Dr. John Streicher on how HSP90 flips direction between brain and spinal cord, why isoform-selective inhibitors may rescue oral delivery of opioid adjuncts, and how a student's side project on intermittent fasting erased morphine reward in mice. << Back to podcast list Strategic Partner(s) Dr. John Streicher: Reorganizing Opioid Signaling Beyond the Receptor The dominant strategy for improving opioid therapy has been to engineer new ligands at the receptor itself — biased agonists, partial agonists, multi-target molecules. Dr. John Streicher's laboratory at the University of Arizona works a different angle. His team treats opioid signaling as a problem of circuit organization: the same kinases and second messengers produce radically different outcomes depending on how they are scaffolded inside a cell, and the chaperones that do that scaffolding are themselves druggable. In this conversation, Dr. Streicher describes how heat shock protein 90 plays directly opposite roles in the brain and the spinal cord, why isoform-selective HSP90 inhibitors may finally solve the "brain always wins" problem of oral delivery, and how a graduate student's skeptically-received side project on intermittent fasting produced some of the strongest opioid-sparing data his lab has generated. He came to this field because a signaling cascade felt like a puzzle he could not stop thinking about, and the puzzle has only gotten more interesting. Listeners will get a concrete look at what it means to modulate opioid pharmacology downstream of the receptor — and why the safety margins the field has been chasing for decades might actually live there. About the Guest Dr. John Streicher is an assistant professor in the Department of Pharmacology at the University of Arizona. His lab combines cell and molecular biology with animal pharmacology to identify new signaling regulators of the mu, delta, and kappa opioid receptors. Current lines of work include isoform-selective HSP90 inhibition as a strategy for widening the opioid therapeutic index, signal organization downstream of opioid receptors, and the unexpected effects of intermittent fasting on morphine pharmacology. Dr. Streicher trained in signal transduction during his PhD on heart failure and p38 MAP kinase, and moved into opioid pharmacology as a postdoctoral fellow with Dr. Laura Bohn at Scripps Research Institute. Scientific Themes of the Conversation Opioid signaling specificity as a problem of circuit organization, not molecular identity HSP90 as a region-specific signaling scaffold — opposite roles in brain and spinal cord Isoform-selective chaperone inhibition as an alternative to receptor-level drug design The current state and replication troubles of biased agonism at the mu opioid receptor Downstream pharmacology as an underexplored route to safer opioid therapy Intermittent fasting as a metabolic modulator of opioid antinociception and reward Key Insights from the Conversation Specificity lives in circuit architecture, not in the kinase itself. ERK MAP kinase is Dr. Streicher's recurring example: the same molecule promotes opioid antinociception in one context, drives chronic pain in another, and functions as a mitogen in cancer. You cannot explain specificity by assuming each node does one thing. What differs is how scaffold proteins localize the kinase into distinct submolecular circuits. He teaches his students to think of kinases as components — a diode in a radio and a diode in a nuclear bomb can be identical — and the organization around them decides the outcome. HSP90 runs opposite programs in brain and spinal cord. In the brain, HSP90 promotes ERK activation downstream of the mu opioid receptor and is required for antinociception. In the spinal cord, the same chaperone acts as a brake on ERK activation. Block it spinally and the dorsal horn lights up with phospho-ERK in response to opioid, routing through RSK1/2 to stronger pain relief. Block it in the brain and antinociception collapses. This is not a quirk — it is the central clue the lab has built a therapeutic strategy around. The "brain always wins" problem is solved by isoform selectivity, not by dose. With a non-selective HSP90 inhibitor given systemically, the brain effect dominates and pain relief is lost. But the brain only uses HSP90α in this context, while the spinal cord recruits α, β, and GRP94. Collaboration with Dr. Brian Blagg at Notre Dame on β-and-GRP94-selective compounds has produced proof-of-concept IV data that reproduces the spinal-cord benefits — more potent morphine, reduced tolerance — without the brain blockade. The route from "intrathecal only" to "oral pill" runs through isoform selectivity. Biased agonism is in a harder place than the field often acknowledges. TRV-130 was denied FDA approval for lack of clear safety advantage. A phospho-null mu knock-in mouse from Stephan Schulz's group showed reduced tolerance but no respiratory-depression benefit. Attempts to replicate the arrestin-knockout phenotypes on clean mouse backgrounds have failed. Dr. Mary Canals' group has argued that some of the apparent bias benefits may actually reflect low intrinsic efficacy. Dr. Streicher calls himself an "informed outsider" on bias now, but his read is that the field needs deeper mechanism before the strategy can be rescued. A student's side project erased morphine reward. Graduate student David Duran wanted to test intermittent fasting in mice. Dr. Streicher was skeptical but gave the project room. The result: a six-hour feeding window for seven days increased morphine's antinociceptive efficacy in multiple pain models, strongly reduced tolerance and constipation, and completely blocked morphine reward in conditioned place preference. Receptor signaling assays showed efficacy shifts in the spinal cord and tolerance attenuation in the periaqueductal gray. The paper is published in Pain , and the translational path is unusually short — you don't need a ten-year IND process to test a feeding schedule in patients. Do not pursue something "completely novel" as a junior scientist. HSP90 in opioids was far enough off the beaten path that Dr. Streicher spent years fielding reviewer skepticism — no one has studied this, is this even real? His retrospective advice is to pick something novel but "still in the tent" — close enough to what the field recognizes that you earn credibility before trying to chase the real heresies. The lesson is not to play it safe; it is that unfamiliarity costs you credibility before your data can speak. Broad targets are not automatically undruggable. HSP90 is 2–3% of the protein content of every eukaryotic cell. A trained pharmacologist's first instinct is that the side effect burden would be crushing. But second-generation pan-HSP90 inhibitors have shown acceptable tolerability in oncology trials, Dr. Brian Blagg's KU-32 actually promotes neuronal survival in diabetic peripheral neuropathy and is now in Phase 1, and isoform selectivity narrows the footprint further. Dr. Streicher argues the field's default assumption — pick a low-expression, tissue-restricted target — is more habit than rule. Episode Timeline Timestamps were generated using AI for readability. 00:00 Introduction 01:22 Meet Dr. John Streicher 01:49 From heart failure to opioids — a path through signaling 07:49 Why the mu receptor still anchors his lab 09:51 The specificity puzzle — why ERK does a million things 13:31 What happened to biased agonism — replications in trouble 19:08 What's missing, and why HSP90 flips in the spinal cord 28:44 The "brain always wins" problem and isoform selectivity 33:05 HSP90 as Pac-Man — co-chaperones and the AHA1 clue 38:52 Picking projects that are "novel but in the tent" 47:25 The student's side project that blocked morphine reward 59:52 Running a lab through the first months of COVID Selected Quotes "A diode in your radio at home and a diode in a nuclear bomb could be exactly the same component but do radically different things depending on how they're organized." "The brain always wins. And when the brain wins, the antinociception is blocked — which is not what you want." "I'm normally a pretty skeptical, hard-headed person. But the data is the data. And I'm going to follow it." "Pick something that is novel, but is sort of still in the tent." About this episode Our guest in this episode of the Dr.GPCR podcast is Dr. John Streicher from the department of pharmacology at the University of Arizona. John started grad school in 1999 and spent some time figuring out what he was interested in. It turns out that it was signal transduction, and he worked on the signaling cascades involved in heart failure. His encounter and interest in signaling in the context of GPCRs during his postdoctoral training in Dr. Laura Bohn’s lab at Scripps Research Institute in Florida. Today, John and his team focus on understanding how signal transduction cascades downstream of the opioid receptors work, including the unique organization of chaperone protein Hsp90 modulation of opioid signaling in the brain versus the spinal cord. Dr. John Streicher on the web University of Arizona Department of Pharmacology Google Scholar Pubmed 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. 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Explore the milestones of Dr. GPCR, from its founding to today’s global community, and discover the journey that’s shaping the future of GPCR science. From Vision to Global Impact What began as a simple idea — to connect GPCR scientists and share knowledge freely — has grown into a global ecosystem driving collaboration, innovation, and discovery. Since 2020, Dr. GPCR has united researchers across disciplines and continents through conversations, summits, and shared milestones. 2020 🌱 The Beginning of a Community Vision & Launch Driven by a simple but powerful idea — to bring GPCR scientists together — Dr. Yamina Berchiche launched the Dr. GPCR Ecosystem , a space designed to break silos, spark collaboration, and open real dialogue across disciplines. Early Initiatives Feb 18, 2020 — The very first podcast episode was recorded. Jun 2020 — The first newsletter went out — to just three people . A small start, but the spark had been lit. Podcast Debut Jul 7, 2020 — The first Dr. GPCR Podcast episode premiered, featuring Dr. Paul Insel from UC San Diego — marking the beginning of hundreds of scientist-to-scientist conversations that would follow. First Summit Sep 14–18, 2020 — The inaugural Dr. GPCR Summit brought together researchers from five continents , with 5 live sessions , 26 pre-recorded talks , and five industry sponsors . A milestone moment that proved the power of community — even in a virtual world. Featured Appearances Aug 2020 — Featured on 17 Minutes of Science with Advancing GPCR Drug Discovery Through Collaboration . Oct 2020 — Presented at ERNEST with Beyond the Lab . Nov 2020 — Invited to the 9th GDR Meeting with Beyond the Lab . 2021 Expanding the Conversation Podcast Milestones Jan 2021 — Episode #26 released featuring Dr. Debbie Hay , University of Otago. Feb 2021 — Episode #27 released featuring Dr. Robert J. Lefkowitz , 2012 Nobel Laureate in Chemistry. 2nd Annual Summit Sep 13–19, 2021 — The 2nd Dr. GPCR Summit expanded the community’s reach and impact, featuring 27 live talks , 10 pre-recorded sessions , and five sponsors . Featured Appearances Jul 2021 — Featured at ECR Transatlantic with From Idea to Ecosystem . Oct 2021 — Featured at ERNEST with Where All GPCRs Are Created Equal . 2022 Building Momentum Podcast Growth May 2022 — Episode #37 released featuring Dr. Sam Hoare , Pharmechanics. May 2022 — Episode #42 released featuring Dr. Randy Hall , Emory University. New Programs Aug 11, 2022 — Virtual Café Series launched, featuring 16 episodes . Sep 20, 2022 — First contributor article published: Therapeutic validation of an orphan G protein‐coupled receptor by Inês Pinheiro . Oct 10–16, 2022 — Hosted the 3rd Annual Dr. GPCR Summit , featuring 34 live talks , 12 poster presentations , one pre-recorded session , and four partners . Dec 9, 2022 — GPCR Weekly News launched — now over 120 editions published . Community Engagement Mar 2022 — Featured at ERNEST with Dr. GPCR Ecosystem 2.0: Collaborating Better . Mar 2022 — Featured at ERNEST with Beyond the Lab . Mar 2022 — Media Partner at GPCR Targeted Drug Discovery Summit . May 2022 — Media Partner at GPCR Retreat . Jul 2022 — Media Partner at GPCR ECI Transatlantic . Nov 2022 — Featured at PhageMed Unige with Leadership Is a Learned Skill . 2023 A Year of Reflection and Growth Podcast Milestones Jan 2023 — Released the Dr. Marc Caron Tribute Episodes ( #100 , #101 & #102 ), featuring over 30 expert guests , including Dr. Kathleen Caron and Dr. Brian Kobilka , 2012 Nobel Laureate in Chemistry. First Symposium May 19, 2023 — Hosted the inaugural Dr. GPCR Symposium , bringing together over 100 attendees and featuring 11 live talks Community Engagement Feb 2023 — Media Partner at GPCR Targeted Drug Discovery Summit . Jun 2023 — Featured Talk Molecular Pharmacology GRC and GRS in Switzerland. Jun 2023 — Hosted Meet the Inoviem Team session. Nov 2023 — Co-organized the 22nd Great Lakes GPCR Retreat 2024 Strengthening Foundations and Expanding Horizons Educational Initiatives Feb 8, 2024 — Launched Dr. GPCR University with the first GPCR Course led by Dr. Terry Kenakin , enrolling 30+ students . Podcast Milestones May 9, 2024 — Episode #150 introduced the Dr. GPCR Team . May 16, 2024 — Episode #151 featured the Dr. GPCR Board . Community Engagement Mar 2024 — Media Partner at 3rd GPCR Targeted Drug Discovery Summit . Apr 2024 — Media Partner at Endocrine and Metabolic GPCRs meeting. Oct 2024 — Co-organized the Adhesion GPCR Workshop in Mexico City, with by 65+ participants . Oct 2024 — Media Partner at Discovery on Target . Non Profit Status Apr 2024 — Officially obtained non-profit organization status . Jul 12, 2024 — Hosted the first Board Meeting . Community Impact & Reach Podcast 180+ episodes 200+ guests 4,500+ hours of interviews 49,000+ plays Community 1,300+ ecosystem members 4 team members 6+ symposiums 15+ virtual café episodes Content 4,500+ GPCR papers categorized 200+ weekly news editions 100+ contributor articles 6 university courses Reach 3,800+ Twitter followers 3,000+ LinkedIn followers 100,000+ site sessions 400+ job listings shared

At Dr. GPCR, we are committed to making knowledge and resources accessible to researchers worldwide. If you live and work in a developing country, you may qualify for a 90%. Access for All: Supporting Scientists Worldwide Access shouldn’t depend on geography. If you live and work in a developing country, you can join the global GPCR community with 90% off Premium access. Advancing GPCR science, together—everywhere. Researchers in developing countries receive 90% off Premium Memberships, ensuring access to world-class GPCR training and collaboration tools. 🌍 Global Access for GPCR Scientists Scientific progress should never be limited by geography. To support the global GPCR community, Dr. GPCR offers significantly reduced Premium Membership pricing for scientists and professionals based in countries classified as developing economies by the World Bank. Our goal is simple: ensure that researchers everywhere can access the knowledge, tools, and community advancing GPCR drug discovery. Eligible members receive discounted access to Dr. GPCR Premium including but not limited to: Dr. GPCR Masterclass Live events Dr. GPCR Masterclass On-Demand library Dr. GPCR Weekly News Because breakthrough science happens faster when the global scientific community can fully participate. 💡 Questions about eligibility? Contact us at Hello@DrGPCR.org — we’re happy to help.e World Bank country classification . How does it work? 1️⃣ Confirm Your Eligibility This discount applies to individuals who live and work in developing countries, as defined by international economic classifications. 2️⃣ Submit Your Details Fill out the short form below with your name, email, institution, and country. 3️⃣ Receive Your Discount Code Once verified, we’ll send you a personalized code to unlock your discount on annual Premium access. 4️⃣ Activate Your Membership Sign up with your code and gain full access to courses, expert talks, community tools, and job resources — the same as every Premium member. Application Form First name* Last name* Email* Phone* Address* Affiliation* Position* Affiliation Website* Public Profile/LinkedIn* Apply

Join us as a featured guest on the Dr. GPCR Podcast! Explore the fascinating career journeys, groundbreaking discoveries, and impactful contributions of experts in GPCR biology. Share your insights and be part of the conversation. Complete the form below to become a guest - we'll reach out within 48 hours. Don't miss this opportunity to showcase your expertise! Be Our Guest – Dr. GPCR Podcast Share Your Research. Inspire the GPCR Community. Every episode of the Dr. GPCR Podcast features leading scientists, innovators, and biotech professionals whose work is advancing the understanding of G Protein-Coupled Receptors (GPCRs). We discuss breakthrough discoveries, career paths in pharmacology and molecular biology, and how each guest’s research contributes to the global GPCR ecosystem. If you’re working on exciting GPCR-related research — from structural biology to drug discovery — we’d love to feature your story. Fill out the form below and our team will contact you within 48 hours. Fill out this form Frequently asked questions About the Dr.GPCR Podcast At the high of the pandemic, I created the Dr. GPCR Podcast with three major goals in mind: Share the latest scientific discoveries in the GPCR field through discussions with experts Provide researchers with a different outlet to make their work known and Inspire young scientists to work on GPCRs It’s been a privilege to chat with so many GPCR scientists since 2020. Dr. GPCR’s mission is to bring together the GPCR community from all corners of the world to connect, exchange, and collaborate to improve human health through a better understanding of GPCR biology. So far we have recorded and released over 156 episodes and hosted GPCR specialists from all over the world, includingDr. Bryan Roth, Dr. Robert Lefkowitz, Dr. Fiona Marshall, Dr. Sam Hoare, Dr. Graciela Pineyro, Dr. Debbie Hay, Dr. Randy Hall, tributes toDr. Marc Caronwith over 30 guests includingDr. Kathleen Caron, Dr. Brian Kobilka, and many other amazing scientists. What is the format of the Dr.GPCR Podcast? Our podcast typically follows an interview-style format. We aim to have engaging conversations about you as a scientist, your career, your work, and anything related to GPCRs to provide valuable insights for our listeners. How long will the podcast recording take? The duration of the podcast recording may vary depending on the episode's topic and the flow of the conversation. On average, recordings usually take around 1 hour. We strive to keep the conversation focused and efficient while allowing enough time for in-depth discussions. How do I book the meeting on Calendly? In the invitation we provided a booking link. When clicking the link you’ll see a calendar, pick any date, and the schedule options will pop up. Then you will be asked to leave your name and email for future automated messages around our meeting. Can I reschedule or cancel our meeting? Yes, you can reschedule or cancel our meeting through Calendly. What should I expect during the recording process? Before we hit record, we will have a few minutes to discuss any questions or concerns and give you time to get comfortable. During the recording process, we will begin by introducing the episode and presenting you as our guest. We'll then engage in a conversation centered around your career and how you got introduced to GPCRs. Feel free to share your thoughts, experiences, and insights openly. If there are specific questions or talking points we plan to cover, we'll provide them in advance to help you prepare. We aim to ensure you have a great time and give a sneak peek at who you are as a scientist to the GPCR community. How should I prepare for the podcast recording? We always send our guests a Podcast Episode Outline, which includes all the questions we typically ask during the recording. You can take some time to gather your thoughts around these key points. These questions just serve as a guide, and we don’t have to go through all of them. Think of our chat as a casual discussion at an in-person conference where we are meeting for the first time. Sometimes we don’t follow the questions outlined because the discussion takes us to an also relevant and interesting conversation. We want to make sure that you are comfortable and we will never ask questions that would make you uncomfortable. Do I need to bring any equipment for the recording? In most cases, you won't need to bring any equipment for the recording as computers usually have all the necessary equipment integrated. If you do have an external microphone or webcam you’d like to use, it will make a difference, just make sure they are connected and working properly before going into the meeting. How do I join the recording session? All recordings are conducted via Zoom. Please ensure you test your Zoom setup before the meeting to avoid any technical issues. Are there any features you’d recommend to use? Recordings are done on Zoom. Touch-up- my appearance. Adjust for low light. We encourage you to have a headset with a good microphone. We also encourage you to be sitting in front of a window or in front of a sort of light so that your entire face can be seen in the recording. Please note that we do record audio and video. Can I promote my work or projects during the podcast? Absolutely! We encourage our guests to share information about their work, projects, or any relevant initiatives they are involved in. Our podcast is a great platform for you to showcase your expertise and connect with the GPCR community. Please feel free to mention and discuss your work during the conversation. Will there be an opportunity for me to ask questions or clarify any points? Yes, we value the interactive nature of our podcast and welcome your questions or requests for clarification. If you'd like to ask anything or any points you'd like to clarify before, during, or after the recording, please don't hesitate to speak up. We want to ensure that the discussion is engaging and informative for both our guests and our community. How will the podcast episode be promoted? Once the episode is recorded and edited*, we will promote it through various channels, including our website, multiple podcast streaming platforms, social media platforms, and email newsletters. We encourage you to share the episode with your audience as well. Together, we can maximize the episode's reach and impact. *Note that by editing, we mean removing any interruptions, or background noises, from the recording. We will not edit what you say unless you ask us to remove or add sections, sometimes we can re-record. When can I expect my podcast episode to be released? Your podcast episode will be released based on our production schedule and the order of episodes in the queue. We aim to provide an estimated release date after recording. Typically, episodes are released 4-6 weeks after recording. We'll notify you once it's live so you can share it with your network. Note that this timeline may vary if we take a break from releasing episodes, usually between December 15 and January 15. Can I listen to the episode after it’s been recorded? If you would like to listen to the episode after being recorded, we are more than happy to send it to you for your review. That being said, if there’s anything you’d like us to edit, feel free to reach out so we can work on it before it gets published. Can I watch the video podcast after it’s been published? The podcast video recordings are only available for the Premium Members on our Ecosystem. Anyone with a Free website membership or with an account on the different streaming platforms will have access to the podcast version only. How can I stay updated on future episodes or collaborate again in the future? To stay updated on future episodes and potential collaboration opportunities, we recommend subscribing to our podcast on your preferred platform. If you are interested in collaborating again, you can always fill out this form again and/or write to any of the following emails: hello@drgpcr.com I am still an undergraduate, Ph.D. student, or a post-doc, am I welcome to join as a guest? Yes, we value what anyone in the GPCR field has to say. For Dr.GPCR you are an expert in your own project, and we highly encourage you to accept our invitation to participate in the Podcast. Don’t hesitate to reach out to us if you’d like to recommend a colleague as a guest. Do you have any suggestions in terms of podcast equipment? Yes, here’s a list of accessible items we recommend for podcast creators: Video conference Lighting Kit Wireless microphone Any tips on achieving good lighting for the video podcast recording? Good lighting is key for any type of video. Here are some easy tips: Sitting in front of a window is always the best option for good lighting on any type of video. If we are recording at night or you don’t have natural light in your usual space, you can always use a desk lamp and put it next to the computer. The front light is always more flattering than the top light, which is what we usually have in house spaces. If you want to go like a pro, you can turn on a front light, and a backlight, that way you won’t look plain on camera. Listen and subscribe where you get your podcasts

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<< Back to podcast list Strategic Partner(s) Yao Lu (Jackie) About Yao Lu (Jackie) "Jackie is a Ph.D. student, at Monash University, Australia, investigating the role of functional selectivity in a novel class of potential antipsychotics for the treatment of schizophrenia. Her work involves the pharmacological and structural characterisation of novel putative antipsychotic small molecules. Her research aims to provide a molecular explanation of small molecules for their pre-clinical efficacy and to support the design of novel therapeutics. " Yao Lu (Jackie) on the web Monash University Georgina Sweet Fellowship Authorea 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 >>

Masha Niv on bitter taste GPCRs, the drug bitterness blind spot, and what heavy water reveals about the sweet taste receptor. << Back to podcast list Strategic Partner(s) Masha Niv: Bitter Taste Receptors and the Drug Discovery Blind Spot Taste receptors are among the most overlooked GPCRs in pharmacology - and Masha Niv has spent her career building the tools to change that. This conversation explores the biology, diversity, and unexpected reach of human taste GPCRs, beginning with the 25-subtype family of bitter taste receptors and extending into sweet receptor signaling, extraoral tissue expression, and the emerging science of taste-based drug prediction. Niv describes how bitter taste receptors differ structurally from most other GPCRs - missing conserved motifs, more prone to activation, and resistant to pharmacological blockade - and why those properties have shaped both the therapeutic opportunities and the research challenges her lab works on. She traces the receptor-ligand matchmaking problem at the heart of the field: 25 subtypes, thousands of known bitter compounds, and a network of associations that a machine learning recommendation system is now beginning to map. The conversation also covers what happens when taste pharmacology intersects with drug development - a collision that, for most of pharmaceutical history, has occurred too late. Niv's early exposure to bitterness as a formulation problem rooted her work in a question that still matters every time a patient refuses a pill. ABOUT THE GUEST Masha Niv is associate professor and vice dean of research and development at the Hebrew University of Jerusalem's Faculty of Agriculture, Food and Environment, located in Rehovot. A computational pharmacologist by training, she built BitterDB - the first dedicated database of bitter compounds - and has mapped the structural and chemical properties governing ligand promiscuity across all 25 human bitter taste receptor subtypes. Her lab uses homology modeling, machine learning, and collaborative sensory experiments to predict bitterness, identify antagonists, and understand how taste GPCRs function in tissues far from the tongue. She was also a key contributor to the GCCR consortium's large-scale chemosensory research during the COVID-19 pandemic. SCIENTIFIC THEMES OF THE CONVERSATION The architecture of bitter taste receptor diversity - 25 subtypes, ligand promiscuity, and the challenge of orphan receptors with no known ligand Extraoral expression of taste GPCRs - physiological roles in the airways, gut, heart, and cancer tissues Receptor-ligand matchmaking - applying recommendation system logic to the bitter taste receptor family Sweet taste receptor biology and the heavy water paradox - what a single atomic substitution reveals about receptor sensitivity Bitterness as a drug development variable - machine learning prediction, formulation consequences, and the FDA's late entry into the conversation COVID-19 and chemosensory science - how a global consortium formed from a handful of tweets and what it found about taste and smell loss KEY INSIGHTS FROM THE CONVERSATION 1. Bitter taste receptors are built to activate, not to be blocked Bitter taste GPCRs are structurally unusual within the broader GPCR family - they lack several conserved motifs and disulfide bridges present in most other subfamilies. Niv argues this architecture reflects evolutionary logic: a receptor whose job is to detect potential toxins before consumption should be maximally sensitive to activation. The cost is that finding antagonists for these receptors has proven far more difficult than finding agonists, a pharmacological asymmetry her lab is actively working to resolve. 2. Bitterness and toxicity are not the same thing - and the field had to prove it A long-standing assumption in both traditional medicine and drug development treated bitterness as a proxy for toxicity. Niv's work directly challenged that correlation: many intensely bitter compounds are non-toxic, and many toxic compounds are not bitter at all. Recognizing that distinction opened space for a more nuanced view of bitter compounds in nutrition and pharmacology - including the possibility that some bitterness in diet is associated with health benefit, not harm. 3. The drug bitterness blind spot persisted for decades because no one built the right tool early enough Drug discovery workflows screen extensively for efficacy, safety, and pharmacokinetics - but bitterness prediction was rarely incorporated until clinical or even post-market stages. Niv's lab developed a machine learning predictor trained on intensely bitter compounds that can flag bitterness risk from chemical structure alone, early in the development pipeline. The FDA recently made taste reporting a formal requirement, a regulatory shift Niv sees as overdue. 4. A single atomic change in water is enough to activate the sweet taste receptor Deuterated water - in which hydrogen is replaced by the heavier isotope deuterium - produces a measurable sweet signal in sensory experiments. Niv's lab showed that this response depends on the T1R2/T1R3 heterodimer sweet taste receptor: a known receptor inhibitor suppresses the sweetness of heavy water. What makes this finding unusual is the magnitude of the effect relative to the size of the chemical change - the mechanism is still under investigation, but the receptor involvement is established. 5. Taste receptor expression throughout the body reshapes the meaning of drug off-targets Bitter taste receptors are expressed not only in taste receptor cells on the tongue but in the upper airways, gut, heart, and certain cancer tissues. This extraoral distribution has practical consequences: drugs targeting other receptors may be inadvertently activating bitter taste GPCRs in the lung or intestine, contributing to effects that were never attributed to the right target. Niv sees this as one of the more underexplored dimensions of polypharmacology. 6. COVID-19 taste loss was a scientific detour that became something larger Niv had not planned to work on COVID-19 - she had never worked on viruses and was cautious about entering a field she did not know. When reports of taste impairment emerged, she felt obligated to contribute. A small cluster of Twitter exchanges became email threads, became a Slack workspace, became the GCCR consortium - a rapid-assembly international collaboration that surveyed tens of thousands of patients and found that while both smell and taste are impaired in the majority of symptomatic cases, smell loss is the stronger diagnostic signal. 7. The matchmaking problem - and why recommendation systems belong in receptor pharmacology With 25 subtypes, thousands of known bitter ligands, and a matrix of partial associations, the question of which compound activates which receptor is too large and too sparse for classical screening alone. Niv's lab is developing a recommendation system - trained on known receptor-ligand pairs and the structural properties of both - that can suggest candidate receptors for any new compound. The analogy she uses is direct: the system works the way a streaming platform learns your preferences from what similar users have watched. EPISODE TIMELINE Note: Timestamps below are AI-generated from the episode transcript and are approximate. Exact times may vary slightly from the final edited audio or video. 00:00 - Introduction and Dr. GPCR announcements 01:26 - Niv's career path - from theoretical chemistry in Russia and Israel to biotech, then a Cornell postdoc 08:03 - Choosing taste GPCRs as a research focus - how the arrival of GPCR structures made this the right moment 10:49 - The bitter taste receptor family - 25 subtypes, BitterDB, and the receptor-ligand matchmaking challenge 15:53 - Extraoral expression - bitter taste receptors in the airways, gut, heart, and cancer tissues 19:37 - Sweet taste receptors and an unexpected result - heavy water activates the T1R2/T1R3 heterodimer 23:53 - COVID-19 and chemosensory loss - how a global research consortium assembled from a handful of tweets 31:01 - The formulation problem - when a clinically effective drug fails because no one screened for bitterness 38:55 - Why bitter taste GPCRs resist antagonists - structural architecture and pharmacological consequences 41:58 - Taste GPCRs as drug targets - asthma, cardiac physiology, and early signals in cancer biology 44:18 - Rethinking bitterness in nutrition - the case for accepting bitter compounds in Western diet 50:13 - Advice for junior scientists and resources for the GPCR community SELECTED QUOTES "They are more prone to getting activated. They're missing some of the conserved motifs, some of the disulfide bridges. I think it has something to do with their architecture that makes it easier to activate them." "I often tell new PIs that the fact that I had to choose a topic with a specific flavor - that actually was good for me. Because that kind of made for me a niche which would be different from what my postdoc lab was doing." "It's such a small change and you get this effect. We know that the sweet taste receptor is involved - and how exactly, that is ongoing." "Let's not think about bitter as something just to get rid of, or try to put a lot of sugar on top of it so you don't feel it. Instead, try to get used to it - and accept that it's actually not bad." About this episode Dr. Niv is currently an associate professor and vice dean for research at the Hebrew University of Jerusalem. The Niv lab is also part of the Global Consortium for Chemosensory Research. Masha earned her Bachelor’s degree in chemistry, followed by a direct Ph.D. at the Institute of Chemistry, at The Hebrew University of Jerusalem in Israel. Dr. Niv trained as a postdoctoral fellow at Weill Cornell Medical College. Her work focuses on both sweet and bitter taste receptor GPCRs and her lab established the BitterDB . Dr. Masha Niv on the web Niv Lab LinkedIn Twitter Pubmed Google Scholar 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 >>

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Can models predict drug outcomes? Jens Carlsson shares how GPCR modeling is moving from explanation to real prediction in drug discovery. << Back to podcast list Strategic Partner(s) Model. Predict. Discover. with Dr. Jens Carlsson What if models didn’t just explain the past — but could truly predict what comes next? In this episode, Dr. Jens Carlsson reveals how computational modeling is evolving from explanation to real prediction—and how that shift accelerates real-world discovery. Dr. Jens Carlsson, Professor of Computational Biochemistry at Uppsala University, joins Dr. Yamina Berchiche to share his unconventional journey from aspiring engineer to GPCR modeler. With a deep focus on structure-based drug design, Jens discusses how his lab bridges simulation and experiment—and why understanding the limits of prediction is just as critical as the predictions themselves. From virtual screening of billions of molecules to leveraging AlphaFold for structure prediction, Jens shares the cutting-edge tools his lab uses—and the collaborative mindset required to turn models into testable hypotheses. Along the way, he reflects on key career moments, the role of mentorship, and how curiosity continues to drive his work across both academic and industry settings. Why This Matters Computational models are moving beyond interpretation into real-world prediction of ligand-receptor interactions. Bridging computation, chemistry, and pharmacology is key to speeding up drug discovery. AI and machine learning are opening new doors—but only if scientists know their tools’ limits. What You’ll Learn Why Jens Carlsson believes modeling should predict , not just explain How his team uses structure-based modeling to identify novel GPCR ligands The value of failure—and how it shaped his path as a scientist Why collaborations between modelers and experimentalists are more vital than ever How AlphaFold is shaking up structural biology—and where it still falls short Advice for junior scientists: what really matters when building a research career Who Should Listen GPCR scientists and pharmacologists Computational chemists and structural biologists Early-career researchers exploring drug discovery Biotech leaders and R&D strategists Anyone interested in predictive modeling, AI in biology, or structure-function relationships About Jens Carlsson Jens Carlsson is a Professor of Computational Biochemistry at Uppsala University, where his research group uses structure-based modeling to investigate GPCRs. His team focuses on understanding how ligands modulate receptor function and how those insights can drive drug discovery. By combining molecular docking, molecular dynamics, and machine learning, Jens works at the intersection of computation and pharmacology, often in close collaboration with experimental labs. Trained initially as a biotechnology engineer, Jens discovered his true calling during an internship where his modeling skills stood out, mainly because his bench skills didn’t. That moment launched a career built around using computational tools to answer big biological questions. His journey took him from Sweden to Scripps Research and UCSF, where he was first introduced to GPCRs and mentored by pioneers like Brian Shoichet and Ken Jacobson. Jens is passionate about prediction over explanation: building models that can guide experiments, not just interpret them. Outside academia, he advises companies through a consulting arm focused on ligand design strategy. With a reputation for collaborative science, Jens is a strong advocate for bringing together chemists, modelers, and biologists to accelerate discovery and train the next generation of GPCR researchers. Jens Carlsson on the web Carlsson Group Uppsala University LinkedIn Hit play now to hear how prediction is reshaping GPCR science, and what that means for the future of 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 >>

Advanced GPCR webinars for pharmacologists and biotech scientists. Live Q&A. Deep mechanistic insight. Reserve your seat. University / Free & Live Webinar Live GPCR Webinars with the World's Leading Experts. Deep-dive sessions focused on real pharmacology, real drug discovery challenges, and real translational insight. Live Q&A with the scientists shaping the field. Live for those who can be there. On demand for everyone else. 👉 Sign Up for Notifications Get the live link before each session Strategic Partners Webinars Upcoming Live & On Demand Webinars Tuning GPCR System Sensitivity: Revealing True Drug Activity Through Functional Volume Control Speaker: Dr. Terry Kenakin | Terry's Pharmacology Corner What you'll learn during the session: How functional system sensitivity for receptor expression becomes a tool for determining the properties of a molecule Why testing agonists in low sensitivity systems separates affinity and efficacy and enables prediction of agonism in other systems How testing antagonists in high sensitivity systems detects low levels of efficacy and, through constitutive activity, inverse agonism How volume control reveals essential properties of allosteric modulators, including PAM-agonism and changes in efficacy 📅 September 24, 2026 at 11:00:00 AM Details Recombinant Antibodies for GPCRs: A Challenge to the Community Speakers Dr. Alexander Ball, MD Dr. Alexander Ball of GeneTex joins Dr. GPCR to walk through what the company is doing about it, and the challenge it comes with: A high-throughput recombinant antibody platform built for specificity at scale Prioritized validation: CRISPR KO/KD, endogenous expression, cell fractionation, comparable antibodies, application-specific testing VirDTM-GPCR arrays for cross-reactivity screening when feasible More than 300 recombinant mAbs against almost 200 human GPCRs, and growing Free samples for GPCR researchers who will test the antibodies in their own labs and give structured feedback 📅 June 25, 2026 at 11:00:00 AM Details Receptor Signaling Bias: A Valuable and Accessible Property of New Drug Candidates Speaker Dr. Terry Kenakin - UNC Chappel Hill | Terry's Pharmacology Corner Topics Covered The biological basis of receptor signaling bias and ligand-dependent conformations How to design functional assay panels that quantify bias rather than infer it Interpretation pitfalls and what assay system choice does to bias estimates Translating pathway-level data into lead selection and optimization decisions Why potency alone is not enough for candidate-level decisions 📅 May 28, 2026 at 11:00:00 AM Details 1 2 1 ... 1 2 ... 2 1,400+ Scientists in the Ecosystem 30+ Countries Represented 60–90 Scientists per Live Session Free Always. No Paywall. No Catch. Use It Tomorrow Practical takeaways, every session. Walk away with something you can apply in your next experiment, assay, or project decision. Together in the Room Scientists from around the world, in the same conversation. The chat, the Q&A, the shared curiosity — the community thinking together in real time. Free and Generous No paywall. No catch. The ecosystem gives this away because GPCR scientists deserve access to high-quality science. Sign up, show up, bring your questions. Direct Access Ask an expert a live question and get a real answer. That direct access doesn't exist at conferences — it exists here. No Borders Live for those who can be there. On demand for everyone else. The GPCR community doesn't stop at borders — and neither do we. Stay Ahead Learn about methods, tools, and approaches before they become widely known. Be ahead of colleagues who aren't in the ecosystem. What Makes These Webinars Different? Not a lecture. A scientific exchange. Built for the GPCR community, by the GPCR community. Every session is designed to move your science forward. First Dr. GPCR event? Welcome. This is what the community looks like — scientists from around the world, thinking through discovery challenges together. There's no paywall, no catch. Just real science and real exchange. If this is your first session, there's a lot more where this came from. Want to Go Deeper? This Is Just the Beginning If a free webinar is this good, imagine what the full ecosystem looks like. Dr. GPCR University brings you premium Masterclass sessions, 200+ recordings, weekly curated news, and a global community of GPCR scientists — all in one place. Webinar → Weekly News → 14-Day Trial → University Premium 👉 Sign Up for Notifications These sessions are part of a larger mission: building the most trusted home for GPCR scientists worldwide. Frequently Asked Questions Questions about the webinars What are GPCR webinars? GPCR webinars are free, live online scientific sessions focused on G protein-coupled receptor biology, pharmacology, signaling, and drug discovery. Each session explores mechanistic models, translational challenges, and real-world therapeutic implications through presentations and live Q&A. They're designed for scientists who want deep, data-driven discussion rather than surface-level overviews. Who should attend? Any scientist working with GPCRs — pharmacologists, medicinal chemists, cell biologists, translational researchers, discovery teams, postdocs, PIs, and industry scientists. Whether you're deep in receptor biology or evaluating assay tools, these sessions are built for you. Are the webinars free? Yes. Always. No paywall, no catch. Sign up with a free registration and you'll receive the live link before each session. Recordings are also freely available on demand afterward. Are the webinars live or pre-recorded? All webinars are live events with real-time Q&A — that's the point. After the live session, the full recording becomes available on demand so scientists in every time zone can access the same content and depth. How are these different from conference talks or academic seminars? The Q&A is the core, not an afterthought. These sessions are designed for interaction — scientists asking direct questions and getting real answers. There's no travel required, no registration fee, and you're in a room with researchers from dozens of countries who share your focus on GPCRs. What topics are typically covered? GPCR pharmacology, signaling, structural biology, allosteric modulation, biased agonism, assay design, drug discovery workflows, translational challenges, and the science behind emerging tools and methods. Every session is grounded in receptor biology with a focus on what's practical and applicable. Do I need prior knowledge of GPCR pharmacology? A working understanding of GPCR biology helps you get the most from each session. That said, the presenters are skilled at making complex science accessible, and the Q&A often covers foundational questions alongside advanced discussion. Where can I find more advanced GPCR training? If you want to go deeper, Dr. GPCR University offers premium Masterclass sessions with frontier science, unresolved questions, and extended scientific exchange — exclusively with independent scientists. The webinars are the open door; Masterclass is the room you earn access to. You can explore University with a 14-day trial. Be in the Room When the Science Moves Forward Sign up to get notifications about upcoming webinars. Bring your questions. 👉 Sign Up for Notifications

Discover Media Partner Packages with Dr. GPCR Ecosystem. Amplify your brand, reach a targeted scientific audience, and showcase your organization in the GPCR community. The Yearly Glow Only 12 companies per year are invited to become Yearly Glow partners. This isn't advertising — it's a strategic partnership that puts your brand at the center of the scientific conversations that matter most. 1,400+ GPCR scientists reached 25–50% Newsletter open rate 12 strategic partnerships per year — because quality matters Partner with us Today! Who Media Partnerships Are For? Companies that think in years, not quarters Strategic Media Partnerships are ideal for GPCR-focused companies that want to: Strengthen brand credibility and recognition within the GPCR research community Associate their brand with high-quality science, experts, and long-term ecosystem initiatives Be consistently visible across trusted educational and content platforms Build awareness and trust over time — not chase immediate leads If your primary goal is to drive inbound inquiries or make your services discoverable at the point of need, the GPCR CRO Bank may be a better fit. "Dr. GPCR is the world's largest nonprofit community focused on GPCRs. As a strtegic partner, you'll gain trusted access to an engaged audience of academic researchers, biotech teams, and drug discovery innovators — without having to fight for attention." Why Partner with Dr. GPCR? Featured across our nonprofit platform, trusted by thousands As a media partner, you'll be featured across our nonprofit platform, trusted by thousands of GPCR scientists and biotech professionals. Reach Qualified Researchers Connect with scientists who are actively looking for tools like yours, without the noise of general platforms. Build Trust Develop content that speaks their language and establishes your credibility in the GPCR research community. Join a Curated Ecosystem Become part of a collaborative, curated ecosystem — not just another name on a crowded vendor list. What You Get as Media Partner? Active visibility, not passive placement These touch points are designed to reinforce brand presence and credibility through repeated, trusted exposure — not direct lead generation. Yearly Glow Exclusive Gated Content Premium content assets created in partnership — gated to capture and nurture scientist engagement while contributing genuine value to the community. Strategy Partnership Ongoing strategic collaboration to align visibility initiatives with your goals and the community's needs. Launch Campaigns Strategic campaigns that actively drive scientist awareness and traffic toward your offerings, timed to maximize community attention. Logo Positioning Strategic Partner logos are featured across multiple high-traffic ecosystem pages, creating repeated visual association with trusted GPCR content and resources. Base Package — Included 🎙️ Featured Podcast Episode ✓ Be the guest on a dedicated episode of the Dr. GPCR Podcast ✓ Feature up to 3 team members to share your story ✓ Distributed across podcast platforms and social media ✨ Logo positioning ✓ Strategic Partner logos are featured across multiple high-traffic ecosystem pages, creating repeated visual association with trusted GPCR content and resources. 📣 Social Media Promotion ✓ Engaging posts about your organization ✓ Targeted to GPCR researchers and biotech professionals ✓ Shared on LinkedIn and X (Twitter) 📝 Blog Contributions ✓ Contribute to blog posts on the Dr. GPCR platform as a valued partner ✓ Share insights on product launches, scientific discoveries, or customer stories ✓ Reach a targeted scientific audience with your contributions. 📄 Custom Company Page ✓ Permanent company profile on the Dr. GPCR Ecosystem ✓ Logo, branding, and description of your mission ✓ Contact links and key highlights 📬 Newsletter Visibility ✓ Featured in our highly read weekly newsletter ✓ Tell your story with context, clarity, and purpose ✓ Bonus: Mentioned in podcast intros/outros 👩🔬 Premium Licenses ✓ 10 Scientists Premium Accounts ✓ 3 Non-Scientists Premium Accounts 🎤 Co-Branded Events & Training ✓ Collaborate on webinars and virtual training sessions to showcase your expertise ✓ Host educational events that focus on GPCR research ✓ Engage directly with the GPCR research community through these initiatives 12 per year — a commitment to quality Only 12 Yearly Glow seats are available each year to keep our ecosystem curated, impactful, and community-focused. Every partner deserves dedicated attention, personalized strategy, and genuine integration. This is real selectivity — a reflection of how seriously we take partner quality and community trust. Previous Partners Join these leading organizations Join these leading organizations in the GPCR research ecosystem. Book Book a 30-minute Strategy Call with Yamina Ready to Connect with the GPCR Community? With only 10 spots remaining for 2026... Secure your place in our exclusive media partner program today.

< Back to Webinars 📅 Tuesday, March 3, 2026 at 10:00:00 AM EST 🤝 Webinar in collaboration with: Celtarys Research Fluorescent Probes for GLP-1R and GIPR Imaging: From Cell Assays to In Vivo Systems Fluorescent tools for imaging endogenous incretin receptors across biological systems Interrogating Incretin Receptor Biology Across Biological Complexity GLP-1 and GIP receptors have emerged as central targets in metabolic medicine, yet their precise localization, nanodomain organization, and functional engagement within complex biological systems remain incompletely understood. Fluorescent chemical probes offer one of the most direct approaches for investigating receptor distribution and dynamics in native contexts — without relying on receptor overexpression or genetic modification. This webinar introduces two families of advanced fluorescent probes developed specifically for working with endogenous GLP-1R and GIPR across a range of biological complexity. Attendees will gain a technical understanding of probe design, selectivity, and validated applications — as well as practical guidance on handling, reconstitution, dilution, and storage to support immediate laboratory deployment. LUXendin Family Red and far-red fluorescent GLP-1R antagonists derived from Exendin4(9–39). Enable high-specificity labeling of endogenous GLP-1R in live and fixed cells, pancreatic islets, and whole-organ preparations — without triggering receptor activation. Available across multiple spectral ranges for confocal, super-resolution, and intravital imaging. daLUXendin Family Fluorescent dual agonists for both GLP-1R and GIPR (daLUXendin544+ and daLUXendin660+), structurally related to tirzepatide. Enable simultaneous visualization of endogenous receptor localization and nanodomain organization in pancreatic islet cells and neural sites of action in vivo. Speakers Dr. Johannes Broichhagen Group Leader Leibniz Research Institute for Molecular Pharmacology (FMP), Berlin Dr. Broichhagen trained in chemistry at the University of Erlangen-Nuremberg, completed his doctorate at LMU Munich in 2014, and undertook postdoctoral work at EPFL (Switzerland) and the Max Planck Institute for Medical Research (Heidelberg). Since 2020, he leads an independent research group at the FMP Berlin. His group focuses on the development of chemical tools — including fluorescent ligands and photopharmacological compounds — to investigate GPCR biology with spatial and temporal precision. He is a principal architect of the LUXendin and daLUXendin probe families. Dr. David Hodson Robert Turner Professor of Diabetic Medicine Oxford Centre for Diabetes, Endocrinology and Metabolism, University of Oxford Dr. Hodson is a veterinary surgeon by training who pursued postdoctoral studies at the CNRS in Montpellier before establishing his independent laboratory at Imperial College London as a Diabetes UK RD Lawrence Fellow. He previously served as Professor of Cellular Metabolism and Institute Deputy Director at the University of Birmingham. His research group develops and applies novel technologies to investigate GLP-1 and GIP receptors — two class B GPCRs central to glucose homeostasis, food intake regulation, and inflammation — within complex tissue environments including the pancreas and brain. His work carries direct translational relevance to diabetes and obesity therapeutics. Organizers Celtarys Research Celtarys develops and commercializes fluorescent chemical tools and related screening services that enable fluorescence-based methods across drug discovery. The company's portfolio is built around high-affinity, selective fluorescent ligands for GPCRs, supporting researchers working at the interface of chemical biology and pharmacology. Broad GPCR fluorescent ligand portfolio across multiple receptor families Fluorescence Polarization, HTRF, and High-Content Screening formats Fluorescence microscopy and flow cytometry applications Screening services using proprietary probes in living cells Custom chemical development for probe and ligand creation Dr. GPCR Dr. GPCR is a membership-based nonprofit ecosystem dedicated to advancing GPCR-targeted drug discovery. It provides curated industry intelligence, expert-led masterclasses, and structured engagement opportunities for scientists and biotech leaders working across pharmacology, translational research, and therapeutic development. Curated intelligence on GPCR drug discovery trends and developments Expert-led webinars and masterclasses with leading researchers Structured networking for scientists and biotech professionals Nonprofit model — community-first, member-driven Free membership tier available Previous Webinar Next Webinar Don’t Miss the Next Live Session Dr. GPCR membership gives you access to all upcoming live, interactive webinars. Free. Takes less than a minute to join. Cancel anytime. Sign Up for Free

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Live webinar with Dr. Terry Kenakin on detecting, quantifying, and applying receptor signaling bias in GPCR drug discovery. May 28, 2026. Free. < Back to Webinars 📅 Thursday, May 28, 2026 at 11:00:00 AM EDT 🤝 Webinar in collaboration with: Eurofins DiscoverX Receptor Signaling Bias: A Valuable and Accessible Property of New Drug Candidates Turning functional selectivity into a practical decision-making tool in GPCR drug discovery Beyond Potency: What Ligand-Dependent Signaling Reveals About Drug Candidates G protein-coupled receptors can signal through multiple intracellular pathways, and ligands do not necessarily engage those pathways to the same extent. This phenomenon, receptor signaling bias or functional selectivity, is now recognized as a meaningful property of many drug candidates and a potential route to improved efficacy, better tolerability, and new opportunities in challenging targets. Bias is not an anomaly. It is a consequence of ligand-dependent receptor conformations and allosteric probe dependence, and it can be revealed with the right combination of functional assays. This webinar explains the biological basis of signaling bias, shows how to detect and quantify it using reliable functional assays, and discusses how these data can guide lead selection and optimization. Practical assay strategies, interpretation pitfalls, and the value of comparing pathway outputs quantitatively, rather than relying on potency alone, sit at the center of the session. The Biology Behind Bias Ligands produce differential pathway engagement at a single receptor because they stabilize distinct receptor conformations. These conformations determine which downstream pathways are favored and which are muted. Due to this potential inherent bias, it is best practice to evaluate multiple pathways using different GPCR assays to obtain a better understanding of the ligand effects on the GPCR system. Speaker Dr. Terry Kenakin Professor of Pharmacology & Pharmacology Course Coordinator Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill. Dr. Kenakin trained in chemistry and pharmacology at the University of Alberta and completed postdoctoral work at University College London in the laboratory of Sir James Black. He spent 25 years in drug discovery at Glaxo (now GlaxoSmithKline) before joining UNC Chapel Hill, where he teaches and leads research in receptor pharmacology. His work is central to the quantitative framework used today to describe receptor signaling bias, allosteric function, and agonism. He proposed one of the first mechanistic explanations of biased signaling and co-authored the widely-applied simple method for quantifying functional selectivity. He is the author of A Pharmacology Primer, Editor-in-Chief of the Journal of Receptors and Signal Transduction, and a Fellow of the British Pharmacological Society, recognized with the Goodman and Gilman Award from ASPET and the Gaddum Memorial Award. Within the Dr. GPCR ecosystem, Terry hosts Terry's Corner, a live room where GPCR scientists get direct access to him. It's where the mechanistic questions that usually sit beneath the data get asked out loud, and where receptor theory, biased signaling, and the pharmacology of real drug discovery decisions are worked through together. Organizers Eurofins DiscoverX Eurofins DiscoverX is a one-stop-shop for GPCR drug discovery and development, with 25+ years of expertise and validated cell-based assays spanning basic research through therapeutic discovery, optimization, and regulatory submission. Their assays are industry-standard, accepted for regulatory potency testing, and backed by thousands of peer-reviewed publications and partnerships with leading pharma and biotech companies. 1,500 human GPCR products covering ~90% of the GPCR-ome, including orphan receptors and ortholog variants Multiple mechanisms of action: cAMP accumulation, β-arrestin recruitment, receptor internalization, ligand binding, calcium flux, and pharmaco-chaperone discovery Flexible formats: cell line assay kits, ready-to-use eXpress kits, qualified bioassays, membrane preps, detection kits, and custom products Applications across target identification, HTS, lead optimization, ligand bias and allostery evaluation, safety assessment, and regulatory potency testing Dedicated portfolio for obesity and diabetes GPCR targets (GLP-1R, GIPR, GCGR, MC4R, AMY receptors, and more) Dr. GPCR Dr. GPCR is a membership-based nonprofit ecosystem dedicated to advancing GPCR-targeted drug discovery. It provides curated industry intelligence, expert-led masterclasses, and structured engagement opportunities for scientists and biotech leaders working across pharmacology, translational research, and therapeutic development. Curated intelligence on GPCR drug discovery trends and developments Expert-led webinars and masterclasses with leading researchers Structured networking for scientists and biotech professionals Nonprofit model, community-first, member-driven Free membership tier available Previous Webinar Next Webinar Don’t Miss the Next Live Session Dr. GPCR membership gives you access to all upcoming live, interactive webinars. Free. Takes less than a minute to join. Cancel anytime. Sign Up for Free

< Back to Vault Title I'm a paragraph. I'm connected to your collection through a dataset. Click Preview to see my content. To update me, go to the Data Manager. This Vault is available to Dr. GPCR Premium members. Built for founders who prefer clarity over chaos and confusion. Biotech Decision Vault by Attila Foris Strategic Business & Operating Systems Advisor Dr. GPCR Ecosystem

Dr. Alexander Ball of GeneTex on the recombinant platform and validation strategy behind a challenge to GPCR researchers. Free live webinar, June 25. < Back to Webinars 📅 Thursday, June 25, 2026 at 11:00:00 AM EDT 🤝 Webinar in collaboration with: GeneTex Recombinant Antibodies for GPCRs: A Challenge to the Community Test them in your lab. Tell GeneTex what works and what doesn't. A reagent gap that holds back the biology GPCR activity is targeted by one-third of all FDA-approved drugs. Yet much remains to be learned about how these 800-plus receptors are expressed and how they function in living systems. Part of the gap is biology. Multipass transmembrane proteins are genuinely difficult targets. Part of the gap is the reagents. Reliable antibodies for human GPCRs are scarce, and without them, basic questions about expression and physiological function stay out of reach. Producing specific antibodies for human GPCRs is a formidable job. Expression levels in common cell lines are often low. Identifying an immunoreactive antigen sequence that is specific for a single receptor and detectable across applications is difficult on its own. The literature often disagrees on which antibodies actually work. Proving specificity for the intended GPCR is rarely straightforward. GeneTex is tackling that problem with a high-throughput recombinant antibody platform paired with enhanced validation strategies. The approach has already generated more than 300 recombinant monoclonal antibodies against almost 200 human GPCRs, and the catalog keeps growing. Inside the platform The production workflow is built to detect promising clones early and to hold specificity, scalability, and consistency steady once those clones are selected. Dr. Ball will walk through how the recombinant platform was built, what it takes to produce specific antibodies against multipass transmembrane targets including GPCRs at scale, and how the workflow handles the realities of low endogenous expression and tight specificity requirements. Validation that earns the catalog its place Every antibody is characterized through a prioritized validation set: CRISPR-based knockout and knockdown protocols, endogenous expression detection, cell fractionation, comparable antibody testing, and application-specific testing. When feasible, GeneTex uses VirDTM-GPCR arrays (CDI Labs, Mayagüez, PR), which present a nearly comprehensive library of human non-olfactory GPCRs individually expressed on herpes simplex virion envelopes for cross-reactivity screening. Dr. Ball will walk through each, explain why KO/KD testing is prioritized, and show how the validation data is shared with researchers. The challenge: test them in your lab This is the goal of the Dr. GPCR x GeneTex partnership. GeneTex is offering free samples of the recombinant antibodies to GPCR researchers in exchange for structured feedback, positive or negative. As Dr. Ball puts it in his own words, the primary goal is to get these reagents tested and evaluated by GPCR researchers. That is how a catalog earns the trust of the community, and how the community ends up with reagents it can actually rely on. Dr. Ball will explain how the challenge works, who it is for, and how to request samples. Speaker Dr. Alexander Ball , MD, Senior Scientist, GeneTex, Inc. Dr. Ball has been with GeneTex since 2012 and leads the company's enhanced antibody validation initiative. He earned an M.D. from the University of Southern California School of Medicine and completed internal medicine training at California Pacific Medical Center in San Francisco. He transitioned from clinical medicine to academic research at UC Irvine, where he worked on protein complexes mediating chromosome dynamics. At GeneTex, that background shapes how he thinks about reagent quality. Antibodies are tools scientists depend on, and validation is not optional. Organizers GeneTex GeneTex is a multinational antibody manufacturer founded in San Antonio, Texas in 1997. Since 2020, its recombinant monoclonal antibody facility has produced reagents paired with enhanced validation protocols and a strong emphasis on KO/KD testing. The company's GPCR program is building a comprehensive catalog of recombinant monoclonal antibodies for the human nonsensory and orphan GPCRs. More than 300 recombinant monoclonal antibodies against almost 200 human GPCRs, and growing Prioritized validation: CRISPR KO/KD, endogenous expression, cell fractionation, comparable antibodies, application-specific testing VirDTM-GPCR arrays for specificity screening when feasible Free samples available to GPCR researchers willing to give structured feedback Yearly Glow Strategic Partner in the Dr. GPCR ecosystem Dr. GPCR Dr. GPCR is a nonprofit ecosystem dedicated to advancing GPCR-targeted drug discovery. Through curated intelligence, community engagement, podcasts, webinars, and editorial content, Dr. GPCR connects scientists, tools, and decision-makers across academia and industry, all year round. Previous Webinar Next Webinar Don’t Miss the Next Live Session Dr. GPCR membership gives you access to all upcoming live, interactive webinars. Free. Takes less than a minute to join. Cancel anytime. Sign Up for Free

< Back to Vault Title I'm a paragraph. I'm connected to your collection through a dataset. Click Preview to see my content. To update me, go to the Data Manager. This Vault is available to Dr. GPCR Premium members. Built for founders who prefer clarity over chaos and confusion. Biotech Decision Vault by Attila Foris Strategic Business & Operating Systems Advisor Dr. GPCR Ecosystem

Live webinar with Dr. Terry Kenakin on tuning GPCR system sensitivity to reveal true drug activity. September 24, 2026. Free. < Back to Webinars 📅 Thursday, September 24, 2026 at 11:00:00 AM EDT 🤝 Webinar in collaboration with: Eurofins DiscoverX Tuning GPCR System Sensitivity: Revealing True Drug Activity Through Functional Volume Control Dr. Terry Kenakin shows how tuning receptor expression separates affinity from efficacy, unmasks hidden agonism and inverse agonism, and helps predict how a compound will behave in vivo. The pharmacology of a drug is shaped not only by the molecule but by the sensitivity of the system it is measured in. Receptor density and coupling efficiency change what a ligand appears to do, which is part of why in vitro results do not always translate in vivo . This session presents functional volume control, the deliberate tuning of system sensitivity, as a way to separate a ligand's true affinity and efficacy from the system it was tested in. Dr. Terry Kenakin will show how reducing sensitivity lets you measure affinity and relative efficacy and turn low-efficacy agonists into measurable antagonists, how increasing sensitivity uncovers efficacy hidden in apparently neutral compounds, and how greatly increasing it reveals inverse agonism through constitutive activity. The same approach distinguishes what an allosteric modulator does to affinity versus efficacy, including PAM-agonism. Examples run across inducible, low, and medium expression systems. Why System Sensitivity Changes What You Measure The response to an agonist depends on its concentration and efficacy, and on the system: how many receptors are present and how well they couple to their effectors. Two assays with different sensitivities can report different behavior for the same molecule. Treated as a variable to control for, that is noise. Set on purpose, it becomes a measurement tool. From the Assay to the Candidate Reduce sensitivity and affinity separates from efficacy, so system-independent values can be measured and used to predict behavior elsewhere. Raise it and low-level efficacy that would drive agonism in a sensitive tissue becomes visible. Raise it further and inverse agonism appears where a calcium assay would have called the compound a neutral antagonist. Each setting answers a different question about a real candidate. Speaker Dr. Terry Kenakin Professor of Pharmacology and Pharmacology Course Coordinator Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill Head Instructor, Terry's Pharmacology Corner Dr. Kenakin trained in chemistry and pharmacology at the University of Alberta and completed postdoctoral work at University College London in the laboratory of Sir James Black. He spent 25 years in drug discovery at Glaxo, now GlaxoSmithKline, before joining UNC Chapel Hill, where he teaches and leads research in receptor pharmacology. His work is central to the quantitative framework used today to describe receptor signaling bias, allosteric function, and agonism. He proposed one of the first mechanistic explanations of biased signaling and co-authored the widely applied simple method for quantifying functional selectivity. He is the author of A Pharmacology Primer, Editor-in-Chief of the Journal of Receptors and Signal Transduction, and a Fellow of the British Pharmacological Society, recognized with the Goodman and Gilman Award from ASPET and the Gaddum Memorial Award. Within the Dr. GPCR ecosystem, he is Head Instructor of Terry's Corner, a space for live AMAs, short-form mechanistic discussions, and ongoing dialogue with the GPCR community on receptor theory, biased signaling, and the decisions that shape real drug discovery programs. Organizers Eurofins DiscoverX Eurofins DiscoverX is a one-stop-shop for GPCR drug discovery and development, with 25+ years of expertise and validated cell-based assays spanning basic research through therapeutic discovery, optimization, and regulatory submission. Their assays are industry-standard, accepted for regulatory potency testing, and backed by thousands of peer-reviewed publications and partnerships with leading pharma and biotech companies. >1,500 human GPCR products covering ~90% of the GPCR-ome, including orphan receptors and ortholog variants Multiple mechanisms of action: cAMP accumulation, β-arrestin recruitment, receptor internalization, ligand binding, calcium flux, pharmaco-chaperone discovery Flexible formats: cell line assay kits, ready-to-use eXpress kits, qualified bioassays, membrane preps, detection kits, and custom products Applications across target identification, HTS, lead optimization, ligand bias and allostery evaluation, safety assessment, and regulatory potency testing Dedicated portfolio for obesity and diabetes GPCR targets (GLP-1R, GIPR, GCGR, MC4R, AMY receptors, and more) Dr. GPCR Dr. GPCR is a membership-based nonprofit ecosystem dedicated to advancing GPCR-targeted drug discovery. It provides curated industry intelligence, expert-led masterclasses, and structured engagement opportunities for scientists and biotech leaders working across pharmacology, translational research, and therapeutic development. Curated intelligence on GPCR drug discovery trends and developments Expert-led webinars and masterclasses with leading researchers Structured networking for scientists and biotech professionals Nonprofit model, community-first, member-driven Free membership tier available Previous Webinar Next Webinar Don’t Miss the Next Live Session Dr. GPCR membership gives you access to all upcoming live, interactive webinars. Free. Takes less than a minute to join. Cancel anytime. Sign Up for Free

Equip your research team with expert-led GPCR pharmacology training. Get 25% off Annual Premium Memberships for teams of five or more. Activate in days. Home Courses Articles About Log In / Sign Up Equip Your Team with Terry Kenakin’s Pharmacology Frameworks Used by discovery scientists across biotech, pharma, and academia. Shared pharmacology discipline for discovery teams. When scientists interpret pharmacology through the same frameworks, experiments become clearer and program decisions become stronger. Train 5 or more team members and receive 25% off annual access. $2,249.25 per person / year Activate Team Membership Why Teams Use Terry’s Corner Discovery programs move faster when scientists interpret pharmacology through the same mechanistic frameworks. Terry’s Corner helps teams align how they analyze receptor pharmacology, signaling data, and translational outcomes. That alignment reduces misinterpretation and improves experimental strategy across programs. What Your Team Gets? • Pharmacology frameworks used in modern drug discovery • Monthly live AMA discussions with Terry Kenakin • Ongoing Terry’s Corner lessons and analysis • Ability to suggest topics relevant to your programs • Access for biotech, pharma, and academic discovery teams • Full Dr. GPCR University Premium access for every team member How Team Membership Works? 1 — Prepare Your Team Gather at least 5 scientists who will participate. Each participant must have a Dr. GPCR Ecosystem account . 2 — Submit Your Team Details Provide names, emails, and organization information so we can activate access correctly. 3 — Complete the Payment Secure your team membership and receive confirmation. 4 — Membership Activation Our team activates all seats and confirms access. Activation typically takes 3–10 business days . Need to add members later? Our team can help expand your membership anytime. Apply for Team Membership First name* Last name* Email* Company name* Company Website* Names & Emails of Each Team Member (minimum 5)* Team Size* Annual Premium Team access. Minimum five seats. Priced per person per year. $2,249.25 Order Now 💡 Have questions? Contact us at Hello@DGPCR.org Terry’s Pharmacology Corner — Created by Dr. Terry Kenakin , powered by Dr. GPCR . Stay connected on LinkedIn and YouTube . Explore : Foundational Lessons — Build Your Pharmacology Core Emerging Drug Hunter — Expand Your Edge Expert-Level Mastery — Advanced Pharmacology Live AMA Sessions with Terry

< Back Your GPCR Order Has Arrived! ❇ Feb 10 - 16, 2025 🚀 GPCR Pals, Get Ready to Elevate Your Expertise! Welcome back to your exclusive GPCR Weekly Newsletter! We’re thrilled to unveil our ever-expanding course roster—designed to help you stay at the cutting edge of GPCR research. New topics, expert-led sessions, and hands-on learning opportunities await! 🎓 Kicking Off Today: Dr. Terry Kenakin ’s hands-on workshop, The Practical Assessment of Signaling Bias . Didn’t sign up? Don’t worry— registrations are NOW OPEN for the 2025 Dr.GPCR University Courses! This is your chance to learn directly from our world-renowned experts. Come back regularly as we are adding courses each month. Email us if you'd like to teach or if you'd like to learn more about any particular topic. 🗓️ Upcoming 4-Week Course: Development of GPCR Ligands as Therapeutic Drugs starting March 20 – April 10, 2025 (Thursdays, 10:00 AM–12:00 PM EST). Watch Dr. Kenakin as he introduces the key concepts of this brand-new course. During these four sessions, you'll dive into: Advanced pharmacokinetic modeling The Druglike Quality of Chemical Entities Drug Absorption 💡 Looking for workshops? We’ve got you covered! ✅ Practical Quantification of Allosteric Modulation – May 1, 2025 ✅ Applying the Black/Leff Operational Model to Predict Agonism – October 2, 2025 Premium Members save 25% on enrollment. Reserve Your Spot Now! 🔗 Register Today . 🔥 Act Fast – Only 25 Spots Available! ⚡ Don’t miss out! Premium Members save 25% on enrollment! Secure your spot today! Highlights of the Week How Ligands Achieve Biased Signaling toward Arrestins Stéphanie Gaillard , Neha Verma , Leisha A Emens , et. al. A combined in silico approach to design peptide ligands with increased receptor-subtype selectivity Adam Zech , Victoria Most , René Staritzbichler , et. al. A2B adenosine receptor-triggered intracellular calcium mobilization: Cell type-dependent involvement of Gi, Gq, Gs proteins and protein kinase C Qin Wang , Wenwen Hao , Jing Li , et. al. Classified GPCR News Let’s dive into the Classified GPCR News from February 10th to 16th, 2025 Industry News Pain targets in ion channel pathways: an Innovation Distillery spotlight ‘It’s not for the faint of heart.’ How 3 CEOs took their biotechs public Aikium's AI-Driven mRNA Engine Looks to Address Undruggable Disordered Proteins Tectonic Therapeutic Secures Massive $185M PIPE Financing for Clinical Programs Septerna Announces Discontinuation of SEP-786 Phase 1 Clinical Trial and Plans to Advance Next-Generation Oral Small Molecule PTH1R Agonist Call for GPCR Papers NEW Special Issue on Adhesion GPCRs GPCR Events, Meetings, and Webinars March 19, 2025 | Advancing obesity drug discovery: Cell-based assays for GLP-1 and the G-Suite March 17 - 21, 2025 | 2nd GPCR signaling and drug discovery Symposium & Workshop NEW April 2 - 3, 2025 | New therapeutic modalities: Transforming receptor pharmacology April 3 - 6, 2025 | ASPET 2025 April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR Annual Meeting 2025 May 12 - 15, 2025 | PEGS 2025 May 15 - 17, 2025 | 23rd GPCR Retreat 2025 May 20 - 22, 2025 | SLAS Europe 2025 NEW May 20 - 22, 2025 |4th GPCRs-Targeted Drug Discovery Summit June 22 - 26, 2025 | G Protein-coupled Receptor Kinases and Arrestins NEW December 16 - 18, 2025 |Pharmacology 2025 July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs Structural Biologist Associate Director/Director, Platform & Hit-ID Chemistry Lead Junior associate position and a PhD/post-doc level position Postdoctoral Position And PhD Position GPCR Molecular Pharmacologist Scientist - Biology Scientist I Cell Biology - Tectonic Therapeutic Senior Principal Scientist, Medicinal Chemistry PhD fellowship in GPCR mechanosensing GPCR Activation and Signaling Lineage-Specific Class-A GPCR Dynamics Reflect Diverse Chemosensory Adaptations in Lophotrochozoa β-arrestin 1 and integrin-linked kinase interact in epidermal keratinocytes and regulate cell motility The regenerative wound healing effects and molecular mechanism of Isaria cicadae Miquel rice fermentation extract A2B adenosine receptor-triggered intracellular calcium mobilization: Cell type-dependent involvement of Gi, Gq, Gs proteins and protein kinase C GPCRs in Cardiology, Endocrinology, and Taste N-homocysteinylation of β-arrestins biases GPCR signaling and promotes platelet activation GPR180 Reduces Adiposity by Inhibiting Lipogenesis and Fatty Acid Uptake in Adipocytes Derivation of hiPSC line (ICADRB2i007-A-3) from an individual with osteoporosis linked to ADRB2: c.46G > A GPCRs in Neuroscience Effects of chemogenetic virus injection and clozapine administration in spinal cord injury GPR37L1 identifies spinal cord astrocytes and protects neuropathic pain after nerve injury Hypothalamic opsin 3 suppresses MC4R signaling and potentiates Kir7.1 to promote food consumption Reviews, GPCRs, and more How Ligands Achieve Biased Signaling toward Arrestins Structural and Molecular Insights into GPCR Function A combined in silico approach to design peptide ligands with increased receptor-subtype selectivity Ligand-Independent Spontaneous Activation of Purinergic P2Y6 Receptor Under Cell Culture Soft Substrate 🔎 GPCR KEYWORDS Class-A G protein-coupled receptors , Lophotrochozoa , echinoderms , Arrestins , ILK , directional migration , epidermis , keratinocytes , scaffold proteins , β-arrestin , Hippo pathway , IMFRE gels , Regenerative healing , Skin repair , Wound healing , A2B adenosine receptor , Calcium , G protein , GPCR , Gi , Gq , Gs , N-homocysteinylation , Adiposity , Fatty Acid Uptake , Lipogenesis , Induced pluripotent stem cells , Osteoporosis , Reprogramming , AAV5-hSyn-hM3Dq-eYFP , Clozapine , DREADDs , Gq signaling pathway , Neuroregeneration , EPSC , GLT-1 , GPR37L1 , SPM , astrocytes , maresin 1 , microglia , nerve injury , neuropathic pain , spinal cord dorsal horn , OPN3 , cAMP signalin g , MC4R , docking , opioid , peptide ligand design , protein design , Ca2+ oscillation , GPCRs , basal activity , purinergic receptor , substrate stiffness < Previous Next >

< Back Fresh, Fresh, GPCR News ❇ Feb 17 - 23, 2025 Hi friends! Welcome to our weekly update! This week's GPCR roll-up includes the latest insights, research discoveries, and advancements. We'll also preview upcoming courses designed for both experienced researchers and newcomers. 🚀 Develop New GPCR Skills Join Dr. Terry Kenakin’s unique course, Development of GPCR Ligands as Therapeutic Drugs , and gain essential insights into: 🔹 Drug Development Basics – PK-PD insights, absorption, and drug properties 🔹 Clearance & Metabolism – Distribution, renal/hepatic pathways, and elimination 🔹 Safety First – Identifying toxicity risks and drug-drug interactions ⏳ Availability is limited. Register now and shape the future of drug discovery! Premium Members enjoy a 25% discount Secure Your Spot Today! Tune in to Ep.160 of the Dr. GPCR Podcast 🎧 Join Remi Janicot as he shares his educational journey, passion for basketball and science, and career decisions. He discusses biased signaling in GPCR research, developing biosensors for G protein activity, networking, mentorship, PhD resilience, COVID-19 challenges, and his aspiration to transition into biotechnology investment opportunities. Highlights of the week Structural insights into prolactin-releasing peptide receptor signaling and G-protein coupling selectivity Zhangsong Wu , Chen Qiu , Geng Chen , et al. Single-Molecule Insights into GPCR Conformational Landscapes Rajan Lamichhane Discovery of CCR8 Antagonist IDOR-1136-5177 for the Treatment of Cancer Stefan Diethelm , Luboš Remeň , Olivier Corminboeuf , et al. Classified GPCR News Let’s dive into the Classified GPCR News from February 17th to 23rd, 2025 Industry News Septerna Announces Discontinuation of SEP-786 Phase 1 Clinical Trial and Plans to Advance Next-Generation Oral Small Molecule PTH1R Agonist Revolutionizing Protein-Ligand Simulations: OpenMMDL's Open-Source Approach The Rapid Push into Radiopharmaceuticals in Oncology and What’s Next Call for GPCR Papers Special Issue on Adhesion GPCRs GPCR Events, Meetings, and Webinars March 19, 2025 | Advancing obesity drug discovery: Cell-based assays for GLP-1 and the G-Suite - Online March 17 - 21, 2025 | 2nd GPCR signaling and drug discovery Symposium & Workshop - Brazil NEW April 1 - 3, 2025 | 2nd Peptide-Based Therapeutics Summit - USA April 2 - 3, 2025 | New therapeutic modalities: Transforming receptor pharmacology - UK April 3 - 6, 2025 | ASPET 2025 - USA NEW April 14 - 17, 2025 | 20th Drug Discovery Chemistry 2025 - USA April 24 - 27, 2025 | American Physiology Summit 2025 - USA April 25 - 30, 2025 | AACR Annual Meeting 2025 - USA NEW May 1 - 2, 2025 | 5th Ace Drug Discovery Summit 2025 - USA NEW May 12 - 15, 2025 | ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025 - USA May 12 - 15, 2025 | PEGS 2025 - USA May 15 - 17, 2025 | 23rd GPCR Retreat 2025 - USA May 20 - 22, 2025 | SLAS Europe 2025 - Germany May 20 - 22, 2025 |4th GPCRs-Targeted Drug Discovery Summit - USA June 22 - 26, 2025 | G Protein-coupled Receptor Kinases and Arrestins - USA December 16 - 18, 2025 |Pharmacology 2025 - UK July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology - Australia GPCR Jobs NEW Open Postdoctoral position - Stanford University Structural Biologist - Confo Therapeutics Associate Director/Director, Platform & Hit-ID Chemistry Lead - Septerna Junior associate position and a PhD/post-doc level position - Eli Lilly and Company Postdoctoral Posit ion And PhD Position - Autonomous University of Barcelona GPCR Molecular Pharmacologist - Schrödinger Scientist - Biology - Superluminal Medicines Scientist I Cell Biology - Tectonic Therapeutic Adhesion GPCRs A force-sensitive adhesion GPCR is required for equilibrioception GPCR Activation and Signaling Extensive location bias of the GPCR-dependent translatome via site-selective activation of mTOR Light intensity-dependent arrestin switching for inactivation of a light-sensitive GPCR, bistable opsin Diapause hormone receptor affects larval growth and embryonic development in the multivoltine strain of Bombyx more Profiling Allosteric Modulators of CB1R with an Allosteric Fluoroprobe GPCRs in Cardiology, Endocrinology, and Taste Immunolocalization and quantification of the phoenixin and GPR173 in the gastrointestinal tract of Holstein-Friesian bulls Derivation of hiPSC line (ICADRB2i007-A-3) from an individual with osteoporosis linked to ADRB2: c.46G > A GPCRs in Neuroscience Cortical astrocyte activation triggers meningeal nociception and migraine-like pain GPCRs in Oncology and Immunology Spatial analysis of a complete DIPG-infiltrated brainstem reveals novel ligand-receptor mediators of tumour-to-TME crosstalk Discovery of CCR8 Antagonist IDOR-1136-5177 for the Treatment of Cancer The extracellular matrix protein type I collagen and fibronectin are regulated by β-arrestin-1/endothelin axis in human ovarian fibroblasts Methods & Updates in GPCR Research Histamine-modulated wettability switching in G-protein-coupled receptor inspired nanochannel for potential drug screening and biosensing Reviews, GPCRs, and more Single-Molecule Insights into GPCR Conformational Landscapes Covalent functionalization of G protein-coupled receptors by small molecular probes A deadly taste: linking bitter taste receptors and apoptosis Molecular roles in membrane receptor signaling pathways and cascade reactions in chondrocytes: a review Is GCR1 the GPR157 of plants? Structural and Molecular Insights into GPCR Function Structural insights into prolactin-releasing peptide receptor signaling and G-protein coupling selectivity Decoding the structural basis of ligand recognition and biased signaling in the motilin receptor 🔎 GPCR KEYWORDS GPCR , structural biology , biased signaling , metabolism , Chondrocytes , Signaling pathway , Integrin , Taste family 2 receptors , Calcium , Cell death , Mitochondria , macrolide antibiotics , motilin receptor , azithromycin , Extraoral taste receptors . < Previous Next >

Discover top GPCR Courses for your educational journey. Explore a curated list of GPCR Courses to enhance your knowledge and career. Stay at the Forefront of GPCR Drug Discovery Gain insider methods from the pioneers shaping biased signaling, assay design, and pharmacology—skills you won't find in any textbook or paper. ⧖ 20+ Hours of Expert Training ↓ Downloadable Resources ◕ New Courses added Quarterly Get Access to GPCR Courses Learn in 3 Simple Steps Free trailers coming soon Preview every masterclass before joining Unlock full access Get Premium for complete library access Learn anytime, anywhere Access on-demand from any device Join Premium Today Unlock Insider Access to GPCR Science! Free updates, exclusive previews, and highlights from our Masterclasses and Vault. First name Last name Email* Join Our Mailing List Count me in! * Explore the Masterclasses Trailers are free. Full classes require Premium. Filter by Category Filter by Level Filter by Instructor Watch Now INSTRUCTOR Heading 5 I'm a paragraph. Click here to add your own text and edit me. It's easy. Read More INSTRUCTOR Heading 5 I'm a paragraph. Click here to add your own text and edit me. It's easy. Read More INSTRUCTOR Heading 5 I'm a paragraph. Click here to add your own text and edit me. It's easy. 1 2 3 4 5 1 ... 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 65 66 67 68 69 70 71 72 73 74 75 76 77 78 79 80 81 82 83 84 85 86 87 88 89 90 91 92 93 94 95 96 97 98 99 100 ... 100 Learn directly from world leaders in GPCR research Access exclusive training from the scientists shaping the future of GPCR drug discovery Dr. Terry Kenakin Terry's Corner Author of 'A Pharmacology Primer', the definitive GPCR reference used by labs worldwide. Former GSK principal research investigator with 40+ years of industry experience. Dr. Sam Hoare Pharmechanics GPCR signaling & biased agonism expert regularly consulted by top pharma companies for assay design strategies. Pioneer in quantitative pharmacology methods. Dr. Yamina Berchiche Dr. GPCR Community builder for scientists with expertise in GPCR project strategy and translational applications. Unlock All 20+ GPCR Masterclasses – Save 95% Individual courses cost $300–600 each. With Premium, you get everything for just $249.99/year (less than $1/day). 20+ Hours of GPCR Masterclasses Downloadable Resources & Q&A Replays Weekly GPCR Insights (papers, jobs, events) Networking with a global scientist community One failed assay can cost $10,000+ in reagents and months of time. Think of Premium as insurance against wasted experiments and failed drug leads. Best Value Premium Yearly $249.99 $ 249.99 Every year 🚀 Everything you need to master GPCR science — in one membership. Valid until canceled Join Premium Now 🎓 Full GPCR University + 🔬 200+ expert talks 🗞️ Weekly research, careers & event intelligence 🤝 Members-only networking, AMAs & matchmaking 💡 Support open resources for the global GPCR field 🧠 Designed for researchers at every career stage 🚀 Don’t just keep up — lead the way. What Scientists Are Saying Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere Anonymous 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 Anonymous The content had enough depth to satisfy the hunger for theory while being full of practical knowledge Anonymous 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 Anonymous Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him Anonymous 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. Anonymous What are the benefits of becoming a member of Dr.GPCR? As a member, you can access: Dr.GPCR Podcast videos Live GPCR events Weekly classified GPCR news Contributor articles As a premium member, you can access all the free features plus: GPCR courses with a 25% discount Private groups 30+ Symposia recorded talks GPCR Job listings GPCR Event listings Direct access to members of the GPCR community How do I sign up for a membership? To sign up, click the 'Log In/Sign Up' button at the top of the homepage and fill out the registration form. Once your registration is complete, you will receive a confirmation email. Why do I need to fill out a form and wait for approval? We carefully screen anyone signing up to the Ecosystem to ensure they are real humans working on GPCRs. We want to keep our community exclusive to the field, so we need as much information as possible to verify your identity. How long will the Sign-Up process take? We could take up to two (2) business days. I’m just a student starting in the field. Can I sign up to the Ecosystem? Yes, everyone interested in the field is welcome to join. Please let us know about this while filling out the registration form. Why are personnel from US governmental agencies excluded from the free membership? Employees of any branch or department within the US government are not eligible for the free membership. Verification methods can vary but might require a work email address, an official ID, or other employment documentation during the sign-up process to confirm whether the individual is employed by a US governmental agency. If there's any uncertainty about eligibility, the best action is to contact us at hello@drgpcr.com. How much does the premium membership cost? The premium membership is priced at $249.99 per year. We have a 90% discount for people who live and work in developing countries and a 15% discount for team memberships, a minimum of 5 seats. You can also access a 25% discount on our Dr.GPCR University courses as a premium member. 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The Practical Assessment of Signaling Bias Dr. Terry Kenakin < Back Workshop Summary Join Dr. Terry Kenakin , a leading expert in pharmacology, as he unpacks the fascinating world of signaling bias in drug development! 🚀 This workshop will explore how different ligands (compounds) can stabilize unique receptor conformations, leading to distinct signaling outcomes—even when binding to the same receptor. Dr. Kenakin will explain that bias is not an exception but a fundamental principle of pharmacology, occurring whether or not researchers actively seek it. Through an engaging discussion, you'll explore: 🔹 What signaling bias is and why it matters 🔹 How receptor dynamics shape drug responses 🔹 Cutting-edge methods for quantifying bias 📊 🔹 Strategies to harness bias for better drug design —maximizing efficacy while minimizing side effects The session wraps up with a lively Q&A , allowing attendees to explore this game-changing topic in greater depth. Don't miss this opportunity to refine your understanding of bias as a tool, not an obstacle, in pharmacology! Key Highlights 🔍 Bias is Everywhere : Signaling bias naturally occurs in pharmacology—whether we look for it or not! 🧬 Receptor Flexibility : Ligands stabilize different receptor states, creating unique signaling pathways. 📏 Measuring Bias : New techniques allow us to quantify bias and compare drug efficacy more precisely. 💊 Therapeutic Potential : Understanding bias enables researchers to design drugs that target specific effects while avoiding unwanted side effects. 🗣️ Interactive Q&A : The discussion wraps up with an insightful Q&A, tackling real-world drug development challenges. Deep Dives & Insights 📌 Bias is Not an Anomaly—It’s a Feature! 🔹 Instead of avoiding bias, researchers can embrace it to refine drug responses. Dr. Kenakin challenges the traditional approach and encourages leveraging bias for better therapeutic outcomes. 📌 Receptors are Dynamic Players 🔹 Different ligands trigger unique receptor states, meaning the same receptor can signal in entirely different ways depending on what binds to it. Understanding these shifts can revolutionize drug development! 📌 Measuring Bias: A Quantitative Approach 🔹 The operational model provides a structured way to measure bias, combining affinity and efficacy. This allows for a side-by-side comparison of how different compounds influence receptor signaling. 📌 Bridging the Gap: Lab to Clinic 🔹 While measuring bias in a lab is relatively straightforward, translating these findings to clinical applications remains a challenge . The talk explores how to navigate this crucial gap. 📌 The Future of Drug Development 🚀 🔹 By integrating bias into drug design , researchers can craft more selective, effective, and safer therapies. This approach is shaping the next generation of precision medicine! Dr. Terry Kenakin’s workshop offers a fresh perspective on drug discovery . It shows that bias isn’t something to avoid—it’s something to utilize ! Whether you're a researcher, student, or industry professional, this session is packed with insights that will make you rethink your approach to pharmacology . Ready to explore the future of biased drug design? Let’s dive in! 🔬✨ AI Summary - May contain inaccuracies Materials: BIAS_WORKSHOP_PRINT .pdf Download PDF • 9.11MB BIAS_EXERCISE .pdf Download PDF • 721KB What would you like to learn today?

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