs) and the impact on vascular inflammation and cancer progression. PARs are GPCRs that are activated through an atypical irreversible proteolytic mechanism. The precise control of PAR signaling is critical for proper temporal and spatial dynamics of signaling and appropriate cellular responses. Discovering new aspects of PAR signaling is important for increasing the fundamental knowledge of GPCR biology and for the identification of drug targets and future drug development. Dr. Trejo’s research has focused on PAR1, which has important functions in hemostasis, thrombosis, inflammation, and cancer and is an important drug target. She has made numerous important discoveries related to the mechanisms that control PAR1 signaling and closely related family members and published extensively on this topic. Dr. Trejo has been continuously funded by the NIH for >20 years and was a recipient of the prestigious American Heart Association Established Investigator Award. Her laboratory is the recognized expert on protease-activated receptors, particularly PAR1, and over the years she has discovered novel aspects of GPCR biology, acquired critical expertise, and rigorous approaches to examine PAR1 function using human cultured cells and mouse models. Dr. Trejo has presented her studies at 52 national/international meetings and 66 academic seminars across the U.S. Dr. JoAnn Trejo on the web UC San Diego Trejo Lab Wikipedia LinkedIn Google Scholar Orcid Twitter UC San Diego School of Medicine Researchgate Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Join the Dr. GPCR Podcast community and shape our next season! Take our quick 5-minute audience survey to help us tailor our content to your needs. Your input matters in delivering exciting and informative episodes. Thank you for being part of our journey and for tuning in! Dr. GPCR Podcast Audience Survey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player Be our Guest Listen and subscribe where you get your podcasts

Antony Boucard - the scientist who discovered that a cell adhesion molecule and a GPCR share a black widow spider toxin binding site — on adhesion GPCRs, synapse formation, and building a research program where none existed before. << Back to podcast list Strategic Partner(s) Antony Boucard: Adhesion GPCRs and the Molecular Code of Synapse Formation Adhesion GPCRs represent one of the most architecturally complex and least understood branches of the GPCR superfamily. Characterized by extracellular domains exceeding 1,000 amino acids, autoproteolytic cleavage at the membrane, and a near-total absence of characterized ligands, these receptors long resisted the molecular tools that made classical family A GPCRs tractable. Only recently has the field established, with confidence, that adhesion GPCRs couple to G proteins at all. Boucard's laboratory at UNAM in Mexico City sits at this frontier. His research centers on the molecular code governing synapse formation — how adhesion GPCRs, working alongside classical cell adhesion molecules, determine which neuronal partners recognize each other and which synaptic contacts stabilize. The work connects receptor biology to neuropsychiatric disease: addiction, autism spectrum disorder, schizophrenia, bipolar disorder, and cancer. The foundation of this program rests on a serendipitous discovery Boucard made in Thomas Südhof's lab — that a cell adhesion molecule and a GPCR, studied separately for over a decade, both bind alpha-latrotoxin from black widow spider venom, and that together they form an intercellular complex no one had previously described. For Boucard, adhesion GPCRs are not simply a research subject. They are the place where everything he has cared about — biochemistry, cell communication, disease, and the students other institutions overlooked — finally came together. About the Guest Antony Boucard is a biochemist and cell biologist who leads the Boucard Laboratory at the National Autonomous University of Mexico (UNAM) in Mexico City, where he has built one of the only research programs in Latin America focused on adhesion GPCRs. He completed graduate training in biochemistry at the Université de Sherbrooke and his postdoctoral fellowship in the laboratory of Thomas Südhof at UT Southwestern and Stanford University, where he made the initial observation linking cell adhesion molecules and GPCRs through their shared binding to alpha-latrotoxin. His current research programs span synapse formation, addiction, autism, schizophrenia, bipolar disorder, and tumorigenesis, applying cell biology, BRET and FRET assays, microscopy, flow cytometry, and custom protein engineering approaches to probe adhesion GPCR function across physiological and pathological contexts. Scientific Themes of the Conversation Adhesion GPCRs as a distinct receptor class — autoproteolytic architecture, orphan status, and the long-delayed confirmation of G protein coupling The molecular logic of synapse formation and how adhesion molecules encode synaptic specificity in the brain Alpha-latrotoxin from black widow spider venom as an experimental bridge connecting cell adhesion molecules and GPCRs Neuropsychiatric disease through the lens of adhesion GPCR biology — addiction, autism spectrum disorder, schizophrenia, and cancer The structural bottleneck: what cryo-EM cannot yet capture about receptor dynamics at the cell surface Pioneering a research field in an underrepresented scientific ecosystem, and recruiting from communities elite institutions have historically overlooked Key Insights from the Conversation 1. Adhesion GPCRs Were Not Considered Real GPCRs For decades, adhesion GPCRs were assigned to the GPCR superfamily on the basis of their seven-transmembrane topology alone — not because G protein coupling had been demonstrated. Whether they functionally coupled to G proteins remained genuinely open, and for much of the field's history, skepticism was reasonable. Boucard's work on their signaling capacity in the context of synaptic biology sits at this still-resolving frontier, where the biology is catching up to the structural classification. 2. A Forgotten Sample, a First Paper During his graduate studies, Boucard left an enzymatic reaction on his bench over a weekend — called away for army training — and returned to find results that had eluded the lab for months. He nearly discarded the sample. Running it on instinct, he obtained reproducible data that became his first publication. The pattern established there — outcomes shaped as much by openness as by design — has followed him through every phase of his career since. 3. The Black Widow Toxin Nobody Put Together Working in Südhof's lab on cell adhesion molecules, Boucard made a lateral decision: to test whether one of the proteins he was studying might bind to a GPCR he had no reason to investigate. The interaction was real. On a colleague's suggestion, he recognized that both proteins had independently been shown to bind alpha-latrotoxin from black widow spider venom — but no one had ever asked whether they interacted with each other. They formed an intercellular adhesion complex. Südhof himself was skeptical; the field had studied both proteins for over a decade without making the connection. That discovery became the foundation of Boucard's independent research program. 4. Adhesion GPCRs Open a Pandora's Box Adhesion GPCRs appear across nearly every biological process — from embryonic development to synaptic maturation, from immune cell trafficking to tumorigenesis. Boucard describes this breadth not as an opportunity but as a constraint: the challenge for his lab has been choosing which processes to study rigorously rather than chasing the full landscape. Anchoring the work in synapse formation provides a tractable and biologically meaningful lens, while the transversal logic — that what is learned about adhesion in one context often illuminates another — keeps the research portfolio coherent. 5. The Structural Bottleneck Cryo-EM has transformed understanding of classical GPCR structure, but adhesion GPCRs remain dramatically underrepresented in the structural database. The deeper issue, Boucard argues, is not just the quantity of structures but their nature: every cryo-EM image is a frozen moment, capturing a receptor in one state, in one membrane environment, at one point in time. What the field still cannot do is observe the dynamics of receptor assembly, complex formation, and signaling in real time at the cell surface. That gap is where the most important biology is happening. 6. Choosing Mexico City as a Scientific Bet After postdoctoral and faculty positions at Stanford and UT Southwestern, Boucard surveyed the conventional research markets — North America, Western Europe — and concluded that his skills were not especially scarce there. Mexico City offered something different: a research territory in adhesion GPCR biology that was entirely unoccupied, a massive university drawing students from across Latin America and indigenous communities within Mexico, and a scientific culture where his particular combination of biochemistry, cell biology, and translational thinking could do something that wasn't already being done. Eight years in, he has not reconsidered the decision. Episode Timeline Timestamps were generated with AI assistance from the episode transcript and may not reflect exact segment boundaries. Use them as navigational guides. 00:00 Sponsor intro — GeneTex & Eurofins DiscoverX 00:43 Introducing Boucard: a scientific path that was never planned 01:40 From biochemistry by accident: Sherbrooke, Dallas, Stanford, Mexico City 03:43 The summer lab that changed everything — and why he turned down medical school 10:23 Army service, social work in Nicaragua, and the civil war that reframed resources and risk 16:18 Turning down the medical school acceptance — 25 years of no regrets 22:10 Université de Sherbrooke's industry-integrated curriculum and what it modeled about flexibility 26:06 Surviving crisis in Haiti and what scarcity teaches about choice 31:33 The underground restaurant in San Francisco, born out of an immigration emergency — and Chef's Table Season 2 43:45 Time, focus, and the discipline of 15 minutes a day 52:38 Why Mexico City: building a lab for students no one else was recruiting 01:00:00 Adhesion GPCRs — the receptor family that kept calling him back 01:04:58 The black widow toxin discovery — two proteins, 15 years of prior research, one untested pair 01:06:18 Why adhesion GPCRs are among the hardest receptors to work with, and why structures are finally coming 01:09:10 Synapse formation, addiction, autism, schizophrenia, and cancer: the lab's research logic 01:13:45 Assays: BRET, FRET, microscopy, flow cytometry, and engineering membrane-anchored ligands into solution 01:19:29 The dream tool — a nanoscale camera navigating the cell surface in real time 01:22:24 Advice to junior scientists: don't be afraid to be afraid 01:26:00 Three aha moments: socks, a forgotten sample, and one cold email to a Nobel laureate 01:35:33 Lab openings and where to find the Boucard Lab Selected Quotes "Every single one of my days right now has been just to reconstruct what I learned the day before. That's something that I really love — you kind of put yourself in the mindset of the kid once again." "A lot of people say there's a lot of reasons not to do an experiment. There's a ton. But sometimes you can just do one. And you never know." "I can't believe you won the Nobel Prize. Because at home, he can't even pick up his own socks." — Said to Boucard by a fellow Nobel laureate's wife, at a ceremony at Stanford, following the 2013 prize announcement "If you willingly put yourself in a situation where you're willing to take risks, things will fall into place. But if you never try, you might not know. And whether you're there for a short time or for the rest of your life, you'll have the best time of your life during the time you're doing it." About Dr. Antony A. Boucard Jr. Dr. Antony Boucard joined the Université de Sherbrooke (Québec, Canada) as a B.S. student of the Biochemistry program in 1994 from which he graduated in 1997. It is then that his interest bloomed for the study of GPCRs while joining the group of Dr. Richard Leduc and Dr. Gaetan Guillemette in the Pharmacology department at the Université de Sherbrooke. He completed a master’s degree in 2000 and a Ph.D. degree in 2003 with a particular interest in the cardiovascular system by investigating the structure of the Angiotensin and Urotensin receptors through various biochemical approaches centered in the elucidation of ligand binding pocket determinants. Motivated by a new ambition to study the nervous system, Dr. Boucard pursued postdoctoral training at the University of Texas Southwestern Medical Center in Dallas where he joined the group of Dr. Thomas Südhof . In this institution dear to the heart of GPCR enthusiasts given that its faculty personnel included Dr. Alfred Gilman , Nobel Laureate for his discovery of G proteins, Dr. Boucard ventured into the field of synaptic adhesion molecules which would eventually prompt him to investigate the role of a peculiar family of GPCRs belonging to the Adhesion subgroup. After a relocation to Stanford University where he pioneered work on ligand discovery for then orphan adhesion GPCRs, Dr. Boucard moved to Mexico City to establish himself as an independent investigator integrating the department of Cell Biology at the Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN). Dr. Boucard´s lab focuses on molecular and cellular mechanisms underlying the function of adhesion GPCRs in the formation of synapses. Having a particular interest for a three-member family named latrophilins, his lab seeks to decipher the molecular code instructing adhesion events mediated by these GPCRs. The pharmacology of latrophilins brings about a great deal of challenges given that they are highly polymorphic proteins expressed as various alternatively spliced isoforms thus potentially resulting in differential modulation of cell signaling pathways. His lab highlighted the importance of splicing events in biasing latrophilins’ regulation of cyclic AMP pathways and for determining the magnitude of ligand selectivity. Additionally, his team is also interested in understanding the pathophysiological relevance of latrophilins’ function in neuropsychiatric disorders given their association with genetic susceptibility to the neurodevelopmental disorder known as attention deficit hyperactivity disorder (ADHD) but also to a comorbid clinical manifestation linked to addiction. He also actively volunteers as an Associate Professor of the non-governmental organization Institut des Sciences, des Technologies et des Etudes Avancées d’Haïti (ISTEAH) to help consolidate higher education in Haiti. Dr. Antony A. Boucard Jr. on the web Website LinkedIn Researchgate Loop Academia Pubmed Adhesion GPCR Consortium University of Haiti Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Get in touch with Dr. GPCR Ecosystem today! Find our contact information and reach out to us for any inquiries or collaborations. Let's connect! Contact Do you need help with the Dr. GPCR Ecosystem or want to collaborate? Let's Connect! Address 14 Summer St. Malden, MA 02148 Email Hello@DrGPCR.com Phone 646-508-3568 Social Media First Name Last Name Email Message Send Thanks for submitting!

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 Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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) Mark Schmeizl About Mark Schmeizl Mark leverages 30 years in various life science laboratories & commercial roles with his network of VC & PE contacts to help senior-level life science executives identify new opportunities. He has successfully built numerous global life science, leadership teams, & works closely with both clients & candidates to understand their unique needs & culture. Mark believes professional placement should be about matching talented people with companies where they will thrive, “when the match is right, the results are astonishing.” Dr. Mark Schmeizl on the web Website LinkedIn Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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) Chris Langmead Chris Langmead is Professor, Deputy Director, and Better Medicines Theme Leader of the Neuromedicines Discovery Centre at the Monash Institute of Pharmaceutical Sciences (MIPS), a collaborative venture targeting new medicines development for poorly-treated mental health disorders. He also directs a collaborative neuroscience R&D program with Servier (France) and is the co-founder and CEO of Phrenix Therapeutics, a biotech spin-out from the Neuromedicines Discovery Centre that is developing next-generation therapeutics for schizophrenia. Prior to these roles this he was Head of Pharmacology at Heptares Therapeutics Ltd., a UK-based biotechnology company (2009-2012), where he was responsible all of the company’s discovery biology. He is an acknowledged expert in drug discovery, particularly in the field of psychiatry, where he has led multiple projects into late stage preclinical development, many of which have progressed into clinical trials. These successes enabled the US$400M sale of Heptares Therapeutics Ltd. to the Sosei Group Corporation in 2015. Prior to joining Heptares, Chris was a neuroscience researcher at GlaxoSmithKline, UK (1998-2009). He has a degree and PhD in pharmacology from Queens' College, Cambridge and University College London, respectively, was the youngest person to be elected as a Fellow of the British Pharmacological Society in 2012, and was the recipient of the British Pharmacological Society Novartis Prize in 2017. Chris serves on the editorial boards of the British Journal of Pharmacology, ACS Chemical Neuroscience, ACS Pharmacology & Translational Science and Frontiers in Pharmacology. He is also a corresponding member of NC-IUPHAR. He has published over 70 research articles, reviews and book chapters on drug discovery, which have been cited over 5000 times. Christopher Langmead on the web Monash University T witter Google Scholar Linkedin PubMed Monash Neuromedicines Dr. GPCR Ecosystem Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Share your thoughts and help shape the future of the Dr. GPCR Ecosystem. Your feedback guides improvements, new features, and community resources. Dr. GPCR Community Survey Help us build the next evolution of the GPCR Ecosystem — together. Every opinion counts. Whether you’ve joined our University sessions, explored our Job Board, or attended a Happy Hour, your feedback shapes what comes next. Let’s make Dr. GPCR more useful, connected, and inspiring for everyone in the field. 👉 Take the Survey Now Why Your Feedback Matters? We’re growing — and your input helps us grow in the right direction. By sharing your thoughts, you directly influence how we design new features, events, and educational programs. Your responses help us: Improve the Dr. GPCR University curriculum and resources. Make Retreats and Happy Hours more valuable and accessible. Build stronger connections between academia and industry. Develop new tools, training programs, and mentorship programs tailored to your specific needs. Your Voice Shapes Our Future Dr. GPCR was founded to bring the GPCR community together — and every survey response helps us strengthen that mission. This isn’t just a form — it’s how you influence the next generation of education, collaboration, and discovery. 💡 Start the Survey What We’d Love to Learn? We’ve grouped the questions into three sections so your feedback can make a real impact: 1. Your Experience How often do you use the Dr. GPCR platform? Which programs do you engage with most? (University, Retreat, Job Board, Newsletter, etc.) What has been your favorite experience so far? 2. Your Needs What topics or training modules would you like us to add next? What challenges do you face most in your research or biotech journey? How can we facilitate easier collaboration within the community? 3. Your Feedback How likely are you to recommend Dr. GPCR to a colleague? (1–10) What would make your experience even better? Any ideas, suggestions, or features you’d love to see in 2026? Survey 🙏 Thank You for Being Part of the Ecosystem Your feedback helps us: Keep events free or affordable Expand our shared knowledge base Support students and researchers entering the field Together, we’re building a home for everyone passionate about GPCR research and innovation.

<< Back to podcast list Strategic Partner(s) Dr. Aurélien Rizk About Dr. Aurélien Rizk "Dr. Aurélien Rizk is a scientist and entrepreneur in drug discovery. He is Chief Scientific Officer and co-founder of InterAx Biotech, where he specializes in the development of a technology platform deciphering cell signaling pathways combined with AI-based approaches to elucidate structure to signaling relationship. During four years of postdoctoral research at ETH Zurich and the Paul Scherrer Institute in Switzerland, under the guidance of Prof. Gebhard Schertler, he developed methods for kinetic mathematical analysis of GPCR signaling. He also worked on creating novel methods for systems biology using temporal logic specifications while pursuing his Ph.D. at INRIA Paris-Rocquencourt, France. Before focusing on the development of innovative mathematical modeling and simulation methods for drug discovery, Dr. Aurélien Rizk co-founded Algorizk, a company that created real-time physics simulations for education, serving over 1 million users. His academic background includes studies in mathematics, physics, and computer science at the French Grande École, École Normale Supérieure de Cachan." Dr. Aurélien Rizk on the web InterAx Biotech Paul Scherrer Institut The Org LinkedIn Google Scholar Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick recap Yamina Berchiche and Aurelien Rizk engaged in a conversation about their professional backgrounds and current projects. They explored the potential of merging mathematical models with biology, the complexities of GPCRs within cells, and the applicability of technology to other fields. They also discussed the founding of a company focused on GPCRs, the transition from academia to the biotech sector, the evolution of a company that started with the development of technologies combining mathematical methods and a wet lab, and the importance of interdisciplinary teamwork in drug and technology development. They emphasized the significance of mathematical models in systems biology and pharmacology and the challenges of transferring information between different families of GPCRs. They wrapped up the conversation by discussing job opportunities at Interax Biotech and their anticipation for future interactions. Summary Professional Backgrounds and Projects Discussed Yamina Berchiche and Aurelien Rizk had a conversation about their professional backgrounds and current projects. Aurelien Rizk, a co-founder and CEO of Interax Biotech, shared about the company's development of a discovery platform for GPCRs and their focus on signaling pathways. He also talked about his past experiences in mathematics, physics, and computer sciences, and his involvement in developing mathematical models for various systems. The discussion concluded without any clear decisions, action items, or open questions. Integrating Mathematical Models and Biology: A Fascinating Discussion Yamina and Aurelien Rizk had a conversation about the importance of merging mathematical models and biology. They highlighted that while there was a time when biology lagged due to the lack of appropriate tools, it is now progressing faster. They found it fascinating to integrate both fields and the potential it holds. Aurelien Rizk mentioned the importance of being able to test and adjust predictions in real-life scenarios. They also touched upon the transferability of this approach across different systems, which Yamina found attractive. GPCRs, Software, and Fluid Dynamics Yamina Berchiche and Aurelien Rizk discussed the complexities of GPCRs within cells and the potential for applying models from one system to another. Yamina also questioned Aurelien Rizk about his interest in software, computer science, and mathematics. Aurelien Rizk shared his journey of using these disciplines in biology and how his company, Interax, came to be. The discussion ended with Aurelien Rizk sharing his current work on numerical simulations of fluid dynamics. GPCRs: A Focus for New Company Aurelien Rizk and Yamina Berchiche discussed the founding of a company focused on GPCRs and the potential applicability of the technology to other fields. Aurelien Rizk shared that he had always focused on GPCRs but had also worked on other types of receptors, indicating that the technology could be applied broadly. Yamina asked if there was ever a consideration to work on targets other than GPCRs, to which Aurelien Rizk explained that they chose GPCRs due to their wide application and potential impact. The conversation concluded with Yamina asking if Aurelien Rizk had a favorite GPCR to work on, though his response was not included in the transcript. Cell Signaling and Cancer Metastasis Discussion Aurelien Rizk and Yamina Berchiche had a detailed conversation about the intricacies of cell signaling and chemokine receptors. Yamina shared her research experience, emphasizing the fascination of understanding how cells respond to gradients and signals, particularly in relation to cancer metastasis. Aurelien Rizk also contributed to the conversation, highlighting the complexity of the process. However, the transcript is somewhat unclear and disjointed, making it difficult to summarize the specific points discussed. Academia to Biotech: Strategic Planning and Interdisciplinary Approach Yamina Berchiche and Aurelien Rizk discussed the differences between academia and the biotech industry, with Aurelien Rizk sharing his experiences transitioning from academia into the biotech sector. They highlighted the strategic importance of planning in the biotech sector due to limited funds and the need to show positive results when securing new investments. Aurelien Rizk also mentioned the interdisciplinary nature of his company, which includes mathematics, signaling pathways, a wet lab for data generation, and AI and computational chemistry. The discussion also touched on recent changes in leadership at Aurelien Rizk's company, with the introduction of a new CEO a year ago and the valuable contributions of Mark Levick, a former reviewer for the European Medicines Agency and CEO of a biotech company. Technology Evolution and Ligand Residence Time Prediction Yamina Berchiche and Aurelien Rizk discussed the evolution of the company, which started with the development of technologies combining mathematical methods and a wet lab to ensure the technology functioned. They validated their technology and made collaborations for expertise on chemokine receptors. The conversation also revolved around the company's ability to predict the residence time of a ligand and its potential correlation with a therapeutic effect or activation of a specific signaling pathway. The discussion concluded with the idea that ligand residence time could be an important factor in effective therapy. Therapeutic Effect and Receptor Interactions Aurelien Rizk and Yamina had a detailed discussion about the importance of gaining more information about the therapeutic effect in patients or animals and the dynamics of receptor interactions. They emphasized the need to quantify the dynamics of the pathways and the residence time of the receptor. Yamina raised a question about the transferability of information between different families of GPCRs and the possibility of generating a mathematical model for potential patterns. They also discussed the challenges of system dependency in data and the need to express data in a uniform way to apply models. Mathematical Models in Systems Biology and Pharmacology Aurelien Rizk and Yamina discussed the importance and relevance of mathematical models in systems biology and pharmacology. They reminisced about previous meetings and events, including a GPCR retreat where Terry presented his work. Yamina mentioned her struggle with the mathematical aspects of Terry's papers but acknowledged their importance in quantifying and removing system biases. They also discussed plans to offer a course with Terry, due to high interest. Towards the end, Aurelien Rizk shared his top three 'aha' moments as a scientist, emphasizing the importance of learning and controlling systems. Interdisciplinary Teamwork and Drug Development Yamina Berchiche and Aurelien Rizk emphasized the significance of interdisciplinary teamwork in drug and technology development, noting the challenges of communication and collaboration across different fields. They also shared their preference for small molecule therapies over protein therapeutics. Aurelien Rizk confirmed his attendance at the upcoming GPCR-Targeted Drug Discovery Summit in Boston. The discussion concluded with a brief overview of job opportunities at Interax Biotech, with Aurelien Rizk and Yamina clarifying that job openings are communicated via email and through their job board. They expressed their anticipation for future interactions. Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

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 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

<< Back to podcast list Strategic Partner(s) Re-cap of Endocrine Metabolic GPCR 2024 with the Organizers About Dr. Aylin Hanyaloglu Dr. Aylin Hanyaloglu has been a Principal Investigator at Imperial College London since 2007. She received her BSc in Human Biology from King’s College London in 1997, and while her Ph.D. commenced at the MRC Human Reproductive Sciences Centre, Edinburgh, a move to Perth, Australia resulted in her Ph.D. in Molecular Endocrinology being awarded in 2002 with Distinction from the University of Western Australia. Dr. Hanyaloglu undertook her postdoctoral training at the University of California, San Francisco with Professor Mark von Zastrow where she identified novel core cellular machinery critical for G protein-coupled receptor trafficking and signaling. Her research focuses on understanding the fundamental cell biological mechanisms regulating GPCR activity, including spatial control of GPCR signaling and receptor crosstalk, and applying these mechanisms for distinct GPCRs in diverse physiological and pathophysiological systems, with particular focus on women's health, pregnancy, and nutrient sensing in the gut. Her work is currently funded by Biotechnology and Biological Sciences Research Council (BBSRC), Diabetes UK, Wellcome Trust, and the Medical Research Council. Dr. Aylin Hanyaloglu on the web LinkedIn Endocrine Metabolic GPCRs Researchgate Twitter Imperial College London Elsevier Loop Dr. GPCR About Dr. Caroline Gorvin "Dr. Caroline Gorvin is a Wellcome Trust & Royal Society Sir Henry Dale Fellow at the Institute of Metabolism and Systems Research, University of Birmingham. She obtained her PhD in 2012 from the University of Oxford, where her research focused on the cellular mechanisms by which mutations in a chloride-proton antiporter cause the renal disorder Dent’s disease. Caroline continued to undertake postdoctoral research in Oxford, investigating the signalling and trafficking of the G protein-coupled receptor (GPCR), calcium-sensing receptor, and its role in calcium homeostasis. Caroline moved to the University of Birmingham in 2018 to establish her research group investigating metabolic GPCRs. Her current research focuses on how metabolic GPCRs cross-talk and interact to regulate appetite and bone metabolism." Dr. Caroline Gorvin on the web University of Birmingham Endocrine Metabolic GPCRs Society of Endocrinology Google Scholar ResearchGate Loop Twitter Dr. GPCR About Dr. Alejandra Tomas "Dr. Alejandra Tomas is a molecular cell biologist and Senior Lecturer at the Department of Metabolism, Digestion and Reproduction, Imperial College London. She obtained a PhD in Biochemistry from University College London and spent several years in Switzerland working on the study of membrane trafficking processes in pancreatic beta cells before returning to the UK, first to her Department at UCL and then to lead a laboratory at Imperial following the receipt of an MRC New Investigator Award in 2015." Dr. Alejandra Tomas on the web Imperial College London Endocrine Metabolic GPCRs ResearchGate Google Scholar LinkedIn Twitter Dr. GPCR Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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) Annabelle Milner About Annabelle Milner Annabelle completed her undergraduate degree in Biomedical Sciences at the University of Bath. As part of the degree, she undertook a 1-year research-based placement at the Charles Perkins Centre in Sydney, investigating the effects of dietary carbohydrates on metabolic health with Dr. Jibran Wali. From here, she returned to the UK. She began her Ph.D. at Imperial College London with Prof Aylin Hanyaloglu, Prof Gary Frost, and Dr. Alastair Brown (Sosei Heptares), where she is currently a final year Ph.D. student. Annabelle’s Ph.D. work focuses on microbial-derived metabolites that signal through GPCRs expressed in the GI. In particular, she is looking at L- and D-lactate-activated HCAR1 signaling. She presented her Ph.D. work at the Society of Endocrinology Conference 2022 and was awarded the best oral poster prize. Outside the lab, she enjoys baking and swimming and has recently taken up paddle boarding. Annabelle Milner on the web Linkedin Researchgate Pubmed Dr. GPCR Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>

Browse past events hosted by the Dr. GPCR Ecosystem, featuring scientific meetings, workshops, and collaborations that brought the GPCR community together. Past Events - Where the Dr. GPCR community comes alive Welcome to the page where the heart of the Dr. GPCR community comes alive! Here, we celebrate the incredible moments that brought scientists, researchers, and GPCR enthusiasts together to share groundbreaking discoveries, spark new ideas, and forge lasting connections. From immersive workshops and high-energy summits to intimate retreats and virtual conferences, each event represents a milestone in our shared mission to advance GPCR science and collaboration worldwide. 👉 Dive into our event archive below to relive the energy, inspiration, and community spirit that make Dr. GPCR truly special. Be part of our journey — stay inspired by our collective passion for science, learning, and discovery. Adhesion GPCR Workshop 2024 Endocrine Metabolic GPCRs Meet Inoviem Team GPCR ECI Transatlantic 2022 Editorial: GPCR and G Protein-Mediated Signalling Events in the Nervous System Dr. GPCR Ecosystem 2.0: Collaborating better Dr. GPCR: Advancing GPCR Drug Discovery Through Collaboration Discovery On Target 2024 GPCR targeted drug discovery Summit 2024 GPCR targeted drug discovery Summit 2023 The Dr. GPCR Podcast GPCR targeted drug discovery Summit 2022 Dr. GPCR: Where all GPCRs are created equal Dr. GPCR: Beyond the lab GRS and GRC Switzerland GPCR Retreat 2023 Leadership is a learned skill - PhageMed Unige GPCR Retreat 2022 Dr. GPCR: Beyond the lab Dr. GPCR: From idea to Ecosystem Dr. GPCR: Beyond the lab

Discover how GPR65 reshapes our understanding of GPCR signaling and its role in cancer, with Dr. Ian Chronis on the Dr. GPCR podcast. << Back to podcast list Strategic Partner(s) Signals, pH, and Discovery : Cracking GPCR Mysteries with Dr. Ian Chronis In this episode, we welcome Dr. Ian Chronis, a recent Ph.D. graduate preparing to begin his postdoctoral work at the University of Michigan. Host Yamina Berchiche sets a welcoming tone as they dive into Ian’s unique academic journey—from early interests in medicine to his pivot toward pharmacology and GPCR research. His story offers valuable insights for anyone navigating the path from student to scientist. Ian discusses how his experiences at the University of Chicago and the University of Michigan shaped his scientific curiosity, particularly around G protein-coupled receptors (GPCRs) . His research centers on the beta-2 adrenergic receptor and GPR65 , a proton-sensing receptor with promising implications in cancer biology. He shares fascinating findings from his work on GPR65 , highlighting its unusual constitutive internalization and its ability to signal from acidic endosomes. This dual functionality—environmental sensing and compartment-specific signaling—offers a new layer of complexity in GPCR behavior. Yamina underscores the therapeutic potential of GPR65, especially in the context of cancer immunotherapy, and how understanding receptor activity in acidic micro environments could unlock new therapeutic strategies. Throughout the episode, Ian reflects on the value of a supportive lab culture , the need for better experimental tools in GPCR signaling , and the importance of engaging with the broader GPCR research community to drive innovation. The conversation wraps with a playful exchange about possible podcast titles, with Yamina suggesting "Ancient Greek Chemistry and GPCRs"—a nod to Ian’s heritage and the wide-ranging themes covered. This episode is both educational and inspiring, offering a behind-the-scenes look at a rising scientist’s journey in the ever-evolving world of GPCR research. About Ian Chronis I recently finished my PhD in the lab of Dr. Manoj Puthenveedu at the University of Michigan, where I am now working as a postdoc. My research has looked at the trafficking and signaling of adrenergic and proton-sensing receptors, with specific focus on identifying novel regulatory proteins governing their function. Ian Chronis on the web LinkedIn Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ 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 >>