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<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Shivani Sachdev About Dr. Shivani Sachdev "Dr. Sachdev is an early career researcher in the National Institute of Diabetes and Digestive and Kidney Diseases at the National Institutes of Health. Her research centers on developing nanobody-ligand conjugates to target GPCRs, with a focus on receptors relevant for treating osteoporosis, diabetes, and pain. She received her undergraduate degree in Biotechnology from KIIT University in India. She subsequently joined Professor Mark Connor's laboratory at Macquarie University in Australia. Dr. Sachdev pursued Ph.D. in the same lab where she investigated the molecular pharmacology of cannabinoid receptors. She is also very active within the pharmacology community and currently serves on the editorial board of the British Journal of Pharmacology. Given her expertise in GPCR pharmacology and scientific communication, she is poised to make valuable contributions to the field and expand our understanding of GPCR signaling." Dr. Shivani Sachdev on the web NIDDK ReseachGate Google Scholar LinkedIn Twitter Dr. GPCR 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Paul Insel About this episode In 1975, Dr. Paul Insel was at the FASEB experimental biology meeting in Atlantic City. During dinner with colleagues and Alfred Gillman , co-recipient of the 1994 Nobel Prize in Physiology or Medicine for their discovery of G-proteins and their role in signal transduction in cells, Paul was designated to go to Gillman’s lab . That summer, he used radioligand binding methods to dissect receptor function from the adenylyl cyclase activated by ligands, including adrenaline. From that point on, Paul was hooked and has since studied receptor function in human physiology, receptor molecular pharmacology in cells, and animal models, and as he puts it has now he’s "gone full circle" back to studying GPCRs important in human pathophysiology. Today, Paul and his team focus on previously unrecognized receptors with the hopes to use these as novel drug targets. Dr. Paul Insel on the web Insel Laboratory Institute of Engineering in Medicine UC San Diego UCSD Profiles Google PubMed Dr. GPCR Ecosystem 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 4 Date & Time Friday, November 3rd / 3:00 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Home → Flash News → How does a superagonist activate M2 muscarinic receptors? New simulations reveal the conformational changes from inactive to active states to highlighting how ligand dynamics drive GPCR activation! Catch the full story in the Ecosystem! https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/visualizing-agonist-induced-m2-receptor-activation-regulated-by-aromatic-ring-dynamics #GPCR #drGPCR #M2R #drugdiscovery #moleculardynamics Published on March 31, 2025 Category GPCR Weekly News How does a superagonist activate M2 muscarinic receptors? New simulations reveal the conformational changes from inactive to active states to highlighting how ligand dynamics drive GPCR activation! Catch the full story in the Ecosystem! https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/visualizing-agonist-induced-m2-receptor-activation-regulated-by-aromatic-ring-dynamics #GPCR #drGPCR #M2R #drugdiscovery #moleculardynamics Previous Next Recent Articles

Home → Flash News → 📢 All 2025 Dr.GPCR Courses Are Open for Registration! Which one will you choose? 🚀 Whether you're diving into GPCR drug discovery, pharmacology, or advanced modeling, there's a course for you. 💡 Bonus: Premium Members enjoy 25% off on all courses! 🔗 Explore & register today: https://www.ecosystem.drgpcr.com/gpcr-courses #GPCR #DrGPCR #Biotech #DrugDiscovery #Pharmacology Published on March 4, 2025 Category GPCR Weekly News 📢 All 2025 Dr.GPCR Courses Are Open for Registration! Which one will you choose? 🚀 Whether you're diving into GPCR drug discovery, pharmacology, or advanced modeling, there's a course for you. 💡 Bonus: Premium Members enjoy 25% off on all courses! 🔗 Explore & register today: https://www.ecosystem.drgpcr.com/gpcr-courses #GPCR #DrGPCR #Biotech #DrugDiscovery #Pharmacology Previous Next Recent Articles

Pharmacology moves fast. Adaptive thinking—not just tools—keeps you in the game. Join Terry’s Corner for real-world insights from Terry Kenakin. Home → Flash News → ama session sept 18 post 3 “Technologies come and go. If that’s all you know, you’ll be out of the game fast.” Published on October 30, 2025 Category Terry's Corner “Technologies come and go. If that’s all you know, you’ll be out of the game fast.” In our AMA, Terry Kenakin shared timeless career advice for young pharmacologists navigating a fast-changing field: “Try to keep a finger on the pulse of as much as you can… that was one of the main reasons for doing Terry’s Corner. New ideas come up, and if we can encapsulate them and expose them, you can just hit a button, hear about it, and pursue it.” To stay relevant in the next decade, it’s not about chasing the latest assay or tool. It’s about building adaptive thinking—knowing where the field is moving and being ready to pivot with it. That’s what Terry’s Corner was built for: a space to turn decades of industry experience into short, targeted insights that keep you ahead of the curve. 🟢 Join Terry’s Corner → https://www.ecosystem.drgpcr.com/terry-corner ✳️ Next AMA Session: ⚠️ Today, Oct 30 | 12–1 PM EST #GPCR #DrGPCR #Pharmacology #DrugDiscovery #CareerDevelopment #Biotech #Mentorship #EarlyDiscovery #ScientificLeadership Previous Next Recent Articles

Home → Flash News → 🔍 Running a GPCR lab? Applying for grants? Launching a nonprofit? Ep.165 of the Dr.GPCR Podcast is your finance + operations crash course—delivered by two experts who support early-stage mission-driven teams like Dr. GPCR. 🎧 Smart, practical, and full of real talk: Ep 165 with Chuck DeWeese & Joe St. Germain #gpcr #DrGPCR #ScienceStartup Published on May 15, 2025 Category Dr. GPCR Podcast 🔍 Running a GPCR lab? Applying for grants? Launching a nonprofit?Ep.165 of the Dr.GPCR Podcast is your finance + operations crash course—delivered by two experts who support early-stage mission-driven teams like Dr. GPCR. 🎧 Smart, practical, and full of real talk: Ep 165 with Chuck DeWeese & Joe St. Germain #gpcr #DrGPCR #ScienceStartup Previous Next Recent Articles

Home → Flash News → A high-resolution deep mutational scan of MC4R reveals how thousands of genetic variants impact obesity-linked signaling pathways and highlights new opportunities for precision drug discovery Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/high-resolution-deep-mutational-scanning-of-the-melanocortin-4-receptor-enables-target-characterization-for-drug-discovery #gpcr#drgpcr Published on May 5, 2025 Category GPCR Weekly News A high-resolution deep mutational scan of MC4R reveals how thousands of genetic variants impact obesity-linked signaling pathways and highlights new opportunities for precision drug discovery Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/high-resolution-deep-mutational-scanning-of-the-melanocortin-4-receptor-enables-target-characterization-for-drug-discovery #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → Disrupting VIPR2 dimerisation halts breast cancer spread—could TM3-4 peptides be the next breakthrough in targeted cancer therapy? Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/gpcrs-in-oncology-and-immunology/dimerisation-of-the-vip-receptor-vipr2-is-essential-to-its-binding-vip-and-g%CE%B1i-proteins%2C-and-to-its-functions-in-breast-cancer-cells #gpcr#drgpcr Published on May 12, 2025 Category GPCR Weekly News Disrupting VIPR2 dimerisation halts breast cancer spread—could TM3-4 peptides be the next breakthrough in targeted cancer therapy? Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/gpcrs-in-oncology-and-immunology/dimerisation-of-the-vip-receptor-vipr2-is-essential-to-its-binding-vip-and-g%CE%B1i-proteins%2C-and-to-its-functions-in-breast-cancer-cells #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → Check out our #SpotifyWrapped 🚀! In 2024, Dr. GPCR reached listeners worldwide, sparking conversations about GPCRs with top experts. Thank you for tuning in! 📊🎙️ ✳️Check out our top episode: https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ep-148-with-dr-arthur-christopoulos #gpcr #drgpcr Published on January 29, 2025 Category Check out our #SpotifyWrapped 🚀! In 2024, Dr. GPCR reached listeners worldwide, sparking conversations about GPCRs with top experts. Thank you for tuning in! 📊🎙️ ✳️Check out our top episode: https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ep-148-with-dr-arthur-christopoulos #gpcr #drgpcr Previous Next Recent Articles

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Leave for dinner reception Coming Soon < Previous Session Next Session >

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Juan José Fung About Dr. Juan José Fung Dr. Juan José Fung is a Principal Scientist at GPCR Therapeutics, Inc , a drug discovery company focused on targeting GPCR heteromers in cancer, headquartered in Seoul, Korea, with an R&D facility in the SF Bay Area. Dr. Fung received his Ph.D. from the Stanford University School of Medicine under the mentorship of Dr. Brian Kobilka , studying the dimerization of GPCRs. Dr. Fung continued his Postdoctoral training in Dr. Kobilka’s lab contributing to the elucidation of high-resolution structures of various GPCRs. Dr. Fung has spent significant time in the industry studying membrane proteins, antibodies, and HTS methods for drug discovery. His current work is mainly focused on screening and assay development to bridge the gap between in vitro and in vivo GPCR pharmacology. Dr. Juan José Fung on the web LinkedIn GPCR Therapeutics Dr. GPCR Ecosystem 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Brian Shoichet About Dr. Brian Shoichet BSc in Chemistry from MIT, Ph.D. with Tack Kuntz at UCSF; Postdoc with Brian Matthews in protein stability-activity tradeoffs, crystallography; started my independent lab at Northwestern University Medical School (1996) was recruited back to UCSF in 2003. Dr. Brian Shoichet on the web Google Scholar Shoichet Lab Twitter Dr. GPCR Ecosystem 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

GPCR scientist Ben Clements shares how positive allosteric modulators could transform opioid therapy by boosting efficacy and reducing side effects. << Back to podcast list Dr. GPCR Podcast Strategic Partners When to Walk, When to Run: Lessons from the GPCR Trenches with Dr. Ben Clements 1. The Power of Inclusion in the GPCR Field This episode kicks off with a celebration of early-career scientists. Host Dr. Yamina Berchiche emphasizes the importance of diverse voices in the GPCR community: “It’s been a very difficult path to get more early-career scientists on the podcast. But it’s important to make your voice heard.” Benjamin Clements , a postdoctoral fellow at the University of Michigan, joins the conversation as a rising voice in GPCR pharmacology. His journey highlights the transition from general drug development to a deep dive into G protein-coupled receptors. 2. From Aspirations to Application: Ben’s Path into Science Ben shares his winding yet deliberate entry into science. Initially driven by a general passion for biology and a childhood dream of being an astronaut, he began with intestinal choline transport research at UNC. The realization that basic science could impact real patients was transformative. “It’s not just raw science — this can help someone at the end of the day.” – Ben Clements His pivot into neuroscience and pharmacology during grad school at the University of Minnesota laid the groundwork for his current work in GPCR pharmacology. 3. GPCRs and the Opioid Crisis: A New Pharmacological Frontier Now at the University of Michigan, Ben focuses on positive allosteric modulators (PAMs) targeting opioid receptors. The goal: maximize analgesia while minimizing side effects . “We’re enhancing the powerful pain-relieving effects of opioids while limiting respiratory depression, constipation, and abuse liability.” He is particularly excited by the novel application of PAMs in chronic and neuropathic pain models , including the neuroma model , which is typically opioid-insensitive. 4. Allosteric Modulation: The New Frontier of GPCR Drug Discovery Ben reflects on the emerging potential of allosteric modulation in GPCRs — a field that has lagged behind ion channels in clinical applications. “Allosteric modulation in GPCRs is so novel and so exciting. There’s so much availability, so much we don’t know yet.” By working with distinct chemical scaffolds like thiazolidines and xanthinediones, Ben is helping define how structurally different PAMs may act on similar receptor sites. 5. Scientific Rigor: The Value of ‘Old School’ Pharmacology Despite the availability of modern tools, Ben stresses the enduring value of classical methods like GTPγS assays , radioligand binding , and basic PK/PD models . “It doesn’t matter how many cool, fun tools you have. If you don’t understand the math that underlies an allosteric modulator, you won’t understand what’s happening.” This mindset keeps his science grounded, reproducible, and rooted in fundamentals. 6. Mentorship, Team Culture, and the Joy of Science Science is serious work, but Ben believes fun and collaboration fuel great outcomes. At Michigan, his lab balances rigor with light-hearted engagement — like daily squirrel trivia on their whiteboard. “Science is fun. We produce great data, but we also joke around. That’s how we work best.” Strong mentorship, open communication, and peer learning — especially from undergraduate trainees — shape his development as both a scientist and future educator. 7. Translating Discovery into Therapy: Bench to Bedside Vision Ben’s work seeks to merge in vitro mechanistic data with in vivo efficacy , guiding medicinal chemists toward creating druggable PAMs . “The goal is to smash all the amazing biology together and make a drug.” Using site-directed mutagenesis and pharmacological synergy assays , his team aims to understand how and where these compounds interact with the receptor, paving the way for structure-based drug design . 8. Structural Biology Roadblocks: The Cryo-EM Challenge One bottleneck in Ben’s work is visualizing binding sites of PAMs via cryo-EM , due to low compound potency and membrane-embedded binding pockets. “Our compounds don’t bind well enough to be seen clearly. That’s a real challenge with allosterics.” Still, by collaborating with structural biology teams and combining cryo-EM with NMR , his lab is narrowing down potential binding regions. 9. Lessons in Confidence, Collaboration, and Aha Moments From asserting himself as an undergrad to mastering unique techniques in grad school, Ben has accumulated key “aha” moments that shaped his confidence: Standing up to big names when safety was compromised. Realizing his technical skills were indispensable to the team. Discovering breakthrough results in neuroma pain models via a spontaneous collaboration. “We found something incredible — a tenfold shift in the methadone dose-response with our PAM.” 10. Advice for Junior Scientists: Read, Rest, Run Ben closes with wisdom for early-career researchers: “Academia is about knowing when to walk and when to run.” – Advice from Kelsey Flepsen He advocates: Reading one paper a day. Taking care of yourself when possible. Pushing hard when deadlines or breakthroughs demand it. “Your brain’s not a machine. Let it rest. That’s when the best ideas come — in the shower or on a walk.” Summary made with AI ________ Key Takeaway Episode 166 with Ben Clements is a deep dive into the pharmacological potential of GPCRs , the power of mentorship, and the mindset required to thrive in science. With clarity, curiosity, and a collaborative spirit, Ben reminds us that impactful science isn’t just about technology — it’s about people, persistence, and timing. “Science is all about knowing when to walk and knowing when to run.” Keyword Cloud GPCR research community , Dr. GPCR ecosystem , GPCR online course , GPCR scientist network , GPCR drug discovery , GPCR training program , G protein-coupled receptors , GPCR podcast , GPCR webinar series , GPCR data platform Summary created by AI About Ben Clements Dr. Ben M Clements is a behavioral pharmacologist who uses in vitro and in vivo models to discover and characterize novel treatments for chronic pain and opioid use disorder. He received his Ph.D. in Pharmaceutics from the University of Minnesota in 2022, studying the pharmacokinetics and pharmacodynamics of NMDA receptor antagonists. At the University of Michigan, Ben focuses on determining the mechanisms of action of a series of positive allosteric modulators of the mu-opioid receptor. This project involves molecular pharmacology in cell models to determine binding sites and mechanisms of allostery, as well as efficacy studies in mouse and rat models of acute and chronic pain. Dr. Clements' work is primarily focused on translational developments of small molecule therapeutics, and intends to apply these ideas to an independent academic laboratory. In addition, he plans to continue studying how neuromodulators, both exogenous and endogenous, can influence cellular activity, physiological behaviors, and human health. Ben Clements on the web University of Michigan X Google Scholar LinkedIn 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Discover how GPR65 reshapes our understanding of GPCR signaling and its role in cancer, with Dr. Ian Chronis on the Dr. GPCR podcast. << Back to podcast list Dr. GPCR Podcast Strategic Partners Signals, pH, and Discovery : Cracking GPCR Mysteries with Dr. Ian Chronis In this episode, we welcome Dr. Ian Chronis, a recent Ph.D. graduate preparing to begin his postdoctoral work at the University of Michigan. Host Yamina Berchiche sets a welcoming tone as they dive into Ian’s unique academic journey—from early interests in medicine to his pivot toward pharmacology and GPCR research. His story offers valuable insights for anyone navigating the path from student to scientist. Ian discusses how his experiences at the University of Chicago and the University of Michigan shaped his scientific curiosity, particularly around G protein-coupled receptors (GPCRs) . His research centers on the beta-2 adrenergic receptor and GPR65 , a proton-sensing receptor with promising implications in cancer biology. He shares fascinating findings from his work on GPR65 , highlighting its unusual constitutive internalization and its ability to signal from acidic endosomes. This dual functionality—environmental sensing and compartment-specific signaling—offers a new layer of complexity in GPCR behavior. Yamina underscores the therapeutic potential of GPR65, especially in the context of cancer immunotherapy, and how understanding receptor activity in acidic microenvironments could unlock new therapeutic strategies. Throughout the episode, Ian reflects on the value of a supportive lab culture , the need for better experimental tools in GPCR signaling , and the importance of engaging with the broader GPCR research community to drive innovation. The conversation wraps with a playful exchange about possible podcast titles, with Yamina suggesting "Ancient Greek Chemistry and GPCRs"—a nod to Ian’s heritage and the wide-ranging themes covered. This episode is both educational and inspiring, offering a behind-the-scenes look at a rising scientist’s journey in the ever-evolving world of GPCR research. Summary created by AI About Ian Chronis I recently finished my PhD in the lab of Dr. Manoj Puthenveedu at the University of Michigan, where I am now working as a postdoc. My research has looked at the trafficking and signaling of adrenergic and proton-sensing receptors, with specific focus on identifying novel regulatory proteins governing their function. Ian Chronis on the web LinkedIn 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Timo De Groof About Dr. Timo De Groof Dr. Timo De Groof studied Biochemistry and Biotechnology at the University of Ghent where he graduated in 2015. During his master's studies, he specialized in Biomedical Biotechnology and Structural Biology/Biochemistry. During his last year of studies, Timo performed research in the biopharmaceutical company Argen X and gained experience in the identification and characterization of llama-derived antibodies in inflammatory diseases and oncology. From 2015 to 2019, he completed his Ph.D. in the Medicinal Chemistry group at VU University Amsterdam under the supervision of Prof. Dr. Martine Smit . During his Ph.D., Timo, together with Dr. Raimond Heukers , developed a nanobody platform within the research group and used this platform to develop nanobodies targeting viral G protein-coupled receptors with a special focus on the human cytomegalovirus-encoded chemokine receptor US28. During his Ph.D., he used these nanobodies as research tools, to investigate different GPCR conformations, while also focusing on their therapeutic potential in oncology and transplant infectious disease. Starting from September 2019, Timo started working as a postdoctoral researcher at the Vrije Universiteit Brussel in the In Vivo Cellular and Molecular Imaging (ICMI) group that is focused on translational/clinical applications of nanobodies. He currently is focusing on the development of nanobody-based immuno tracers as part of the IMI/EFPIA project entitled "Immune Image". Moreover, he is closely involved in multiple projects where he focuses on the generation of nanobodies against "difficult-to-target" proteins. In the near future, Timo hopes to combine his previous GPCR experience with his current focus to set up his own research line focusing on translational applications of GPCR-targeting nanobodies. Dr. Timo De Groof on the web LinkedIn Researchgate Twitter Medical Imaging Group Google Scholar Dr. GPCR Ecosystem 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Yamina Berchiche About this episode In this Episode 0 of the brand new Dr. GPCR podcast , your host and founder, Dr. Yamina Berchiche introduces the very first podcast dedicated to GPCRs researcher and their work. This podcast is part of the Dr. GPCR Ecosystem, with the goal is to bring together GPCR scientists, biotech, and pharma leaders as well as suppliers working on GPCRs by providing opportunities to connect, share, form trusting partnerships, grow, and thrive together to accelerate GPCR drug discovery and improve human health. Dr. Yamina Berchiche on the web - Website - LinkedIn - PubMed - Twitter - Facebook - Dr. GPCR Ecosystem 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Irfan Dhanidina, Dr. Kathleen Caron and Dr. Lauren Slosky About Irfan Dhanidina "My interest in oncology research led me to pursue a BSc in Biology & Economics from Carleton University, and an MSc in Biotechnology at McGill. However, after insightful experiences in academic, hospital, and industry labs, I decided to pursue a role in business development. In my role at Orion Biotechnology, I work at the intersection of science and business, which includes target selection, preclinical strategy and business development. With respect to GPCRs, I'm particularly interested in peptide/small protein receptors and the mechanisms that facilitate their role in various indications. To that end, I'm grateful to be working alongside the very talented team at Orion who translate important GPCR research into novel therapies for patients. " Irfan Dhanidina on the web LinkedIn The Org DIBIZ Dr. GPCR About Dr. Kathleen Caron " "Kathleen M. Caron, Ph.D. is the Frederik L. Eldridge Distinguished Professor and Chair of the Department of Cell Biology & Physiology at The University of North Carolina at Chapel Hill—a large, interdisciplinary basic science department consistently ranked in the Top 5 in the Nation in NIH funding. Dr. Caron received a BS in Biology and BA in Philosophy at Emory University and a PhD at Duke University while training with Dr. Keith Parker to elucidate the role of steroidogenesis in regulating sexual determination and adrenal and gonadal development using genetic mouse models. She pursued postdoctoral training with Nobel Laureate Dr. Oliver Smithies at UNC-CH, where she was the first to discover the essential role of adrenomedullin peptide for embryonic survival. With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular biology, the Caron laboratory has gained valuable insights into the genetic basis and pathophysiology of lymphatic vascular disease, preeclampsia and sex-dependent cardiovascular disease. Dr. Caron has received numerous awards including a Burroughs Wellcome Fund Career Award in the Biomedical Sciences, an Established Investigator Award and an Innovator Award from the American Heart Association, a Jefferson Pilot Award in Biomedical Sciences and a UNC-CH Mentoring Award. She currently serves as Associate Editor of Physiological Reviews; the #1 ranked journal in Physiology (IF 46.5). Dr. Caron is also past Associate Editor at JCI and served as the inaugural Associate Editor at ACS-Pharmacology and Translational Science. Dr. Caron currently holds multiple scientific advisory roles in academia, industry and the National Institutes of Health." " Dr. Kathleen Caron on the web UNC-Chapel Hill Department of Cell Biology and Physiology UNC Lineberger Comprehensive Cancer Center Twitter Google Scholar ORCID ResearchGate Dr. GPCR About Dr. Lauren Slosky "Lauren Slosky is an Assistant Professor in the Department of Pharmacology and a member of the Medical Discovery Team on Addiction, a multidisciplinary initiative within the University of Minnesota’s Medical School to advance research and treatment in the field of drug addiction. Dr. Slosky’s research is focused on understanding how neuropeptide G protein-coupled receptors (GPCRs) regulate motivated behavior and how these receptors can be targeted for therapeutic benefit. Dr. Slosky was awarded a B.S. with honors in Molecular and Cellular Biology and Psychology from The University of Arizona in 2011. She received a Ph.D. in Medical Pharmacology from The University of Arizona in 2015 and completed a postdoctoral fellowship in the laboratory of Dr. Marc G. Caron at Duke University. Dr. Slosky opened her laboratory at the University of Minnesota Medical School in 2021. While a postdoctoral fellow, Dr. Slosky characterized a new class of β-arrestin biased allosteric modulators (BAMs) for the neurotensin receptor 1. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling. Critically, these ligands reduce addiction-associated behaviors in animal models without the side effects characteristic of balanced receptor activation. Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor signaling, they are exciting tools for linking distinct signaling pathways with their physiological effects and may serve as the basis for more selective therapeutics. This work was made possible by the optimization of longitudinal intravenous self-administration paradigms for genetically modified mice. Integrating GPCR biology, behavioral pharmacology, and systems neuroscience approaches, the Slosky Lab is now working to understand how the principles of receptor allosterism and functional selectivity can be leveraged in the development of safe and effective treatments for stimulant and opioid use disorders. Dr. Slosky’s work has been recognized through several travel and research awards, including the William James Psychology Award, the Hank Yamamura Endowed Fellowship in Pharmacology, an NIH F32 Postdoctoral Fellowship, and an NIH K99/R00 Pathway to Independence Award. In addition to research, Dr. Slosky is passionate about training the next generation of scientists and increasing diversity, equity, and inclusion in science. An advocate for trainees at all levels, she served as Service Chairperson and Interim President of the Duke University Postdoctoral Association. She is currently a faculty trainer for the University of Minnesota's MS and Ph.D. programs in Pharmacology, Graduate Program in Neuroscience, and Life Sciences Summer Undergraduate Research Program and is working to build relationships with key stakeholders through institutional and community service." Dr. Lauren Slosky on the web University of Minnesota Department Page Twitter LinkedIn Google Scholar PubMed Research Gate Dr. GPCR 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Principles of Pharmacology in Drug Discovery II Dr. Terry Kenakin Get Started Premium Members benefits: - Subscribe and save 25% on every GPCR Course - Early-bird access - Recordings will be available < Back to GPCR courses Watch recording Your Instructor Dr. Terry Kenakin

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Genetic Deletion of Atypical VGLUT3 Rescues Huntington’s Disease Phenotype and Neurodegeneration in zQ175 Mice Date & Time Friday, November 3rd / 2:10 PM About Karim Ibrahim "A postdoctoral researcher, interested in studying G-protein coupled receptors and their role in neurodegenerative disorders, including Alzheimer's and Huntington's diseases." Karim Ibrahim on the web X (Twitter) Google Scholar Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Illuminating Functional Selectivity and Allosterism at GPCRs. Date & Time Saturday, November 4th / 11:30 AM Abstract Coming Soon About Stéphane Laporte "Dr. Stéphane Laporte is a Professor of Medicine, and the Director of Research of the Division of Endocrinology and Metabolism at McGill University. He is also an Associate Leader of the Experimental Therapeutics and Metabolism Program and the Director of the Molecular Imaging Platform at the Research Institute of the McGill University Health Centre (RI-MUHC). He is a member of the Executive Committee of the Réseau québécois de recherche sur les médicaments. He has received many awards, including a Canada Research Chair, FRSQ scholarships and the CDA/CSEM/Merck Frosst Young Investigator award. His expertise is in molecular pharmacology and his research program focuses on the molecular and cellular mechanisms regulating G protein-coupled receptor (GPCR) responses, a class of receptors involved in many, if not all, physiological responses, with the ultimate goal of improving drug action. He has developed innovative methods for in-cellulo measurement of protein-protein interactions, receptor trafficking and signalling, useful for drug discovery programs. His research program also studies the allosteric, biased signalling regulation of GPCR and has contributed to the validation of small molecules that block myometrial contraction in pre-term birth. He has contributed to the generation of many intellectual property agreements and patents, and published his findings in high-impact journals. The Canadian Institutes for Health Research and March of Dimes currently support his research." Stéphane Laporte on the web Laporte Lab McGill University LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VII Physiological and pathological roles of AGPCRs in the nervous system Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Beatriz Blanco Redondo The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Willem Berend Post Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Beatriz Blanco Redondo Abstract "The Drosophila genome contains five loci encoding adhesion G-protein coupled receptors (aGPCRs). Phylogenetic analysis revealed that the remoulade (remo) gene is a homologue of the vertebrate aGPCR ADGRA family, sharing the same overall receptor domain structure. In vivo expression profiling has shown Remo expression in the central (CNS) and peripheral nervous systems (PNS) of third-instar larvae (L3) and adults. In L3 PNS specimen Remo is expressed in a subset of neurons expressing the DEG/ENaC channel pickpocket (PPK), which is involved in transduction of sensory information like nociception. remoKO larvae and animals, in which remo was knocked down in ppk-neurons through RNA interference, show a higher nocifensive response compared to wildtype remorescue controls indicating that remo is required in PPK-neurons for this behaviour. Furthermore, with the aim to analyse the biochemical properties of Remo, we performed immunoprecipitation analysis. We found that the receptor is cleaved despite the lack of a consensus GPS sequence. Hence, Remo is proteolytically processed, either by the GAIN domain or an alternative protease that cleaved Remo near the GPS. We also aimed at identifying the signaling pathway that Remo is involved in. The mammalian Remo homolog ADGRA2/Gpr124 cooperates with other GPCRs of the Frizzled family, and the transmembrane proteins RECK and Lrp5/6. Collectively these proteins form a cell surface complex that acts as a recognition platform for Wnt ligands. Knowledge of the structural dynamics of this complex is limited and pharmacological and in vivo systems that would allow its characterization are scarce. Remo may serve a role in this peculiar signaling pathway and require further analysis." Authors & Affiliations "Auger, Genevieve Marie1, Bigl, Marina1, America, Michelle2, Vanhollebeke Benoit2, Langenhan Tobias1 1Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, Johannisallee 30, 04103 Leipzig, Germany 2Laboratory of Neurovascular Signaling, Department of Molecular Biology, ULB Neuroscience Institute, Université libre de Bruxelles (ULB), Gosselies B-6041, Belgium" About Beatriz Blanco Redondo "I studied Biomedicine at the University of Barcelona. After my bachelors, I moved to Germany where I obtained my Master’s of Science and PhD degree in Dr. Buchner’s group at the University of Wuerzburg. Shortly after receiving my PhD, I joined Dr. Neil Shneider’s group as a postdoctoral research scientist at Columbia University, New York, where I studied the mechanisms of motor neuron degeneration in Amyotrophic Lateral Sclerosis (ALS). In 2017, I joined the group of Prof. Langenhan where I am studying and characterizing newly generated adhesion GPCR receptors in Drosophila as a model organism for future pharmacological applications." Beatriz Blanco Redondo on the web Blanco-Redondo Lab LinkedIn Google Scholar X (Twitter) The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Willem Berend Post Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Groß Victoria Elisabeth 1, Matúš Daniel 2,3, Kaiser Anette 4, Ließmann Fabian 5, Meiler Jens 5, Schöneberg Torsten 2,6, Prömel Simone 1 1 Institute of Cell Biology, Department of Biology, Heinrich Heine University Düsseldorf, Düsseldorf, Germany 2 Rudolf Schönheimer Institute of Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany 3 Department of Molecular and Cellular Physiology, Stanford University, Stanford CA, USA 4 Department of Anaesthesiology and Intensive Care, Medical Faculty, Leipzig University, Leipzig, Germany 5 Institute for Drug Discovery, Faculty of Medicine, Leipzig University 6 School of Medicine, University of Global Health Equity, Kigali, Rwanda" About Willem Berend Post "Willem Berend Post is a PhD student in Cell Biology at Heinrich Heine University in Düsseldorf, Germany. His research focuses on the relevance of aGPCRs in physiology and signaling using both in vitro and in vivo approaches." Willem Berend Post on the web Cell Biology LinkedIn < Previous Session Next Session >

Home → Flash News → What do mission-driven teams and world-class science have in common? ✅ Integrity ✅ Systems that last ✅ The right people In this episode, Joe & Chuck from Company Launch Partners share what it means to build something that endures. 🎧 Catch the full episode: Ep 165 with Chuck DeWeese & Joe St. Germain #gpcr #DrGPCR #ScienceStartup Published on May 6, 2025 Category Dr. GPCR Podcast What do mission-driven teams and world-class science have in common? ✅ Integrity ✅ Systems that last ✅ The right people In this episode, Joe & Chuck from Company Launch Partners share what it means to build something that endures. 🎧 Catch the full episode: Ep 165 with Chuck DeWeese & Joe St. Germain #gpcr #DrGPCR #ScienceStartup Previous Next Recent Articles

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Jennifer Pluznick About this episode Dr. Pluznick discovered that olfactory receptors in mice are also expressed in their kidneys and blood vessels. Her research is focused on the role of chemosensory GPCRs in regulating renal and cardiovascular function, and identifying renal/cardiovascular olfactory receptor ligands, and relating them to whole-animal physiology. This work contributes to a better understanding of how the kidney helps maintain homeostasis in humans. Jennifer is currently an assistant professor of physiology at the Johns Hopkins School of Medicine. She received her undergraduate degree in biology from Truman State University and earned her Ph.D. in renal physiology from the University of Nebraska Medical Center. She then spent five years training as a postdoctoral fellow in the laboratory of Michael Caplan at Yale University, where she studied both renal physiology and sensory biology systems and focused on olfaction. Dr. Jennifer Pluznick on the web John Hopkins Pluznick Lab Pubmed Ted Talk Dr. GPCR Ecosystem 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Bianca Plouffe About Dr. Bianca Plouffe Dr. Bianca Plouffe obtained her B.Sc. in Biochemistry in 2003 from Université de Sherbrooke (Qc, Canada). She then completed an M.Sc. in Physiology from the same university in 2005 by investigating the molecular mechanisms involved in the angiotensin type 2 receptor (AT2R)-mediated neurite outgrowth while characterizing new selective AT2R agonists. In 2006, Bianca obtained a Doctoral Scholarship from the Fonds de Recherche du Québec en Santé. She moved to the University of Ottawa to complete a Ph.D. in Neuroscience. She identified the molecular mechanisms involved in the opposite regulation of dopamine D1 and D5 receptors by protein kinase C. After obtaining a Postdoctoral Fellowship from the Canadian Institutes of Health Research in 2012, Bianca joined the research group of Prof Michel Bouvier at Université de Montréal. As part of Bouvier’s team, Bianca used Bioluminescence Resonance Energy Transfer (BRET)-based technology to tackle important questions related to GPCRs. She identified the structural determinant controlling biased signaling of melatonin type 2 receptors in the context of protection against type 2 diabetes. Bianca also collaborated with Prof. Robert Lefkowitz , which led to the finding that both β-arrestin and G protein can simultaneously bind to some GPCRs when signaling in endosomes by forming a megaplex. In 2018, Bianca was appointed Vice-Chancellor’s Fellow at Queen’s University Belfast to develop her research program. Funded by a Wellcome Trust Seed Award, she investigated biased and compartmentalized G protein signaling by the vasopressin type 2 receptor. In 2021, Bianca secured a permanent position as a lecturer. Her subsequent work has focused on understanding the role of compartmentalized Gq signaling by the cytomegalovirus-encoded chemokine US28 receptor in the context of glioblastoma. Dr. Bianca Plouffe on the web Queen's University Belfast website LinkedIn ResearchGate ORCID Dr. GPCR Ecosystem 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Dr. GPCR Podcast Strategic Partners Dr. Pierre Eftekhari About Dr. Pierre Eftekhari "Clinical physiologist and biologist , with more than 25 years of experience in drug development. have been engaged in GPCR cellular and clinical pharmacology as scientist or PI in neonatal lupus, Cardiomyopathy, hypertension, chagas disease. I have participated and initiated methodologies for development of pharmacologically active anti-GPCR antibodies like agonist, antagonist, inverse agonist or blocker. During my Scholar period I have published or contributed in 38 published scientific work mainly in the field of immunology and pharmacology of GPCR. The majority of my research is concentrated on rhodopsin family with a few works on metabotropic receptor. Since the creation of Inoviem scientific in Nov. 2011 by myself we have been regularly working with GPCRs for our pharma and biotech clients. The latter mainly in target deconvolution and patient stratification." Dr. Pierre Eftekhari on the web Inoviem Scientific ResearchGate LinkedIn Twitter Dr. GPCR 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule A positive Allosteric Modulator of M1 Acetylcholine Receptors Improves Cognitive Deficits in Male and Female Alzheimer’s Mice Date & Time Friday, November 3rd / 1:55 PM About Khaled Abdelrahman Dr. Khaled Abdelrahman graduated in 2006 with a BSc in Pharmaceutical Sciences from Alexandria University (Egypt) followed by MSc in Pharmacology in the same university that was conferred in 2009. He joined the laboratory of Dr. William Cole at the University of Calgary in 2010 for his Ph.D. where he studied the molecular basis underlying altered cerebrovascular function and blood flow in type 2 diabetes. In 2015, He joined Dr. Stephen Ferguson’s laboratory in the Departments of Cellular & Molecular Medicine and Neuroscience at the University of Ottawa as a Postdoctoral Fellow to explore novel G protein-coupled receptor (GPCR) candidates that can be targeted pharmacologically to slow neurodegeneration. He has been also studying what aspects of GPCR signaling are regulated in a sex-selective manner and how this can influence drug discovery in the area of neurodegenerative diseases. He is also a Registered Pharmacist in Canada and held two of the most prestigious Clinician Postdoctoral Fellowships offered by Alberta Innovates and Canadian Institutes of Health Research. He received the Canadian Society of Pharmacology and Therapeutics Postdoctoral and Publication awards along with many Young Scientist Awards from the American Society for Pharmacology and Experimental Therapeutics. Khaled Abdelrahman on the web University of British Columbia Twitter PubMed Google Scholar Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Strategic Project Management for scientists Dr. Yamina Berchiche Get Started Premium Members benefits: - Subscribe and save 25% on every GPCR Course - Early-bird access - Recordings will be available < Back to GPCR courses Watch recording Your Instructor Dr. Yamina Berchiche

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Developing a PROTAC to Degrade the Constitutively Active Onco-GPCR in Uveal Melanoma Date & Time Friday, November 3rd / 4:20 PM About Victoria Rasmussen "Victoria Rasmussen is a graduate fellow in Dr. Thomas Sakmar’s laboratory at Rockefeller University, where she studies the signaling and degradation of G protein-coupled receptors. She completed her undergraduate education at Providence College, receiving a B.S. in Biology and a B.A. in Psychology. During her time at Providence College, she received the Walsh Grant Fellowship to develop novel methods of synthesizing 2-imidazoline scaffolds to be used as proteasome modulators in the laboratory of Travis Bethel. Victoria started her Ph.D. at the Tri-Institutional Ph.D. program in Chemical Biology, where she joined the lab of Thomas Sakmar at Rockefeller University. She is currently working to understand the signaling and degradation of GPCRs in disease states to help test the feasibility of using protein-targeted degradation as a therapeutic strategy. " Victoria Rasmussen on the web Tri-Institutional PhD Program Chemical Biology LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

<< Back to podcast list Dr. GPCR Podcast Strategic Partners A Brief History of allosteric modulation with Dr. Arthur Christopoulos About Dr. Arthur Christopoulos " Arthur Christopoulos is the Professor of Analytical Pharmacology and the Dean of the Faculty of Pharmacy & Pharmaceutical Sciences, Monash University, Australia. His research focuses on novel paradigms of drug action at GPCRs, particularly allosteric modulation and biased agonism, and incorporates computational and mathematical modelling, structural and chemical biology, molecular and cellular pharmacology, medicinal chemistry, and preclinical models of behaviour and disease. His work has been applied to studies encompassing neurological and psychiatric disorders, cardiovascular disease, obesity, diabetes, chronic pain and addiction. He has received substantial, long-term support from international and national competitive, charitable and commercial sources, as well as being academic co-founder of three GPCR-focussed biotechnology companies. Professor Christopoulos has over 360 publications, including in leading international journals such as Nature,Science and Cell, and has delivered over 180 invited presentations. He has served on the Editorial Board of 8 international journals and was a Councillor of the International Union of Basic and Clinical Pharmacology (IUPHAR). He has also been the recipient of multiple awards, including the John J. Abel Award and the Goodman and Gilman Award from the American Society for Pharmacology and Experimental Therapeutics; the Rand Medal from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists; the British Pharmacological Society’s Gaddum Memorial Award; the IUPHAR Sir James Black Analytical Pharmacology Lecturer; the GSK Award for Research Excellence and a Doctor of Laws (Honoris Causa) from the University of Athens. Since 2014, Clarivate Analytics have annually named him a Highly Cited Researcher in ‘Pharmacology & Toxicology’, and in 2021 also named him a Highly Cited Researcher in the additional category of ‘Biology & Biochemistry’. In 2017, he was elected a Fellow of the Australian Academy of Health and Medical Sciences, in 2018 as a Fellow of the British Pharmacological Society, and in 2021 he was elected a Fellow of the Australian Academy of Science for his seminal contributions to drug discovery. In 2023, he was elected a Fellow of the Pharmaceutical Society of Australia. " Dr. Arthur Christopoulos on the web Monash University Wikipedia Google Scholar LinkedIn Dr. GPCR AI Summary Quick recap Yamina and Arthur discussed Arthur's career journey in pharmacology, including his mentors and significant discoveries related to allosteric receptors. They explored the evolution of the field, allosteric modulation concepts, and potential therapeutic approaches involving autoantibodies and allosteric modulators. Additionally, they covered the importance of target product profiles, reproducibility in experiments, and collaborative efforts such as a potential book on GPCR history. Next steps - Arthur will continue to collaborate with other researchers and drug companies to advance the understanding and application of allosteric modulation. - Arthur will work on designing ligands for specific receptors, aiming to create biased agonists for therapeutic use. Summary Arthur's Career Journey and Allosteric Receptors Yamina and Arthur discussed Arthur's career journey and his contributions to the field of pharmacology, with a focus on allosteric receptors and their modulation. Arthur highlighted his mentors' influence, such as Fred Mitchelson and Nigel Burch, and significant discoveries like the concept of synthetic allosteric modulators by Bruns and Fergus. He also discussed the evolution of the field, from biochemical radioligand binding assays to cell-based functional assays, and the influence of Terry Kenakin and chemical programs on his later work. The conversation ended with Arthur's ongoing research and his development of a new operational model. Yamina emphasized the importance of understanding the historical context of the field and the significance of Arthur's contributions. Allosteric Modulation and Hybrid Molecules Arthur and Yamina discussed the development of an operational model for allosteric modulation, emphasizing the balance between mechanism and empiricism. Arthur shared his career journey, including his collaboration with Patrick Sexton and Jim Burch, and the discovery of hybrid molecules with functional selectivity. They also discussed the re-emergence of interest in certain programs, the importance of connections across receptor families, and the potential of hybrid molecules. Arthur's strategy of consulting drug companies and targeting their posters at conferences was also shared with Yamina. Pharmaceutical Industry Experiences and GPCR History Arthur shared his experiences in the pharmaceutical industry, highlighting the differences between big pharma and biotech. They discussed strategies for analyzing large compound screening data, emphasizing robust assays and addressing issues like shifting curves. Arthur recounted a 2004 visit to a pharma company using replicates in assays. Yamina proposed compiling a book on GPCR history through collaborative interviews, considering a symposium to align terminology. For their upcoming project, Yamina favored a conversational approach, while Arthur suggested a kickoff meeting, with Yamina planning chapters and interviews. Bias Mitigation in Symposium Ideas Arthur and Yamina discussed the concept of bias in the context of the history of the Symposium idea. They reviewed significant early papers related to the topic, including work by Brian Roth, Terry Kenakin, Bill Clarke, and Kelly Burke. They also discussed their own research on chemokine receptors and the importance of understanding the natural environment in drug discovery. Lastly, they touched on a project with Nicola Smith that challenged their previous theories. Allosteric Modulation and Drug Discovery Yamina and Arthur delved into the complexities of protein-protein interactions, specifically allosteric modulation. They discussed various modulatory elements, such as RAMPs, G proteins, and GRKs, with Arthur recounting his initial collaboration with Patrick Sexton on RAMPs and amylin receptors. They also delved into the different signaling of Class B receptors and the potential for modulation at various levels. The discussion underscored the potential of allosteric modulators as drugs, despite challenges in the past due to a lack of understanding about the principles involved. They highlighted the importance of fine-tuning the approach to suit different diseases and interdisciplinary collaboration. The discussion also emphasized the need for a disease-specific approach, considering the clinical context and dialing in the desired effect, as well as the significance of rational drug design principles. Allosteric Modulation and Autoantibodies Discussion Arthur and Yamina discussed the potential of autoantibodies and allosteric modulation in the context of disease and therapeutic approaches. Arthur explained the concept of endogenous allosteric ligands and the possibility of using a neutral allosteric ligand as a preferred therapeutic approach, emphasizing the importance of looking for low level cooperativity factors. They also discussed the potential of certain drugs, like flumazenil, as 'nails' or compounds that could be developed into medicines. The conversation highlighted the importance of establishing the correct disease context, setting up appropriate assays, and understanding the models for their work. They both agreed on the necessity of understanding the target product for an allosteric modulator and working backwards from there. TPP, Allosteric Modulators, and Reproducibility Yamina and Arthur discussed the concept of a target product profile (TPP) in drug development, with Arthur explaining its application in other contexts as well. Yamina appreciated Arthur's expertise and indicated she would be creating an outline for an episode on allosteric modulators. They highlighted the importance of reproducibility in scientific experiments, sharing personal experiences and anecdotes. They also discussed their upcoming trips to the GPCR Colloquium in California and current research in their fields. 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 Recent Podcast Articles How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling Sparked a Scientific Journey Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>