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<< Back to podcast list Strategic Partner(s) Dr. Nicola J. Smith About Dr. Nicola J. Smith Dr. Nicola J Smith is an expert in molecular pharmacology with a track record in exploring GPCR structure-function relationships in the context of cardiovascular disease and metabolic disorders. She is a National Heart Foundation of Australia Future Leader Fellow and runs a laboratory of 7 Ph.D. and Honours students at UNSW Sydney, where she has recently been promoted to Associate Professor. Most recently, Dr. Smith’s team has made advances in the understanding of how an orphan GPCR exerts its effects both in vitro (cell culture and ex vivo models) and in vivo (measures of physiological and pathological cardiometabolic function in unconscious and conscious mice). Together with Irina Kufareva , UCSD, her team developed a novel approach to identifying ligands for orphan GPCRs by developing a powerful new computational tool for identifying ‘surrogate’ ligands (borrowed from other receptors) for orphan GPCRs, named GPCR-CoINPocket. Her career goal is to leverage this expertise to establish a research program that takes orphan GPCRs from ‘locked’, inaccessible receptors to well-characterized and understood ‘unlocked’ therapeutic targets with high-affinity ligands. Dr. Nicola J. Smith on the web UNSW Sydney LinkedIn Retraction Watch 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Khaled Abdelrahman About Dr. 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. Dr. Khaled Abdelrahman on the web Twitter PubMed 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Gunnar Schulte About Dr. Gunnar Schulte Gunnar Schulte is a Professor in receptor pharmacology and research group leader for the section Receptor Biology and Signaling at the Department of Physiology and Pharmacology. He has a background in biochemistry from the Free University in Berlin/Germany and a Ph.D. in molecular pharmacology (supervisor: Bertil B Fredholm; 1998-2002) from Karolinska Institutet. As a postdoc, he trained first with Ernest Arenas (Karolinska Institutet, Molecular Neurobiology; 2003-2005) and later with Roger J Summers (Monash University, Melbourne Australia, GPCR pharmacology; 2006) before starting his independent research team "Receptor Biology & Signalling" in 2008. Gunnar Schulte is also the scientific secretary of the Swedish Society for Medical Research (SSMF) and a member of the editorial board/editorial advisory board of Molecular Pharmacology, British Journal of Pharmacology, Pharmacological Reviews, and The Journal of Biological Chemistry. General Research Interest: The focus in the Schulte lab is on Frizzled signaling and pharmacology aiming to understand the role of WNT/Frizzled signaling in biology, physiology, and disease. Most importantly my research team tries to understand underlying mechanisms of WNT-receptor interaction, the relevance of receptor dynamics, and receptor complex composition for signal initiation and specification. The ultimate aim is to use the new knowledge to find, create and optimize Frizzled-targeting small molecule drugs to improve future therapies of human disease. Dr. Gunnar Schulte on the web Schulte Lab LinkedIn Google Scholar Orcid YouTube Dr. GPCR Ecosystem 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Sudarshan Rajagopal About Dr. Sudarshan Rajagopal Dr. Sudarshan Rajagopal obtained his B.S. in Chemistry from The University of Chicago in 1998. He subsequently enrolled in the Medical Scientist Training Program at The University of Chicago. During his doctoral work in the lab of Prof. Keith Moffat, he studied the structural mechanisms of bacterial photoreceptors using time-resolved Laue crystallography. He was awarded his Ph.D. in 2004 and his MD in 2006. He then joined the Internal Medicine Residency training program at Duke University Medical Center. During his Cardiology fellowship, he trained in the lab of Dr. Robert J. Lefkowitz , where his research focused on biased agonism, with the development of approaches to quantify ligand bias and the identification of beta-arrestin-biased receptors. After completing his training in clinical cardiology, he started as an Assistant Professor of Medicine at Duke University School of Medicine. The main focus of his lab’s research is on the mechanisms underlying biased agonism at chemokine receptors and how that contributes to inflammation. The chemokine system is relatively unique in having multiple receptors and multiple ligands that display considerable promiscuity for one another. His group and others have shown that many of these ligands act as biased agonists for the same receptor. His lab is also interested in identifying novel signal transduction mechanisms of GPCRs, such as the formation of complexes between G proteins and beta-arrestins. His clinical focus is on pulmonary arterial hypertension, a disease of the pulmonary arterioles that causes right heart failure, and he serves as co-director of the Duke Pulmonary Vascular Disease Center. Dr. Sudarshan Rajagopal on the web LinkedIn Website Google Scholar LinkedIn Dr. GPCR Ecosystem 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Fiona Marshall About this episode Fiona Marshall got fascinated with GPCRs after attending a lecture on how the beta-adrenergic receptor in the heart is activated by adrenaline, during her undergraduate studies at Bath University. She then pursued her Ph.D. in neuroscience at Cambridge University. An expert in GPCR biology, Fiona published the first description of the cloning and structural requirements of the GABAB receptor. One of her career path-defining moments came when she visited Dr. Chris Tate and Dr. Richard Henderson at the Laboratory of Molecular Biology in Cambridge, UK. As a co-founder of Heptares Therapeutics , now called Sosei Heptares , a GPCR-focused drug discovery and development biotechnology company, Fiona and her team made considerable breakthroughs in the field of GPCR stabilization and structure-based drug design. Today, Dr. Marshall is the VP Head of Neuroscience Discovery and Head of Discovery UK, Global Head of Neuroscience discovery research leading teams in West Point, Boston, and London at MSD. Join me and learn more about her fascinating career trajectory. Dr. Fiona Marshall on the web LinkedIn Twitter Google Scholar MSD UK 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Lauren M. Slosky About Dr. Lauren M. 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 M. Slosky on the web Twitter University of Minnesota Department Page LinkedIn Google Scholar PubMed Research Gate 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Arun Shukla About this episode In this episode of the Dr.GPCR podcast , my guest is Dr. Arun Shukla from the Indian Institute of Technology in Kanpur, India. Arun is currently an Associate Professor & Joy Gill Chair Professor, Intermediate Fellow, Wellcome Trust DBT India Alliance Swarnajayanti Fellow & EMBO Young Investigator at the Department of Biological Sciences and Bioengineering. He earned his master's degree in biotechnology from Jawaharlal Nehru University in India and it was during a biochemistry class where he learned about cell signaling that he became curious and wanted to learn more about it. Arun first started working on GPCRs and their structural characterization at the Max Planck Institute of Biophysics where he completed his doctoral studies in the lab of Dr. Hartmut Michel . Fascinated by GPCRs he wrote to Dr. Bob Lefkowitz and asked him if he could join his lab at Duke University. Dr. Shukla spent several years in the Lefkowitz lab and collaborated extensively with Dr. Brian Kolbika of Stanford University. Join us and learn more about Dr. Shukla’s research and how working in the lab instead of going to classes made him realize that research is what he wants to do for the rest of his life. Dr. Arun Shukla on the web Indian Institute of Technology Dr. Arun Shukla Lab Google Scholar PubMed Wikipedia LinkedIn 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Kevin Pfleger About this episode Dr. Pfleger trained as a pharmacologist and obtained his Ph.D. at the University of Edinburgh. I sat down with Kevin to chat about GPCRs, pharmacology, and his contributions to the field in both the academic and biotech worlds. Professor Pfleger has developed extensive expertise in profiling receptor binding and function at the molecular and cellular levels over the last 20 years, particularly involving GPCRs. He also has globally-recognized expertise in bioluminescence resonance energy transfer (BRET) technology, including his patented Receptor-Heteromer Investigation Technology (Receptor-HIT) for studying heteromers. Kevin is also Director, Biomedical Innovation at The University of Western Australia (UWA) and the MTPConnect Western Australian Life Sciences Innovation Hub. He is Head of Molecular Endocrinology and Pharmacology at the UWA Centre for Medical Research and Harry Perkins Institute of Medical Research, Deputy Director of the Australian Research Council Centre for Personalised Therapeutics Technologies, Chief Scientific Advisor to Dimerix, and co-founder of RAGE Biotech . He currently serves on the Board of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists and is a member of the British Pharmacological Society International Advisory Group. Join me and learn more about Kevin’s work and how he manages all his responsibilities. Dr. Kevin Pfleger on the web LinkedIn ResearchGate Pubmed Google Scholar University of Western Australia Harry Perkins Institute of Medical Research Dr. GPCR Ecosystem 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Raul Gainetdinov About Dr. Raul Gainetdinov Raul R. Gainetdinov is the Institute of Translational Biomedicine Director at Saint Petersburg State University (SPBU), Russia. Before SPBU, Raul R. Gainetdinov was a Senior Researcher in the Department of Neuroscience and Brain Technologies at the Italian Institute of Technology in Genova, Italy (2008-2016) and an Associate Research Professor in the Department of Cell Biology at Duke University in North Carolina, USA (1996-2008). From 2013-2018, he was also a Professor at the Skolkovo Institute of Science and Technology (Skoltech), Moscow. Before joining the Department of Cell Biology in 1996 as a postdoc and becoming faculty at Duke in 2000, he researched at the Institute of Pharmacology Russian Academy of Medical Sciences in Moscow (1988-1996). He received a Ph.D. in pharmacology in 1992 from the Russian Academy of Medical Sciences and an M.D. in 1988 from the Second Moscow Medical Institute, Moscow, Russia. Since 2013, he has been elected Chair of the subcommittee for the Dopamine receptors of the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR). As of August 2022, he has over 270 publications in scientific journals (including Science, Nature, Cell, and PNAS) and co-authored 13 patents. His papers were cited over 28,000 times (H-index – 81, ISI Web of Science). In 2018-2020, Raul R. Gainetdinov was included in the Web of Science (WOS) Highly Cited Researchers (HCR) list, representing the top 0.1% of scientists worldwide. Dr. Raul Gainetdinov on the web Saint-Petersburg State University Wikipedia Google Scholar Researchgate Google 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Graeme Milligan About Dr. Graeme Milligan Professor Graeme Milligan is Gardiner Professor of Biochemistry, Dean of Research, and Deputy Head of the College of Medical, Veterinary, and Life Sciences at the University of Glasgow. His main research group centers on the function, structure, and regulation of G protein-coupled receptors (GPCRs) and their interacting proteins. His experience also includes translating knowledge generated into the selection of targets, screening, and identification of small molecule regulators of these proteins, and progressing such ligands in drug development programs. Prof. Milligan has published more than 550 peer-reviewed articles and his research has been cited more than 35,000 times. He was elected to the Fellowship of the Royal Society of Edinburgh in 1998 and to the Fellowship of the Academy of Medical Sciences in 2016. Prof. Milligan is the co-founder of both Caldan Therapeutics (2015) which discovers novel therapeutics for metabolic diseases including Type 2 Diabetes and other indications including non-alcoholic steatohepatitis (NASH) and inflammatory diseases and Keltic Pharma Therapeutics (2020) which is developing new treatments for malaria. Dr. Graeme Milligan on the web University of Glasgow ResearchGate PubMed Orcid Google Scholar LinkedIn 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 Asking Better Questions in Science: A Practical Guide for Emerging Researchers When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Monitor GPCR internalization in real time with pHSense™ – no-wash, TR-FRET reagents from Revvity. Fast, clear, live-cell receptor trafficking detection. Unlock microscopy-free real-time GPCR internalization with pHSense pHSense™ probes are optimized reagents for plate readers, specifically designed to study internalization using time-resolved fluorescence (TRF) detection. They offer high-sensitivity, no-wash detection of internalization events in a scalable, plate-based format. This technology supports robust analysis even at low endogenous receptor expression levels. Suitable for basal/constitutive and agonist-induced GPCR internalization Compatible with TRF plate readers No-wash protocol simplifies workflow Formats available for modified GPCR cell lines or unmodified primary cells Explore pHSense Products Powered by Revvity’s legacy of innovation in translational science. Dr. GPCR Ecosystem Partner Visit Website Precision Tools for Translational Science Revvity is a global leader in life science innovation, delivering tools and technologies that bridge the gap between discovery and real-world impact. With decades of expertise and an unwavering focus on precision, Revvity empowers scientists to simplify complex workflows, accelerate discovery, and drive breakthroughs in drug development, diagnostics, and disease biology. Whether you’re decoding signaling pathways or designing the next generation of therapeutics, Revvity isn’t just a provider—they’re your partner in discovery. Discover pHSense™ portfolio From binding to signaling to internalization: Cell-based fluorescence assays for complete GPCR characterization The principle of pHSense™ relies on the pH-dependent fluorescence activation of a europium-labeled antibody to monitor receptor internalization in live cells. Neutral pH = low signal: The probe is minimally fluorescent at extracellular neutral pH (≥7), which means it doesn't emit a strong signal when bound to the surface. Internalization into acidic compartments = signal activation: Upon receptor-mediated endocytosis, the probe is internalized into acidic intracellular compartments (like early/late endosomes and lysosomes). The europium complex becomes increasingly fluorescent as the pH drops, enabling dynamic tracking of internalization. Time-Resolved Fluorescence (TRF) = High Signal-to-Background: Europium’s long-lived fluorescence allows TRF detection, which effectively filters out short-lived background signals. This results in high sensitivity and specificity in no-wash, plate-based live-cell assays. pHSense™ Eu Anti-FLAG Designed for the detection of FLAG-tagged receptor and membrane protein internalization. View Product pHSense Eu SNAP Labeling Reagent Can be used to label receptors and membrane proteins carrying an extracellular SNAP sequence with a pHSense probe to monitor their internalization View Product pHSense Fab Anti-Human or Anti-Mouse IgG Fab fragments for monitoring GPCR and antibody internalization in unmodified cells The Fab Anti-Human IgG Eu-conjugate can be used in combination with a neutral anti-GPCR to address unmodified receptors in primary cells View Product The Fab Anti-Mouse IgG2 Eu-conjugate is suited to study mouse biologics targeting GPCR and confirm their internalization effects on receptors. View Product The pHSense™ Advantage Clarity. Consistency. Compatibility. Purpose-Built for Live-Cell Internalization Assays The pHSense™ family of europium-labeled, pH-sensitive reagents is designed to simplify and accelerate the study of GPCR and membrane protein internalization in live cells. These reagents are fully compatible with plate-based, no-wash workflows and use time-resolved fluorescence (TRF) to eliminate background noise—delivering clear, quantifiable signals as targets move into acidic intracellular compartments. What Sets pHSense™ Apart ✅ Time-resolved detection minimizes background noise, which enhances detection sensitivity. ✅ No-wash protocol preserves cell integrity and kinetic detection. ✅ High-throughput ready: faster time-to-results and streamlined data acquisition. ✅ Comprehensive validation: validated for GPCRs, but also antibodies and ADCs. ✅ Versatility across suspension and adherent cells The Full GPCR Toolkit by Revvity Every step of the signaling cascade. One trusted source. GPCRs are among the most powerful and complex targets in biomedical research. Revvity offers a comprehensive reagent portfolio to match that complexity—supporting every stage of the signaling pathway, from ligand binding and G-protein activation to intracellular signaling readouts. With formats including TR-FRET, radioligand binding, cAMP, IP-One, and phospho-protein assays (ERK, AKT, CREB, MEK), this toolkit is built for speed, reproducibility, and translational insight. Proprietary no-wash technologies help reduce hands-on time while maintaining exceptional data quality—so you can move fast without compromise. View Reagents Explore Revvity’s GPCR Assay Technologies Tools designed to illuminate every step of GPCR signaling—from binding to downstream response. Ligand binding Measure receptor engagement with high sensitivity using TR-FRET, radioligand, and Fluorescent Tag-lite® formats. G-Protein Activation Quantify Gs, Gi, and Gq activation in real time with cAMP, GTP, and IP-One assays. Arrestin Recruitment Detect β-arrestin recruitment with TR-FRET and luminescence assays tailored for biased signaling studies. Intracellular Signaling Track key downstream events like ERK, AKT, and CREB phosphorylation with high-throughput precision. Build Your GPCR Assay Workflow Meet the Team behind pHSense™ Eric TRINQUET Sr Director Life Sciences Reagents, Revvity Eric Trinquet is a recognized expert in the field of immunoassays and fluorescence technologies. He currently leads Revvity's Research and Development activities, focusing on biochemical and cellular assay platforms related to Life Sciences Reagents. Before joining Revvity, Eric worked for Cisbio Bioassays first as Director of Technological Development and then as R&D Director. His career is marked by significant contributions, from introducing HTRF technology in the field of high-throughput screening to developing innovative solutions such as the IP-One kit for studying G Protein-Coupled Receptors (GPCRs) and the Tag-lite platform. Elodie DUPUIS R&D Senior project manager, team leader. Elodie Dupuis earned her Master’s degree in biology and biotechnology engineering from the University of Sciences of Nîmes and the Ecole des Mines engineering school (France) in 2009. She then joined Cisbio Bioassays, and later Revvity, as project leader and team manager in the Research & Development department, leading her team on the development of innovative HTRF™ and AlphaLISA™ kits for pharma, biotech, and academic partners. Through her research contributions, she has co-authored numerous scientific publications and holds several patents as an inventor. She has been leading collaborative projects with public research institutes and pharmaceutical companies, most notably the joint Revvity/Institute of Functional Genomics team, EIDOS. In 2020, together with her team, she initiated a long-term research effort that enabled the creation of a new and innovative portfolio for GPCRs, antibody drug conjugates, and several other applications: pHSense™. 2025 marked the commercial launch of the first pHSense products by Revvity. Mathis LAFFENETRE Product Manager, Immunoassay Reagents. Mathis holds a biotechnology engineering degree from the National School of Biomolecule Technology of Bordeaux and an MS in biomedical business management from the Grenoble School of Management. He joined Revvity (then Cisbio) in 2016 as part of the scientific marketing effort to build brand recognition for the HTRF technology and accelerate the company’s reagents use in academic labs, biotech companies, and pharma. In the following years, he held several marketing and strategic positions in France and the US, primarily related to the Immunoassay portfolio. As of 2025, he is part of the Immunoassay & Imaging Reagents Portfolio group as a product manager for the GPCRs, and is responsible for supporting the adoption and expansion of the reagent portfolio into the hands of scientists and researchers. Inside the Science: A Conversation with Revvity's Dr. Eric Trinquet From Rare Earth Probes to Internalization Assays: The pH Sense Story If you’ve ever used HTRF or wondered what goes into making a product worthy of your next experiment, this is your backstage pass. More about this conversation Our Partnership Dr. GPCR Spotlights Revvity’s pHSense™ Reagents for Real-Time GPCR Internalization A new reagent family designed to unlock high-throughput internalization workflows—now featured across the Dr. GPCR Ecosystem Boston, MA – September 2025 — Dr. GPCR, the global nonprofit platform dedicated to advancing GPCR research and drug discovery, is proud to spotlight the launch of pHSense™, a new reagent family from Revvity designed to bring unprecedented clarity, speed, and scalability to the study of receptor internalization. Internalization is a core—but often overlooked—dimension of GPCR biology. Traditionally, studying it has meant long workflows, low throughput, or expensive imaging platforms. pHSense™ changes that by combining europium-based, pH-sensitive probes with no-wash, live-cell protocols and TRF-based detection—making it possible to monitor internalization in real time, in standard plate-based assays. “When we saw dose-dependent internalization in endogenous GLP1R cells—without microscopy—that was the turning point,” said Dr. Eric Trinquet, Director of Research and Development at Revvity. “We knew pHSense could offer something truly new to the GPCR field.” A Tool Designed for Real Research Needs Built on more than two decades of GPCR assay innovation, pHSense™ was developed to overcome three persistent barriers in internalization studies: Complexity of imaging-based workflows Lack of scalability for high-throughput screening Difficulty detecting endogenous receptor activity With pHSense™, scientists can finally move beyond proxy readouts and track GPCR internalization as it happens—even at physiological expression levels. All four formats are validated in well-established models like GLP1R and Mu opioid receptor (MOR), and are compatible with HTRF plate readers already used in most labs. Related Articles How Breakthroughs Happen: Eric Trinquet on Innovation, Serendipity & GPCRs Discover how Dr. Eric Trinquet, creator of HTRF and IP-One assays, turned failure into breakthrough tools for GPCR science. Learn why play, serendipity, and partnerships fuel innovation—and how this mindset can transform your research and biotech career. Dr. GPCR Podcast Oct 16, 2025 4 min read The Truth About GPCR Product Launches: Years in the Making What it really takes to launch a GPCR product—years of failure, science, and strategy. Go behind the scenes of pH-Sense with Revity’s Dr. Eric Trinquet. Dr. GPCR Podcast Oct 8, 2025 4 min read Innovative Data-Driven Solutions: The pHSense Revolution A powerful new tool tracks GPCR internalization in native cells—no imaging, no overexpression. Learn how pH Sense changes the game for drug discovery. Dr. GPCR Podcast Sep 26, 2025 3 min read Dr. GPCR Ecosystem Partner Contact Revvity

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

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

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, including Dr. Bryan Roth , Dr. Robert Lefkowitz , Dr. Fiona Marshall , Dr. Sam Hoare , Dr. Graciela Pineyro , Dr. Debbie Hay , Dr. Randy Hall , tributes to Dr. Marc Caron with over 30 guests including Dr. 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

Home Registration Full Agenda Venue Travel Tips Sponsors Special Issue on Adhesion GPCRs CINVESTAV, Mexico City, Mexico October 23-25 Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE Oct 23 - 9:00 AM Registration & Coffee with light breakfast Read More 9:50 AM Welcoming Remarks Read More 10:00 AM Student Flash Presentations Health and Disease, Metabolism, Nervous System, Proteomics and Transcriptomics, Receptor Structure, Signaling and Activation Mechanism Abhishek Kumar Singh · Alex Torrelli-Diljohn · Emmanouil Kyrloglou · Vasiliki Karagiannakou · Lara-Sophie Brodmerkel · Rashed Rezwan Parag · Hailey Steichen · Tyler Bernadyn · Jesse Stillwell Read More 12:00 PM Coffee Break with lights snacks Read More 12:30 PM State of the Art Talk Adhesion GPCR in Mechanobiology Tobias Langenhan Read More 1:00 PM Plenary Lecture Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Jinpeng Sun Read More 2:00 PM Complimentary Lunch Read More 3:00 PM Session I Tethered agonist - dependent/independent activation mechanism in AGPCRs Signe Mathiasen · Demet Araç · Andrew Dates · Frank Kwarcinski · Peng Xiao Read More 4:30 PM Leaving for City Center Read More 5:00 PM Mexico City Nocturnal Tour, Food and drinks Read More Oct 24 - 9:00 AM Session II AGPCR signaling pathways and trafficking Yuling Feng · Monserrat Avila Zozaya · Erwin G. Van Meir · Pal Kasturi Read More 10:30 AM Coffee Break with lights snacks Read More 11:00 AM Session III Molecular tools and biosensors directed at AGPCR signaling and function Stephanie Häfner · Laurent Sabbagh · Ana Lilia Moreno Salinas Read More 12:00 PM Session IV AGPCRs signaling in the nervous system Joseph Duman · Simeon R. Mihaylov · Anne Bormann Read More 1:00 PM Complimentary Lunch Read More 2:00 PM Posters Caroline Formstone · Jianxiang Xue · Virginea de Araujo Farias · Szymon P. Kordon · Tingzhen Shen · Bill Huang · Júlia Rosell · Sheila Ribalta-Mena · Mariam Melkumyan Read More 3:00 PM Session V Structural mechanisms of AGPCR signaling and function Fabian Pohl · Sumit Bandekar · Florian Seufert Read More 4:00 PM Board meeting/General assembly Welcome to Join Read More 5:00 PM Leave for dinner reception Read More 5:30 PM Complimentary Reception dinner Read More Oct 25 - 9:00 AM Session VI AGPCRs shaping the nervous system Yimin Zou · Dimitris Placantonakis · Nicole Perry-Hauser Read More 10:00 AM Coffee Break with lights snacks Read More 10:30 AM Session VII Physiological and pathological roles of AGPCRs in the nervous system Beatriz Blanco Redondo · Willem Berend Post Read More 11:10 AM Dr. GPCR Community Presentation Monserrat Avila Zozaya Read More 11:30 AM Session VIII Physiological and pathological roles of AGPCRs in the periphery Cheng-Chih Hsiao · Anastasia Georgiadi · Douglas Tilley Read More 12:30 PM Complimentary Lunch Read More 1:30 PM Session VIII * Physiological and pathological roles of AGPCRs in the periphery Tobias Langenhan · Anastasia Georgiadi · Douglas Tilley · Hee-Yong Kim · Alain Garcia De Las Bayonas · Gabriela Aust Read More 2:50 PM Session IX / Technology capsule: Light on aGPCR signaling and function NovoiSMART - A new platform for GPCR antibody drug discovery Gavin Zhang Read More 3:20 PM Coffee Break with pastries announcement of the aGEM award Read More 4:00 PM Closing remarks Read More Jinpeng Sun Identification and Functional Characterization of Adhesion GPCRs As Steroid Hormone Receptors and Hearing and Balance Receptors Bill Huang Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Andrew Dates Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Pal Kasturi Site Specific N-Glycosylation Of The N-Terminal Fragment Of ADGRG6 Drives Proteolytic Processing, Trafficking And Signalling Ana Lilia Moreno Salinas Characterizing hADGRE5/CD97 Activation and Signaling: A Mechanical Stimulation BRET-Based Approach (MS-BRET) Florian Seufert Unveiling the GPS Cleavage Mechanism in ADGRL1 with QM/MM Willem Berend Post The Adhesion GPCR Latrophilin Interacts With The Notch Pathway To Control Germ Cell Proliferation Tobias Langenhan The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Rashed Rezwan Parag Novel isoforms of adhesion G protein coupled receptor B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Emmanouil Kyrloglou GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Virginea de Araujo Farias Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Szymon P. Kordon Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Frank Kwarcinski Discriminating between the extracellular scaffolding and G protein signaling roles of GPR56/ADGRG1 via the characterization of a non-cleavable point mutant knock-in mouse, H381S Erwin G. Van Meir Adhesion GPCR BAI1/ADGRB1 can block IGF1R-mediated growth signalling, increase radiosensitivity and augment survival in medulloblastoma. Laurent Sabbagh bioSens-All: A Multiparametric BRET-Based Platform for Comprehensive Profiling of adhesion GPCR Signaling and Pharmacology-Enabling Drug Discovery Fabian Pohl Structural Determinants Of GAIN Domain Autoproteolysis And Cleavage Resistance Of Adhesion G Protein-Coupled Receptors Beatriz Blanco Redondo Uncovering the signaling pathway of the ADGRA homolog Remoulade in Drosophila Douglas Tilley ADGRF5-mediated regulation of cardiac health and disease Abhishek Kumar Singh Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Lara-Sophie Brodmerkel GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Caroline Formstone Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Mariam Melkumyan GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Signe Mathiasen Signaling Properties of ADGRL3 Monserrat Avila Zozaya The ADGRF5/GPR116 receptor is a key regulator of lymphatic endothelial cell identity and function Simeon R. Mihaylov Bai1 Is A Novel Neuronal Substrate Of The Psychiatric Risk Kinase TNIK Sumit Bandekar Structural studies of the CELSR1 extracellular region reveal a compact multidomain module of fourteen domains which regulates signaling Nicole Perry-Hauser Adhesion G protein-coupled receptor latrophilin-3 (ADGRL3) modulation of dopaminergic neurotransmission Anastasia Georgiadi Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Jesse Stillwell Next Generation MBD2 inhibitors for Brain Cancer Therapy Hailey Steichen Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Sheila Ribalta-Mena Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Jianxiang Xue Generation and characterization of collecting duct specific GPR56 knockout mice Demet Araç An ECR-Mediated and TA-independent Mechanism of aGPCR Activation: Direct Communication of Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Yuling Feng Localization of putative ligands for adhesion G protein-coupled receptors in mouse tissues. Joseph Duman BAI1/ADGRB1-mediated Regulation of Mitochondrial Morphology in Axons Yimin Zou ADGRCs in glutamatergic synapse formation, maintenance and degeneration Cheng-Chih Hsiao ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Alain Garcia De Las Bayonas The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alex Torrelli-Diljohn Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Tyler Bernadyn Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tingzhen Shen Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Júlia Rosell Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Peng Xiao Tethered Peptide Activation Mechanism of Adhesion GPCRs Stephanie Häfner The NTF Release Sensor Approach for Drug Discovery for Human Adhesion GPCRs Anne Bormann Intricacies Of Complex Assembly And Ligand Interaction In The Adhesion GPCR Latrophilin/Cirl Dimitris Placantonakis Antibody-drug conjugates targeting CD97 in glioblastoma Gabriela Aust Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Hee-Yong Kim Characterization of Phenotypes Associated with GPR110 Deletion Vasiliki Karagiannakou A single cell GPCR map of thermogenic fat Gavin Zhang NovoiSMART - A new platform for GPCR antibody drug discovery

GPCR Courses Expert knowledge, flexible courses - career-ready skills —build skills that translate at the bench and in the boardroom. 👇 Start Learning! The Practical Assessment of Signaling Bias Signaling bias is an inherent feature of pharmacology, influencing receptor behavior even when unnoticed. Different ligands stabilize distinct receptor states, leading to diverse signaling outcomes. Measuring and understanding bias helps design drugs that maximize therapeutic benefits while minimizing side effects. Terry Kenakin 🔒 Premium Content Watch recording Strategic Project Management for scientists Gain practical project management skills explicitly designed for research and innovation. Learn to plan, execute, and manage scientific projects while balancing timelines, resources, and team coordination. Master strategic planning, risk assessment, and collaboration tools to boost efficiency and project success. Yamina Berchiche 🔒 Premium Content Watch recording Applying Pharmacology to Drug Discovery Class 1 - Fundamentals of Pharmacology Class 2 - Characterizing Agonists Class 3 - Characterizing Antagonists Class 4 - Characterizing Allosteric Modulators Terry Kenakin 🔒 Premium Content Watch recording Advanced data analysis for GPCR pharmacology Class 1 - Concentration-response analysis: Become a CRC super-user Class 2 - Quantifying agonist pharmacology and biased agonism Class 3 - Antagonist pharmacology and binding assay analysis Class 4 - New dimensions of activity: Allosteric modulators and kinetics Sam Hoar 🔒 Premium Content Watch recording Principles of Pharmacology in Drug Discovery II Advanced Methods for the Optimization of Candidate Selection Lecture 1: The Eyes to See- The Importance of Pharmacologic Assays Lecture 2: Drug Disposition in Physiological Tissues as a Therapeutic Variable Lecture 3: The Application of GPCR Ligand Kinetics to Candidate Design Lecture 4: Unconventional GPCR Ligands as Drugs Lecture 5: Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit Terry Kenakin 🔒 Premium Content Watch recording Principles of Pharmacology in Drug Discovery I Techniques for Effective Lead Optimization of Candidate Molecules Lecture 1: GPCR Project Initiation and Design for Discovery of New Molecules Lecture 2: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists Lecture 3: Agonists and Efficacy: A New World of GPCR Efficacies / Biased Signaling Lecture 4: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to quantify the allosteric effect Terry Kenakin 🔒 Premium Content Watch recording What others are saying about the courses 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 The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work Anonymous

Applying Pharmacology to Drug Discovery by Terry Kenakin | Dr. GPCR Courses Applying Pharmacology to Drug Discovery Dr. Terry Kenakin The main objective of this course is to give the registrant a good overall understanding of the unique science of pharmacology and how it can describe drug action in system-independent ways. This allows predictions of drug activity in all physiological systems, not only the system where testing is done. Techniques will be described to quantify drug activity in terms of affinity, efficacy, and allosteric function. Pharmacology is a unique discipline and is critical to drug discovery. Registrants will learn: Methods to characterize the three major drug types. What makes each drug type unique to therapeutic pharmacology? 3. Essential information is needed to characterize a drug's profile aimed at therapy. Modules: Week 1 - Fundamentals of Pharmacology Week 2 - Characterizing Agonists Week 3 - Characterizing Antagonists Week 4 - Characterizing Allosteric Modulators Good to know Registrations start on December 15th and close on February 2nd. Classes will be live from Zoom on Thursdays from 10 am to 11:30 am EST. Sessions will include a 1-hour live lecture plus 30 minutes of Q&A. Every participant will also get the chance to have a 1:1 meeting with Dr. Kenakin during the four weeks, scheduled according to the professor's availability. Participants who complete the course will get an online certification signed by the professor and the Dr.GPCR Team. A splendid time is guaranteed for all. What others are saying about the courses 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 Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him 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 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 The content had enough depth to satisfy the hunger for theory while being full of practical knowledge Anonymous The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work 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 What would you like to learn today?

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Home Courses Articles About Log In / Sign Up Terry's Pharmacology Corner Lost in GPCR Complexity? Step Into Terry’s Corner Finally, See the Signal 🔥 Watch course | Dec 9, 2025 🔥 Watch the AMA Session | Dec 2, 2025 🔥 Watch course | Nov 18, 2025 🔥 Watch course | Nov 11, 2025 🔥 Watch the AMA Session | Sept 18, 2025 🔥 Watch course | Oct 21, 2025 🔥 Watch course | Oct 14, 2025 🔥 Watch course | Oct 7, 2025 🔥 Watch course | Sept 30, 2025 🔥 Watch course | Sept 23, 2025 🔥 Watch course | Sept 16, 2025 🔥 Watch course | Sept 9, 2025 🔥 Watch course | Sept 2, 2025 🔥 Watch course | Aug 26, 2025 🔥 Watch course | Aug 19, 2025 🔥 Watch course | Aug 12, 2025 🔥 Watch course | Aug 5, 2025 🔥 Watch course | July 29, 2025 🔥 Watch course | July 22, 2025 🔥 Watch course | July 15, 2025 🔥 Watch course | July 8, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 🔥 Watch course | July 1, 2025 TCBuyCourse Start Learning with Terry Best Value Terry’s Corner $2,999 $ 2,999 Every year Only Founders Get Discounted Full Vault Access —Then It’s Gone 40 years. One corner. One-time pricing. Valid until canceled 7 day free trial Select Watch 4 New Courses Each Month Connect in a Private Drug Hunter Hub Skip The Fluff, Learn What Matters Join Monthly AMAs with Terry Unlock 40+ Years of Expertise Master GPCRs with Precision 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

Summit 2022 Full Schedule & Details Dr. GPCR Summit 2022 Live Talk Schedule Welcome to the Ecosystem Dr. Yamina Berchiche Mon Oct 10 2022 14:00:00 GMT+0000 (Coordinated Universal Time) Details Neomorphic mutations in GNAO1 encephalopathy: from mechanisms to drug discovery Dr. Vladimir Katanaev Mon Oct 10 2022 16:00:00 GMT+0000 (Coordinated Universal Time) Details Translating the force - Mechano-sensing GPCRs Dr. Ines Liebscher Mon Oct 10 2022 17:00:00 GMT+0000 (Coordinated Universal Time) Details GPCR fragment-based drug discovery enabled by the Confo Therapeutics technology Dr. Christel Menet Mon Oct 10 2022 18:00:00 GMT+0000 (Coordinated Universal Time) Details Targeting muscarinic receptors to slow neurodegenerative disease Dr. Andrew Tobin Mon Oct 10 2022 19:00:00 GMT+0000 (Coordinated Universal Time) Details Regulation of Metabotropic Glutamate Receptor Signaling: Role in Huntington’s and Alzheimer's Diseases Dr. Stephen Ferguson Mon Oct 10 2022 20:00:00 GMT+0000 (Coordinated Universal Time) Details Cancelled / Dr. Devki Sukhtankar & Dr. Juan Jose Fung Talk Dr. Devki Sukhtankar & Dr. Juan Jose Fung Mon Oct 10 2022 21:00:00 GMT+0000 (Coordinated Universal Time) Details Environment Matters: One Receptor but many targets Dr. Rosie Dawaliby Tue Oct 11 2022 12:00:00 GMT+0000 (Coordinated Universal Time) Details Fine-tuning glutamate receptor activity with allosteric modulators for neurodegenerative and psychiatric disorders Dr. Karen Gregory Tue Oct 11 2022 13:00:00 GMT+0000 (Coordinated Universal Time) Details Exploring circuit selective GPCR functions using intersectional Crispr/Cas9 approaches Dr. Martin Beaulieu Tue Oct 11 2022 14:00:00 GMT+0000 (Coordinated Universal Time) Details A Synaptic Adhesion Sensing Code Dictated by aGPCRs Latrophilins Dr. Antony Boucard Tue Oct 11 2022 15:00:00 GMT+0000 (Coordinated Universal Time) Details High throughput GPCR screening technologies enable deciphering host-microbiome communication and the development of drug candidates Dr. Alex Dajkovic Tue Oct 11 2022 16:00:00 GMT+0000 (Coordinated Universal Time) Details Application of optical GPCR & G protein biosensors for drug discovery & assessment of constitutive activity Dr. Hannes Schihada Wed Oct 12 2022 12:00:00 GMT+0000 (Coordinated Universal Time) Details Role of constitutive Gq signalling from endosomes by US28 in glioblastoma Carole Daly Wed Oct 12 2022 12:20:00 GMT+0000 (Coordinated Universal Time) Details Exploration of GPCR signaling using nanobody-ligand conjugates Dr. Shivani Sachdev Wed Oct 12 2022 12:40:00 GMT+0000 (Coordinated Universal Time) Details Getting the most from your biosensor assays: Data analysis for GPCR discovery Dr. Sam Hoare & Dr. Luciana Leo Wed Oct 12 2022 14:00:00 GMT+0000 (Coordinated Universal Time) Details Molecular mechanism of formation of GPCR domains at the cell surface Gabriele Kockelkoren, M.Sc. Wed Oct 12 2022 17:00:00 GMT+0000 (Coordinated Universal Time) Details Location Bias of G Protein-Coupled Receptor Kinases Promotes Biased Signaling at CXCR3 Chloe Hicks Wed Oct 12 2022 17:20:00 GMT+0000 (Coordinated Universal Time) Details Isolating ligand binding kinetics of mini G protein bound GPCR receptor conformations. Dr. Nicola Dijon Wed Oct 12 2022 17:40:00 GMT+0000 (Coordinated Universal Time) Details Functional modulation of PTH1R activation and signaling by RAMP2 Dr. Katarina Nemec Wed Oct 12 2022 18:30:00 GMT+0000 (Coordinated Universal Time) Details Anti-inflammatory drugs for the treatment of neuroinflammation in Glaucoma Joan Serrano-Marín Wed Oct 12 2022 18:50:00 GMT+0000 (Coordinated Universal Time) Details Oxytocin-Vasopressin Ligand-Receptor Bias Kiyan Afzali Wed Oct 12 2022 19:10:00 GMT+0000 (Coordinated Universal Time) Details Cancelled /Data integrity workshop Dr. Nicola Smith Wed Oct 12 2022 21:00:00 GMT+0000 (Coordinated Universal Time) Details A Journey of discovery with CCR5: from basic science to the clinic via new technology Dr. Oliver Hartley Thu Oct 13 2022 13:00:00 GMT+0000 (Coordinated Universal Time) Details Virtual Reality in GPCR Structure-based Drug Design: The Orexin System and Suvorexant Daniel Gruffat, M.Sc Thu Oct 13 2022 14:00:00 GMT+0000 (Coordinated Universal Time) Details Integrating signaling kinetics into GPCR compound profiling Dr. Leigh Stoddart Thu Oct 13 2022 15:00:00 GMT+0000 (Coordinated Universal Time) Details Enabling the discovery of next generation therapeutics via the ebBRET-based biosensor technology bioSensAll Herthana Kandasamy, M.Sc. Thu Oct 13 2022 16:00:00 GMT+0000 (Coordinated Universal Time) Details ArcoScreen a new GPCR screening platform Dr. Margaux Duchamp Thu Oct 13 2022 17:00:00 GMT+0000 (Coordinated Universal Time) Details New GPCRdb structure and ligand resources Dr. David Gloriam, Dr. Albert Kooistra, Gaspar Pandy-Szekeres (M Sc.), Dr. Jimmy Caroli Fri Oct 14 2022 14:00:00 GMT+0000 (Coordinated Universal Time) Details GPCR-mediated regulation of aging-related disease Dr. Stuart Maudsley Fri Oct 14 2022 16:00:00 GMT+0000 (Coordinated Universal Time) Details Biased Allosteric Modulators in Drug Discovery Dr. Brian Arey Fri Oct 14 2022 17:00:00 GMT+0000 (Coordinated Universal Time) Details The Interplay of Incretin Receptor Trafficking and Signaling in Pancreatic Islets Dr. Alejandra Tomas Fri Oct 14 2022 18:00:00 GMT+0000 (Coordinated Universal Time) Details Structure-guided GPCR drug discovery: Focus on psychedelics Dr. Bryan Roth Fri Oct 14 2022 19:00:00 GMT+0000 (Coordinated Universal Time) Details Mechanism of Activation of a Family B GPCR Dr. Kaavya Krishna Kumar Fri Oct 14 2022 20:00:00 GMT+0000 (Coordinated Universal Time) Details Dr. GPCR Ecosystem Partners Tags Dr. GPCR Summit Dr. GPCR Summit 2022 Dr. GPCR Summit 2022 Schedule Dr. GPCR Summit Details Dr. GPCR Summit Pre-Recorded Talks Dr. GPCR Summit Live Talks Dr. GPCR Poster Presentations Submit Pre-Recorded Talk Presentation for Dr. GPCR Summit 2022 Submit Live Talk Presentation for Dr. GPCR Summit 2022 Submit Poster Presentation for Dr. GPCR Summit 2022

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program Download PDF Program Thursday, November 2nd / 11:00 AM - 1:30 PM Registration Read More Thursday, November 2nd / 1:30 PM Welcome Remarks Read More Thursday, November 2nd / 1:45 PM - 2:45 PM Trainee Symposium I Eric Johansen , Johns Hopkins University Grace Mazarura , McGill University Émile Breault, Université de Sherbrooke Bassam Albraidy , Ottawa Hospital Research Institute Read More Thursday, November 2nd / 2:45 PM Coffee Break 1 Read More Thursday, November 2nd / 3:00 PM - 4:00 PM Trainee Symposium II Amr Mousa , University of Western Ontario Louis-Philippe Picard , University of Toronto Remi Janicot , Boston University Meredith Skiba , Harvard University Read More Thursday, November 2nd / 4:00 PM Check In Read More Thursday, November 2nd / 4:30 PM "Have a nice weekend, and I'll see you tomorrow!": RAMP-interacting GPCR Pathways Inaugural Marc G. Caron Keynote Lecture Kathleen M. Caron University of North Carolina at Chapel Hill Read More Thursday, November 2nd / 5:30 PM Welcome Reception and Poster Session 1 Read More Thursday, November 2nd / 8:00 PM Dinner 1 Read More Friday, November 3rd / 7:30 AM Breakfast 1 Read More Friday, November 3rd / 8:30 AM Dopamine-Mediated Motor Recovery after Ischemic Stroke Mario Tiberi Ottawa Hospital Research Institute Read More Friday, November 3rd / 8:55 AM A journey from Duke to McGill along the dopamine circuit Bruno Giros McGill University Read More Friday, November 3rd / 9:20 AM Cannabinoid compounds to augment L-DOPA treatment in Parkinson's Disease Ali Salahpour University of Toronto Read More Friday, November 3rd / 9:45 AM Pharmacological and Genetic Preclinical Models of Ghrelin Receptor Functional Selectivity to Investigate Metabolic Disease Pathophysiology Joshua Gross Duke University Medical Center Read More Friday, November 3rd / 10:25 AM Coffee Break 3 Read More Friday, November 3rd / 10:40 AM Regulation and role of mitochondria delta opioid receptors Louis Gendron Université de Sherbrooke Read More Friday, November 3rd / 11:05 AM Biased agonism at the GLP-1 receptor: from structure to animal models of disease Patrick Sexton Monash University Read More Friday, November 3rd / 11:30 AM Complex Allosteric Cannabinoid Receptor Pharmacology Robert Laprairie University of Saskatchewan Read More Friday, November 3rd / 11:55 AM Unveiling Non-Canonical Functions for Gαq Signaling Pathways Poster Talk Catalina Ribas University Autonoma of Madrid Read More Friday, November 3rd / 12:10 PM Lunch 1 Read More Friday, November 3rd / 1:30 PM Interaction with the cell adhesion molecule NEGR1 affects mGluR5 cell signalling Fabiola Ribeiro Federal University of Minas Gerais, Brazil Read More Friday, November 3rd / 1:55 PM A positive Allosteric Modulator of M1 Acetylcholine Receptors Improves Cognitive Deficits in Male and Female Alzheimer’s Mice Khaled Abdelrahman The University of British Columbia Read More Friday, November 3rd / 2:10 PM Genetic Deletion of Atypical VGLUT3 Rescues Huntington’s Disease Phenotype and Neurodegeneration in zQ175 Mice Poster Talk Karim Ibrahim University of Ottawa Read More Friday, November 3rd / 2:45 PM Removing the GPCR-mediated brake on exocytosis enhances insulin action, promotes adipocyte browning, and protects against diet-induced obesity Heidi Hamm Vanderbilt University Read More Friday, November 3rd / 3:00 PM Coffee Break 4 Read More Friday, November 3rd / 3:30 PM G Proteins and GPCRs in Cancer: Novel Precision Targeted and Immunotherapies J. Silvio Gutkind UC San Diego Read More Friday, November 3rd / 3:55 PM Inhibition of Relaxin Autocrine Signaling Confers Therapeutic Vulnerability in Ovarian Cancer Robert Rottapel University of Toronto Read More Friday, November 3rd / 4:20 PM Developing a PROTAC to Degrade the Constitutively Active Onco-GPCR in Uveal Melanoma Poster Talk Victoria Rasmussen Rockefeller University Read More Friday, November 3rd / 4:35 PM Targeting adenosine signaling for immuno-oncology John Stagg CHUM, Université de Montréal Read More Friday, November 3rd / 5:00 PM Poster Session #2 Read More Friday, November 3rd / 7:00 PM Dinner 2 Read More Friday, November 3rd / 9:30 PM Board Meeting To discuss the next GPCR Retreat All PIs welcome Read More Saturday, November 4th / 7:30 AM Breakfast 2 Read More Saturday, November 4th / 8:15 AM Distinct sub-cellular signal propagation as a component of functional selectivity Michel Bouvier Université de Montréal Read More Saturday, November 4th / 8:40 AM Biochemical Mechanisms Underlying Location Bias in GPCR Signaling Sudarshan Rajagopal Duke University Medical Center Read More Saturday, November 4th / 9:05 AM Structure-based discovery of functionally selective 5-HT1A receptor agonists Peter Gmeiner Friedrich-Alexander University of Erlangen-Nürnberg Read More Saturday, November 4th / 9:30 AM Atypical Structure and Function of Typical Chemokine Receptors Tracy Handel UC San Diego Read More Saturday, November 4th / 9:55 AM Coffee Break 5 Read More Saturday, November 4th / 10:10 AM Using food perception and bioamine signaling networks to slow aging Scott Leiser University of Michigan Read More Saturday, November 4th / 10:35 AM Interrogating Multiscale Receptors Functions in Space Martin Beaulieu University of Toronto Read More Saturday, November 4th / 11:00 AM Atypical Structure and Function of Typical Chemokine Receptors Amy Ramsey University of Toronto Read More Saturday, November 4th / 11:30 AM Illuminating Functional Selectivity and Allosterism at GPCRs. Hyman B. Niznik Keynote Lecture Stephane Laporte McGill University Read More Saturday, November 4th / 12:30 PM Closing Remarks. Lunch and farewell Read More 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

GPCR Courses Expert knowledge, flexible courses - career-ready skills —build skills that translate at the bench and in the boardroom. Go premium to get access The Practical Assessment of Signaling Bias Signaling bias is an inherent feature of pharmacology, influencing receptor behavior even when unnoticed. Different ligands stabilize distinct receptor states, leading to diverse signaling outcomes. Measuring and understanding bias helps design drugs that maximize therapeutic benefits while minimizing side effects. Terry Kenakin 🔒 Premium Content Watch recording Strategic Project Management for scientists Gain practical project management skills explicitly designed for research and innovation. Learn to plan, execute, and manage scientific projects while balancing timelines, resources, and team coordination. Master strategic planning, risk assessment, and collaboration tools to boost efficiency and project success. Yamina Berchiche 🔒 Premium Content Watch recording Applying Pharmacology to Drug Discovery Class 1 - Fundamentals of Pharmacology Class 2 - Characterizing Agonists Class 3 - Characterizing Antagonists Class 4 - Characterizing Allosteric Modulators Terry Kenakin 🔒 Premium Content Watch recording Advanced data analysis for GPCR pharmacology Class 1 - Concentration-response analysis: Become a CRC super-user Class 2 - Quantifying agonist pharmacology and biased agonism Class 3 - Antagonist pharmacology and binding assay analysis Class 4 - New dimensions of activity: Allosteric modulators and kinetics Sam Hoar 🔒 Premium Content Watch recording Principles of Pharmacology in Drug Discovery II Advanced Methods for the Optimization of Candidate Selection Lecture 1: The Eyes to See- The Importance of Pharmacologic Assays Lecture 2: Drug Disposition in Physiological Tissues as a Therapeutic Variable Lecture 3: The Application of GPCR Ligand Kinetics to Candidate Design Lecture 4: Unconventional GPCR Ligands as Drugs Lecture 5: Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit Terry Kenakin 🔒 Premium Content Watch recording Principles of Pharmacology in Drug Discovery I Techniques for Effective Lead Optimization of Candidate Molecules Lecture 1: GPCR Project Initiation and Design for Discovery of New Molecules Lecture 2: Drug Affinity: Measurement of Antagonism (Binding and Function) / Classifying Antagonists Lecture 3: Agonists and Efficacy: A New World of GPCR Efficacies / Biased Signaling Lecture 4: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to quantify the allosteric effect Terry Kenakin 🔒 Premium Content Watch recording What others are saying about the courses 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 The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work Anonymous CoursesListPremium Become a Premium Member Watch Courses Recordings Premium Yearly $ 499 499$ Every year 🚀 Everything you need to master GPCR science — in one membership. Select 🎓 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. 🔒 Grandfather Guarantee, your rate never increases Frequently asked questions What is Dr. GPCR University? Dr. GPCR University is an educational platform that provides in-depth learning and training resources on G protein-coupled receptors (GPCRs). At Dr.GPCR University, you’ll find: Courses: Dive deep into curated educational content designed by experts in GPCR research. Our courses provide comprehensive, on-demand learning to help you expand your knowledge and stay current in the field. Symposia Engage with leading scientists through our symposia, featuring in-depth discussions on cutting-edge research and breakthroughs in GPCR science. Each session brings together a community of experts to share insights and advancements. Summit A global gathering of researchers and professionals showcasing the latest developments in GPCR research. Participate in presentations, networking opportunities, and collaborative sessions. Virtual Café Listen to casual, interactive discussions with experts in the field. How do I register for Dr. GPCR University Masterclasses? To register for any course, you must have a FREE Ecosystem member account . We carefully screen anyone signing up to ensure they are real humans working on GPCRs, so you might not receive confirmation immediately. When signing up for the first time, try to complete as much information as possible about yourself. Who are the Dr. GPCR University Masterclasses designed for? The classes are designed for researchers, students, and professionals in biology, pharmacology, and biochemistry, but anyone interested in GPCR research is welcome to join. What topics are covered in the masterclasses? Masterclasses cover a variety of track including but not limited to p harmacology foundations, agonists, antagonists & core mechanisms , allosteric modulation & kinetics, advanced quantitative approaches and innovation & strategic application Can I register my team for a Dr. GPCR University Masterclasses? To register as a team, one of you must be a Premium Member . This person must email hello@drgpcr.o rg indicating how many people will register for the course, the names of the participants, and their emails. We will contact each person individually to help them set up a FREE Ecosystem Membership . They will be asked to join a private group to keep updated with the latest announcements about the course. Are the masterclasses on-demand or live? Dr. GPCR University offers both on-demand and live classes led by experts in the field. On-demand classes are only available for Premium Members . Do I need prior knowledge of GPCRs to join the masterclasses? Some classes may require basic knowledge of GPCRs, but many are designed to accommodate beginners as well as advanced learners. What kind of certification will I receive upon completing a masterclass? Participants will receive a certificate of completion from Dr. GPCR University, which can be used to showcase your expertise and enhance your professional credentials. Can I access the course material after completing the course? Yes, if you are a premium member.

Get one year of free Dr. GPCR Premium access for your entire academic lab. Teach a course at Dr. GPCR University and unlock expert resources, training, and tools. Academic Team Access Program One Year of Dr. GPCR Premium — Free for Your Entire Lab Empowering academic discoveries with industry-grade GPCR resources. Why We Created This Program? Your research group plays a critical role in advancing GPCR science. We want to support academic labs with the same high-quality tools, courses, and insights used by leading biotech teams—without financial barriers. The Dr. GPCR Academic Team Access Program gives your entire lab one year of Premium membership at no cost, in exchange for contributing to the community’s shared knowledge base through teaching . How does it work? No Cost, No Hidden Requirements The program is 100% free for academic labs who contribute as instructors. No recurring charges. No credit card required. Your Whole Lab Gets One Year of Premium Access Once approved, every member of your team receives free Premium access for 12 months, including: Full access to Dr. GPCR Masterclasses & University Vault Weekly News extended editions Exclusive event recordings, slides, and community decks Premium research insights and ecosystem reports Priority access to certain events and AMAs A Member of Your Lab Teaches at Dr. GPCR University Contribute your expertise by teaching a topic, workshop, or course within the Dr. GPCR University. Format is flexible — we work with your availability. Become part of the Dr. GPCR University Instructor community Learn More & Join the Program To keep things simple, we created a single guide that covers: Eligibility guidelines Teaching formats & examples Instructor expectations Course creation support Application steps Timeline & onboarding What your team receives Renewal options 👉 Everything is explained here *This link takes you to a dedicated page with all the details. Book Ready to Unlock Premium for Your Entire Lab—At No Cost? 👉 Learn More & Get Started Meet directly with Dr. Yamina Berchiche for a focused strategy conversation to align your goals, uncover opportunities, and map your next steps.

Discover special university group pricing for Dr. GPCR courses. Save with discounted packages and provide your students or faculty access to premium GPCR learning resources. Empower Your Team with Dr. GPCR Premium Give your team the tools to grow together and stay at the forefront of GPCR science. Save 15% on annual Premium Memberships when you enroll five or more members. Access expert-led courses, 200+ talks, community tools, and curated insights designed to keep your team connected, informed, and inspired. Important Information To qualify for the team discount, your group must include at least five members. If fewer than five members are submitted: • Memberships won’t be activated. • You’ll receive a 50% refund to cover processing costs. 👉 Please double-check your team list before submitting to avoid delays. Questions? We’re here to help: Hello@DrGPCR.org . How It Works? 1️⃣ Get Your Team Ready Gather at least 5 team members who’ll join under your group plan. Make sure each person has (or creates) an account on the Dr. GPCR Ecosystem . 3️⃣ Confirm and Pay Securely After submitting, review your details and finalize your team payment. You’ll automatically receive a confirmation email once your submission is received. 2️⃣ Submit the Team Form Complete the short form with your team names, emails, and organization details. This ensures every member gets full Premium access and personalized onboarding. 4️⃣ Membership Activation Our team will manually review and activate your group’s memberships. Activation takes 3–5 business days , and we’ll notify you once your access is live. 💡 Need to add someone later? No problem — we’ll help you update your team anytime. Apply for Your Team Discount 👇 📢 Limited-time offer – don’t miss out! 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. $424.15 Order Now 💡 Have questions? Contact us at Hello@DGPCR.org Book Plan Your Next Move in GPCR Discovery Meet directly with Dr. Yamina Berchiche for a focused strategy conversation to align your goals, uncover opportunities, and map your next steps.

Join GPCR Happy Hour to connect with scientists across academia, biotech, and pharma - a free networking event. Sign up and join us! GPCR Happy Hour – Connect, Collaborate, Discover A global networking event where GPCR scientists break silos and build lasting connections. Sign Up to Get Event Updates Happy Hours Partners Why Join GPCR Happy Hour? Scientist-led : Built by GPCR researchers, for GPCR researchers. Cross-sector : Academia, biotech, pharma, CROs all in one room. Consistent : Monthly cadence ensures ongoing connections. Accessible : Online & free to join – no travel barriers. Action-oriented : Conversations designed to spark collaborations, not just chatter. How It Works? Step 1 Register Sign up once to access all upcoming GPCR Happy Hour events. Step 2 Get the Link Receive a secure calendar invite with Zoom/virtual event details. Step 3 Join the Conversation Show up to live sessions and meet GPCR scientists across disciplines. Step 4 Engage & Connect Breakout rooms + structured prompts maximize meaningful networking. Step 5 Follow Up Access shared contact lists and resources to keep collaborations alive. Pricing: Free (sponsored by Dr. GPCR & Partners) Upcoming and Past Happy Hours GPCR Happy Hour – Boston, Sept 2025 Every September, Boston welcomes the global biotech and drug discovery community. Scientists, investors, and CRO professionals fly in from around the world, while Boston’s own vibrant life sciences hub shows up in full force. GPCR Happy Hour is where these two worlds meet. It’s not just networking. It’s where partnerships spark, ideas collide, and the GPCR community grows stronger — together. GPCR Happy Hour Dr. GPCR News Aug 20, 2025 3 min read

Applying Pharmacology to Drug Discovery 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