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Explore GPCR lipid rafts, bitter taste receptor pharmacology, and data integration in this expert interview with Dr. Keyvan Sedaghat. << Back to podcast list Strategic Partner(s) How Lipid Rafts Organize GPCR Signaling This episode features Dr. Keyvan Sedaghat discussing how GPCR function is shaped by lipid raft compartmentalization, the expanding therapeutic landscape of bitter taste receptors, and the importance of data-driven resources. Dr. Sedaghat details the construction of an open-access GPCR-lipid raft database and reviews key findings from his research on D1 receptor desensitization and GRK isoform signaling. Listeners gain insights into how membrane microdomains modulate GPCR activity, the translational impact of taste receptors in cancer and metabolic diseases, and emerging high-throughput methods for functional assay development. The conversation underscores the ongoing need for rigorous experimental validation following computational predictions. For more on advanced topics in GPCR drug discovery and methods, browse additional episodes at Dr. GPCR Premium. Why This Matters How lipid raft microdomains selectively regulate GPCR signaling and internalization Why the localization of Gα subunits impacts antidepressant drug efficacy and diagnostic innovation What the functional diversity of bitter taste receptors means for novel therapeutic targets beyond sensory biology The moment when open-access GPCR data integration improves both research reproducibility and hypothesis generation How computational approaches and wet-lab validation complement each other in functional assay development Who Should Listen If you face complex GPCR questions at the bench or in translational research, this discussion will resonate. When you’re mapping receptor localization and need to understand the mechanistic role of microdomains If you’re expanding functional assays to capture non-canonical GPCR roles in disease When integrating computational predictions with real-world pharmacological readouts If you see the research value in collaborative, up-to-date GPCR data resources About Keyvan Sedaghat Keyvan Sedaghat began his scientific training with a pharmacy degree in Iran, then completed his graduate education in cellular and molecular medicine with a specialization in pharmacology at the University of Ottawa. There, under Professor Mario Tiberi, he focused on G protein-coupled receptors and D1 receptor regulation—work that sparked his ongoing engagement with receptor signaling and microdomain biology. Dr. Sedaghat has accumulated over two decades of teaching and research in pharmacology, contributing as a professor, senior lecturer, editorial board member, and scientific officer in both pharmaceutical and cosmetic sectors. His current efforts bridge teaching in Toronto and ongoing research, including the development of an online GPCR-lipid raft database and investigation of bitter taste receptors’ roles beyond sensory systems. He remains driven by a commitment to rigorous science, data accessibility, and advancing the mechanistic understanding of GPCR pharmacology. Guest on the Web LinkedIn 7TMR-RAFT database Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Terry Kenakin About Dr. Terry Kenakin After obtaining a BSc in chemistry at the University of Alberta Edmonton Canada, Terry received his Ph.D. in Pharmacology from the University of Alberta, Department of Chemistry, Canada. Dr. Kenakin then moved to the UK, where he did a post-doctoral fellowship in University College London with Sir James Black. His next stop took him to Burroughs-Wellcome (BW) in Research Triangle Park (RTP) in North Carolina USA. After 7 years at BW, Dr. Kenakin joined Glaxo Inc in RTP where he remained for 25 years through iterations of Glaxo Inc, GlaxoWellcome , and finally GlaxoSmithKline . Since 2011, Terry works at the Department of Pharmacology at the University of North Carolina School of Medicine Chapel Hill NC. His interests are in receptor pharmacology, allosteric protein function, and drug discovery. Dr. Terry Kenakin on the web LinkedIn UNC Department of Pharmacology Amazon ResearchGate Pubmed . Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Richard Premont About Dr. Richard Premont "Dr. Premont obtained his B.S. in Biology and Chemistry at the California Institute of Technology in 1985, and M.Ph . and Ph.D. in Biomedical Sciences (Pharmacology) at Mount Sinai School of Medicine (City University of New York) in 1990 and 1992, working with Ravi Iyengar on regulation/desensitization of the liver glucagon receptor and glucagon-stimulated adenylyl cyclase system. In 1992, he won a Helen Hay Whitney Foundation fellowship to support his post-doctoral work with Robert Lefkowitz and Marc Caron at Duke University. His initial project to identify and clone taste receptors was unsuccessful, but led to the identification of GRK5 and continued focus on GRKs (particularly GRKs 4,5,6) and arrestins as GPCR regulators and as mediators of distinct signaling pathways through partners including GIT1. In 1999, obtained an independent faculty position at Duke in Gastroenterology, where he remained until 2018 studying GPCRs and their signaling pathways in the liver and in liver disease. In 2018, he moved to Harrington Discovery Institute and Case Western Reserve University, where he studies GPCR regulation by S-nitrosylation. My research focus is on understanding how distinct cellular signaling pathways interact and are coordinated to produce integrated physiological responses, and how dysregulation of this coordination results in pathophysiology. For this, we have worked in three main areas: the regulation of G protein-coupled receptor signaling particularly by the G protein-coupled receptor kinase (GRK) – beta-arrestin system, the coordination of heterotrimeric G protein, small GTP-binding protein and protein kinase pathways by GIT/PIX scaffolding complexes during cellular signaling, and characterizing the role of protein S-nitrosylation as a signaling post-translational modification in mediating and regulating cellular signaling pathways, particularly in conjunction with better characterized signaling systems. In our work, we utilize methods including structural biology and proteomics, molecular biology and biochemical enzymology, primary and model cell culture, and transgenic, knockout, knock-in and conditional models of mouse physiology and behavior." Dr. Richard Premont on the web Google Scholar LinkedIn Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Bruno Giros About Dr. Bruno Giros Dr. Giros' lab investigates how molecular changes at the nerve synapse might impact integrated behavior and what we might learn from these mechanisms to cure mental illness. After doctoral training at the Pierre and Marie Curie University in Paris and a short internship at Genentech Inc. in South San Francisco, he joined the CNRS as a Research Fellow in 1987 in the INSERM Laboratory directed by Jean-Charles Schwartz in Paris, where he cloned and characterized dopamine D2 and D3 receptor subtypes. From 91 to 94, he was an assistant professor at Duke University in North Carolina, working with Marc Caron and Robert Lefkowitz (2012 Nobel Prize in Chemistry) to characterize several neurotransmitter transporters and kinases and establish the first knock-out for these genes. In 1999, in France, Dr. Giros created the INSERM/CNRS laboratory on the "Neurobiology of Psychiatric Disorders," first in Créteil with Marion Leboyer, then at the University of Paris-Sorbonne with Hervé Chneiweiss. Since 2008, he has arrived at McGill University as a Canada Research Chair. At McGill, his laboratory has two main axes of research: 1) Studying interindividual vulnerability to chronic stress and depression and; 2) Understanding the role of phenotypically defined subpopulations of striatal neurons in motor and cognitive functions. Bruno Giros has trained 59 master's, doctoral and postdoc students, most of his trainees obtain positions in the academic or private sectors or are currently pursuing postdoctoral research training or have entered medical studies. Dr. Giros has published more than 200 publications with an H factor of 79 and 32,000 citations (Google Scholar) and has received several distinctions, including the CNRS silver medal, the FRM "Young Researcher" prize, the ISI “Highly Cited” and F-1000 in Pharmacology, and recently received the Heinz Lehmann Award from the Canadian College of NeuroPsychopharmacology and the distinguished James B. McGill Professor Award. Dr. Bruno Giros on the web Dougles Research Center LinkedIn Google Scholar Researchgate Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Thomas P. Sakmar About Dr. Thomas P. Sakmar Tom Sakmar is a physician-scientist and professor at Rockefeller University in New York. While a chemistry undergraduate student at the University of Chicago, he attended a NATO Advanced Study Institute in Les Houches, France in 1979 where he was exposed for the first time to the nascent field of membrane biophysics and intercellular communication. Instructors at the course included Marc Chabre , Harden McConnell , Richard Henderson , Martin Rodbell , Jean-Pierre Changeux , and Martin Karplus . After medical school and clinical training at Massachusetts General Hospital, Tom joined the laboratory of H. Gobind Khorana at the Department of Chemistry at M.I.T. for postdoctoral training, where he learned gene synthesis, cDNA cloning, site-directed mutagenesis, and heterologous expression in mammalian cells. Khorana’s lab made early key contributions and developed strategies to express, reconstitute and assay engineered GPCRs using the visual pigment rhodopsin as a model system. Tom initially focused on structure-activity relationships underlying spectral tuning and identified a glutamic acid residue in rhodopsin that serves as the retinylidene Schiff base counterion. He also went on to discover a “counterion switch” in visual pigments and to develop strategies to assay receptor-G-protein interactions and activation kinetics. After moving to Rockefeller University with a Howard Hughes Medical Institute appointment, Tom advanced a series of novel biochemical and biophysical assay platforms, including FTIR and Raman microprobe spectroscopy to study micro-quantities of expressed visual pigment mutants. This work involved active long-term collaborators, including Richard Mathies and Fritz Siebert , and contributed substantially to elucidating the physical chemistry of spectral tuning, and to a better understanding of the molecular mechanism of activation of GPCRs. Many of the conceptual advances that stemmed from this work, such as the concept of “functional micro-domains” and the “helix movement model of receptor activation” were confirmed later when crystal structures became available. Tom’s lab also pioneered the early use of computational homology modeling, molecular dynamics simulations and coarse-grain sampling approaches for membrane proteins in collaborations with Thomas Huber , Xavier Periole , and Siewert-Jan Marrink . Tom’s lab also developed an amber codon suppression method to genetically encode unnatural amino acids into membrane proteins expressed in mammalian cell culture. The genetic code expansion strategy for unnatural amino acid mutagenesis is a key enabling technology for the field and is being used by many laboratories. Early applications included “targeted photo-crosslinking,” and more recently, the parallel development of bioorthogonal labeling strategies to couple fluorophores to expressed receptors and other membrane proteins has allowed the creation of novel sensor constructs and single-molecule detection strategies. Recently, Tom’s lab discovered, along with Yu Chen and Ping Chi , that a mutant of CYSLTR2 is a driver oncogene in uveal melanoma, the most common eye cancer in adults. The CysLTR2 oncoprotein displays biased constitutive activity – it activates Gq/11 but does not undergo β-arrestin-mediated down-regulation. Dr. Thomas P. Sakmar on the web LinkedIn ResearchGate Pubmed ORCHID Google Scholar Rockefeller University Wikipedia Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Paul J. Gasser About Dr. Paul J. Gasser " I received my BS and MS in Zoology & Physiology at the University of Wyoming, where I studied signaling processes involved in light-induced regulation of melatonin synthesis in the rainbow trout pineal organ, a directly photosensitive endocrine organ. I received my PhD in Biology at Arizona State University, where I worked in the lab of Miles Orchinik, studying cellular mechanisms underlying non-genomic actions of corticosteroid hormones. My postdoctoral work, conducted at the University of Bristol, UK, in Christopher Lowry's lab, examined the role of organic cation transporter 3 (OCT3) in the regulation of monoamine signaling in the brain. I joined the faculty of Biomedical Sciences at Marquette in 2007. I teach undergraduate Biochemistry and a variety of graduate neuroscience courses. Research in my lab is currently focused on understanding the signal transduction pathways activated by beta-adrenergic receptors localized to the inner nuclear membrane and their role in the regulation of gene expression." Dr. Paul J. Gasser on the web Gasser Lab Marquette University Google Scholar ResearchGate LinkedIn Twitter Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

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

<< Back to podcast list Strategic Partner(s) Dr. Andrew Tobin About Dr. Andrew Tobin Andrew Tobin studied Biochemistry at Queen Mary College, the University of London obtaining first-class honors before studying for a Dr. Phil at the University of Oxford. Following a post-doctoral period at Bristol Myers Squibb in Princeton USA, Andrew returned to the UK to establish his own laboratory at the University of Leicester. Funded through three consecutive Wellcome Trust Senior Research Fellowships Andrew established a reputation in the field of receptor signaling. Now at the University of Glasgow, his primary research interests are focused on the rational design of novel drugs to treat the three global health challenges of dementia, asthma, and malaria. In this Andrew runs a research laboratory of around 15 staff supported by basic research grants investigating aspects of disease biology and the action of drugs in the context of disease. The vehicle by which Andrew is translating fundamental findings to commercial products is Keltic Pharma Therapeutics Ltd , a biotechnology company co-founded by Andrew with series A funding from the European Union. Andrew is also the Director of the Advanced Research Centre (ARC) a collaborative initiative at the University of Glasgow underpinned by a £118M new build that will house over 550 researchers designed to drive interdisciplinary research. Dr. Andrew Tobin on the web University of Glasgow ResearchGate Google Scholar Twitter Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Prasenjit Saha About Dr. Prasenjit Saha I conducted my doctoral research at the Indian Institute of Science, Bangalore, India, to investigate the mechanisms behind rare mitochondrial diseases, which can lead to heart failure, muscle fatigue, and neurodegenerative disorders. I am now working at the Cleveland Clinic in Ohio, USA, studying the gut microbiome and its impact on cardiovascular disease (CVD). Specifically, I am interested in understanding dysregulated G-protein coupled receptor (GPCR) signaling linked to atherosclerosis and diabetes. My research goal is to identify novel cellular target receptors of human gut microbe-derived metabolites that are pathologically linked to CVD. Discovering these receptors would be a significant breakthrough in cardiovascular biology as they could be targeted for therapeutic purposes. During my post-doctoral research, I was part of a study that identified the receptors of a novel human gut microbe-derived metabolite called phenylacetylglutamine (PAG), which is linked to cardiovascular disease. This study demonstrated that PAG is a potential diagnostic marker for CVD as it causes serious fatal conditions such as thrombus formation, which can block blood vessels. In this study, I discovered adrenergic receptors (α2A, α2B, and β2-adrenergic receptors) that serve as the gut microbial metabolite (PAG) receptor and characterized the receptor-metabolite interaction. More recently, I have shifted my focus to identifying allosteric modulators of host G-protein-coupled receptors (GPCRs) that contribute to cardio-metabolic disorders. Traditional drug discovery efforts have focused on agonists and antagonists that bind to the orthosteric site of the receptor. However, the pursuit of allosteric modulators has gained attention as they have the potential to fine-tune cellular responses with greater selectivity among the subtypes of GPCRs. My long-term plan is to conduct research in the field of receptor biology, with a focus on GPCRs. They are the largest, most versatile, and most ubiquitous class of plasma membrane receptors and serve as targets for more than one-third of all prescribed drugs currently used in the treatment of human diseases all over the world. Dr. Prasenjit Saha on the web Google Scholar Pubmed LinkedIn Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Elva Zhao About this episode Elva is currently a research fellow at the Monash Institute of Pharmaceutical Sciences. Elva moved to Canada where she obtained her Ph.D. at the University of Western Ontario, working on the regulation of G proteins signaling by accessory proteins, such as RGS proteins and GPSM proteins. After her Ph.D., she moved to Australia and continues working on GPCRs. Her current research focuses on class B GPCRs and understanding how GPCR signaling and function is mediated by various ligands, binding partners, and intracellular machinery. In her spare time, Elva likes to run in the mountains, play with Tilly (a 9-year old retired greyhound), collecting mini shoes, and hang out with friends. Join me to learn more about Elva, class B GPCRs, and Tilly. Dr. Elva Zhao on the web LinkedIn Monash University Pubmed Twitter Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Caron Tribute Part 3 About Marc Caron Dr. Caron and his family moved to Durham, NC in 1977, following receipt of his BSc in Chemistry from Laval University and his Ph.D. from the University of Miami. He joined the faculty of Laval University School of Medicine in 1975 and then returned to join Duke’s faculty, where he remained as a James B. Duke Professor until his death. He and his laboratory members studied the mechanisms of action and regulation of hormones and neurotransmitters and how they might underlie brain and behavior disorders such as schizophrenia, Parkinson's disease, attention-deficit hyperactivity disorder, mood disorders, and addiction. Among his many honors, Dr. Caron was an investigator of the Howard Hughes Medical Institute from 1992 to 2004, a member of the American Academy of Arts & Sciences, a fellow of the American Association for the Advancement of Science, and a recipient of the Julius Axelrod Award. An authoritative and prolific scientist, with over 650 scientific publications, he is most beloved as a mentor and his relentless encouragement that shaped the careers of hundreds of scientists worldwide. About our panelists in alphabetical order and the year they first met Dr. Caron Dr. Jean Martin Beaulieu (2003) Dr. Laura Bohn (1999) Dr. Kathleen Caron - Co-host- (1970) Dr. Henrik Dohlman (1987) Dr. Kafui Dzirasa (2006) Dr. Yasushi Masuda (2004) Dr. Marco Pardo (2002) Dr. Vania Prado (2002) Dr. Amy Ramsey (2008) Dr. Bryan Roth (current) Dr. Ali Salahpour (2007) Dr. Lauren Sloksy (2020) Dr. Josh C Snyder (2012) Dr. William Wetsel (current) Memories our panelists shared with us https://video.wixstatic.com/video/93ce84_656bd30f2f964a8bbfc27d4b7815c38d/1080p/mp4/file.mp4 Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Patrick Sexton About Dr. Patrick Sexton Patrick Sexton is a Professor of Pharmacology, National Health and Medical Research Council of Australia Senior Principal Research Fellow, and Director of the Australian Research Council Centre for Cryo-electron Microscopy of Membrane Proteins ( www.ccemmp.org ). He is a leader in the study of GPCRs, biased agonism, and also on allosteric interactions between GPCRs and other proteins and small molecule ligands. More recently, his team has been at the forefront of the application of cryo-EM to elucidate of the structure and dynamics of GPCRs. Prof. Sexton has published over 320 peer-reviewed journal articles and has been cited >26,000 times (Google Scholar). He is a 2021 Clarivate Analytics Highly Cited Researcher in two disciplines: Pharmacology & Toxicology and Biology & Biochemistry, a corresponding member of the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification, and a member of the Faculty of 1000 (Molecular Pharmacology division) and an elected Fellow of the British Pharmacological Society (BPS). Prof. Sexton’s awards include the Australasian Society for Clinical and Experimental Pharmacologists and Toxicologists (ASCEPT) Lecturer award, Endocrine Society of Australia Senior Plenary award, Rand Medal (ASCEPT), Paxinos-Watson Award (Australian Neuroscience Society), Vane Medal (BPS), Gordon Hammes Lectureship Award (American Chemical Society) and the GSK Research Excellence award. Prof. Sexton is also a co-founder of the San Francisco-based biotechnology company Septerna Inc . Dr. Patrick Sexton on the web CCeMMP Monash University Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Claudia Stäubert About Dr. Claudia Stäubert "I received my degree in biochemistry from Leipzig University (Germany) being already fascinated by G protein-coupled receptors (GPCRs) due to a stay as a scholarship student in the lab of Thue Schwartz (Copenhagen, Denmark). This fascination accompanied me and repeatedly challenged me ever since. During my Ph.D. at the International Max Planck Research School “The Leipzig School of Human Origins”, I focused on the evolutionary aspects of GPCRs. As a postdoc in the lab of Anders Nordström (Umeå, Sweden), I broadened my methodical and scientific horizon and focused on cellular metabolism and drug resistance phenomenon applying metabolomics analyses. Since 2014, I have led a research group at the Rudolf Schönheimer Institute of Biochemistry in Leipzig (Germany). We focus on several aspects of metabolite-sensing GPCRs including signal transduction, intracellular trafficking, and evolution. Our ultimate goal is to understand their role in immune cell function and cancer cell metabolism. " Dr. Claudia Stäubert on the web Stäubert Lab, Rudolf Schönheimer Institute of Biochemistry Leipzig LinkedIn ResearchGate ORCID ResearcherID Scopus Author ID Google Scholar PubMed Twitter Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick recap Yamina and Claudia had a wide-ranging discussion about Claudia's work on metabolites and their effects on the system. They also discussed the challenges of studying metabolites and their receptors, the relationship between metabolites, gut health, and disease progression, and Claudia's career journey in academia. They also explored the possibility of developing an ecosystem for the GPCR University. Summary Interview and Social Media Planning Yamina, from Dr. GPCR, discussed with Claudia, a guest from the Schiller Institute at Campstream, about Claudia's work and future plans. Yamina mentioned that they would use their discussion as a basis for crafting social media posts. Claudia, who has an interest in metabolites and their effects on the system, agreed. Yamina also pointed out that Claudia was their first guest of the year, indicating the start of a new series of interviews. Affordable Childcare and GPCR Research Discussion Yamina and Claudia discussed the importance of affordable childcare and the experiences of PhD students in the US and Europe. Claudia shared her experiences working in Sweden and Germany, and how she secured funding for her research on the effects of metabolites on GPCRs. Yamina expressed interest in attending a meeting about GPCRs and metabolism in the UK, but was unsure if she could make it due to travel constraints. Metabolite Activation of GPCRs: A Fascinating Discovery Claudia and Yamina discussed the role of metabolites in activating GPCRs, a process that they found fascinating. Yamina expressed interest in learning more about this topic as she realized her lack of knowledge on metabolite recognition or binding to GPCRs. Claudia suggested possible next steps, including researching review articles or articles to gain a higher understanding of what is known about this process. Challenges in Studying Metabolites and Receptors Claudia and Yamina discussed the challenges of studying metabolites and their receptors, particularly in relation to fermented foods. They acknowledged the difficulty of distinguishing between different compounds and the effect of media on the cellular system. They also explored the potential for better tools to understand and discover new metabolites or receptors. Yamina suggested the possibility of using native cells with optimized media, but Claudia highlighted the complexity of the system. They briefly touched upon the link between GPCRs and diseases, such as diabetes, but did not delve into detail. Metabolites, Gut Health, and Disease Progression Yamina and Claudia had a discussion about the relationship between metabolites, gut health, and disease progression. Yamina proposed that the metabolites in the gut of a non-healthy person might be different from those of a healthy person, which could affect receptor activity. Claudia agreed, suggesting that the complexity of the gut microbiome is akin to a "complicated city vicus". Yamina shared an example she heard in a podcast about fecal transplants and the relationship between the gut, brain, and metabolism. Both agreed on the complexity of the topic, with Claudia concluding that diseases might first affect the metabolites and not necessarily lack inherited genes. Academia, Career Journeys, and Advice Yamina and Claudia discussed Claudia's career journey in academia. Claudia shared her experiences and her love for her work, emphasizing the importance of research and learning in academia. Yamina highlighted the challenges of career choices, especially when family situations are involved. Claudia also mentioned the significant experiences that shaped her career trajectory, such as her time in an assurance lab and her trip to Sweden. Towards the end, Claudia offered advice to junior scientists, suggesting that they explore different fields and meet a variety of people to find their interests. She also mentioned her team's job openings and where people could find more information. Developing a Research Ecosystem at GPCR University Yamina and Claudia discussed developing an ecosystem for the GPCR University, with the goal of providing a central hub for researchers in the field. Yamina emphasized its vision for the platform to be a place where researchers can find content, ask questions, and collaborate, thereby avoiding the repetition of unsuccessful studies. They also touched on the potential for funding from external sources. Claudia briefly mentioned a recommendation from the Committee on Petitions. Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Exploring Career Paths in GPCR Research with Dr. Jacek Mokrosiński About Dr. Jacek Mokrosiński "Jacek is a Senior Scientist at Novo Nordisk specializing in molecular pharmacology and cell-based screening technologies. He works in a multidisciplinary Chemical Biology team based at the recently established US R&D hub in Lexington, MA. Originally from Łódź, Poland, Jacek completed his Master's degree in Biology, specializing in Biochemistry at the University of Łódź. He then moved to Denmark, where he trained at the University of Copenhagen under supervision of Professor Thue W. Schwartz, and worked closely with Dr Birgitte Holst studying structural and mechanistic properties of ghrelin receptor and GPCRs involved in regulation of metabolism. After completing his Ph.D., he pursued research in genetics of metabolic regulation at the Institute of Metabolic Science - Metabolic Research Laboratories at the University of Cambridge in the team led by Professor I. Sadaf Farooqi. His research aimed at understanding molecular mechanism through which rare genetic variation may lead to or protecting from excessive body weight gain. As part of Farooqi's team, he characterized a series of novel human genetic variants identified in several GPCRs associated with obesity and other metabolic diseases, including GPR10, Melanocortin 4, Serotonin 2C and TRH receptors. Since 2021, Jacek has been working at Novo Nordisk at its research sites in the UK (Oxford) and the US (Indianapolis, Indiana and most recently Lexington, Massachusetts). He is passionate about cell-based in vitro technologies to study mechanistic properties of GPCRs and understanding the dynamics of receptor signalling. He is an avid proponent of close collaboration between industry and academia." Dr. Jacek Mokrosiński on the web ORCID ResearchGate LinkedIn Twitter Dr. GPCR AI Summary AI-generated content may be inaccurate or misleading. Always check for accuracy. Quick Recap Yamina and Jacek discussed their experiences with name mispronunciations, cultural differences, and the importance of a multidisciplinary approach in drug development. They also shared their career journeys, emphasizing the value of being open-minded, proactive, and embracing new opportunities. Lastly, they discussed their research interests, particularly in the field of GPCR, and the importance of method development, integrity, and honesty in scientific research. Next Steps Jacek will collaborate with Alex Romeo on a podcast about transitioning to the industry. In future talks and interviews, Jacek will share his stories and advice about GPCRs. Yamina will schedule a future talk with Jacek about GPCRs as therapeutic modalities. Summary Embracing Cultural Differences and Collaboration Yamina and Jacek shared their experiences with name mispronunciations and variations and discussed the importance of embracing cultural differences. They also discussed their professional backgrounds, highlighting the benefits of a multidisciplinary approach in drug development and the importance of collaboration between academia and industry. They talked about their shared passion for advancing science and improving patient outcomes, and their early interests in science and chemistry. They also shared their appreciation for documentaries showcasing manufacturing processes and the value of true experimentation in scientific research. Jacek's Career Journey and Advice Jacek and Yamina discussed Jacek's career journey, focusing on his experiences, challenges, and lessons learned. Jacek highlighted the importance of being open-minded and proactive, emphasizing that he learned by doing rather than taking specific courses. He also underscored the role of the people around him, expressing gratitude for their guidance and support. His advice was to be ready for changes and to embrace opportunities as they arise. Jacek's career path, which led him from Poland to Denmark and then to the US, exemplified his advice in action. Passion for Science and Career Journeys Yamina and Jacek discussed their passion for science and how it led them to their current careers. Jacek shared his experience of working with Piketa and how he found a job in Seda's lab at Cambridge, where he could immediately contribute due to his technical skills. Yamina agreed with Jacek's sentiments and spoke about her own journey, expressing her happiness in discussing science and reading papers. They emphasized the importance of finding a job that aligns with one's interests and strengths and being open to opportunities. They also highlighted the need for a work-life balance and the joy of a well-done job. Embracing Networking for Professional Growth Jacek and Yamina discussed the importance of building a network and being open to new opportunities. Jacek realized that being introverted doesn't mean he can't benefit from networking and interaction with others. He also highlighted the benefits of attending conferences and engaging with colleagues, sharing examples of how such interactions led to collaborations and new opportunities. Yamina agreed, emphasizing the importance of mental preparation and embracing different social situations, both virtual and in-person. They underscored the value of these interactions for professional growth and encouraged others to adopt a proactive approach to networking. Building Professional Connections Strategies Yamina and Jacek discussed the importance of building professional connections and strategies for introducing oneself to potential contacts. They emphasized the need to be mindful of the other person's time, provide clear explanations for the purpose of the connection, and offer something of value in return. They also highlighted the advantages of using LinkedIn as a tool for networking and the significance of personalizing messages to make a lasting impression. GPCR Research Interests and Collaborations Yamina and Jacek had a deep and engaging discussion about their research interests and achievements, particularly in the field of GPCR. Jacek shared his fascination with the growth hormone secretion receptor and the melanocortin 4 receptor, and their roles in regulating body weight and growth. Yamina, in turn, talked about her work on melanocortin receptors and an upcoming collaboration with a postdoc scientist. They also highlighted the importance of method development, integrity, and honesty in scientific research. The discussion revealed their interest in GPCRs as therapeutic modalities and possible future collaborations. Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Matthew Eddy About Dr. Matthew Eddy Matthew Eddy earned his BA in Chemistry from Oberlin College, where he trained with solid-state NMR expert Professor Manish Mehta . He then earned his Ph.D. in physical chemistry from the Massachusetts Institute of Technology, training under the mentorship of Prof. Robert Griffin . Following this, Dr. Eddy began learning and investigating human GPCRs while training in the laboratories of Professors Raymond Stevens and Kurt Wüthrich at The Scripps Research Institute. Dr. Matthew Eddy on the web Website Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Daniel Isom About Dr. Daniel Isom "Dan was born and raised in the Cleveland area. He is a first-generation college graduate and academic. After spending two years at the Cleveland Institute of Art, he earned degrees in Biochemistry and Chemistry from Case Western Reserve University. He then went on to earn a Ph.D. in Molecular Biophysics from Johns Hopkins University, followed by postdocs at both Duke University and UNC Chapel Hill. Dr. Isom was recruited to the Molecular and Cellular Pharmacology Department at the University of Miami Miller School of Medicine in 2016, where he is currently a practicing molecular pharmacologist and biophysicist, systems and synthetic biologist, technologist, heavy CRISPR user, protein sequence- and structure-based informaticist, computational geometer, virtual screener, and Python, medical, and graduate educator leading a talented and multidisciplinary research team. " Dr. Daniel Isom on the web Isom Lab University of Miami Miller School of Medicine LinkedIn X (Twitter) BlueSky Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Roger Sunahara About Dr. Roger Sunahara Professor Sunahara received his graduate training with Dr. Philip Seeman in the Department of Pharmacology at the University of Toronto. He later joined the laboratory of eminent biochemical pharmacologist, Dr. Alfred G. Gilman, at the University of Texas Southwestern Medical School as a post-doctoral fellow. His training has provided a strong foundation and appreciation for the applications of pharmacology, biochemistry and structural biology to delineate mechanisms of action. Professor Sunahara started his independent research career in the Department of Pharmacology at the University of Michigan Medical School, where he climbed the academic ladder. In 2015 Professor Sunahara moved his laboratory to the Department of Pharmacology at the University of California in San Diego. His main area of research focuses on the structural and pharmacological bases for hormone-mediated activation of G proteins by G protein-coupled receptors (GPCRs). The Sunahara lab utilizes biochemical, biophysical and pharmacological methodologies to study GPCR-G protein interactions. These approaches were invaluable to resolve the crystal structure of the beta2-adrenergic receptor (beta2AR)-G protein complex, team effort with long time collaborator Brian Kobilka . The structure was first snapshot of the agonist- and G protein-bound GPCR, providing valuable models for agonist-mediated activation of G proteins. We continue to utilize these data to better understand the basis for receptor-G protein specificity and agonist efficacy. Our mission is to understand the mechanism and structural bases for ligand binding and efficacy to help optimize the design and engineering of more efficacious therapeutics. This is an important perspective in the pursuit of receptor subtype-specific ligands, a major aspect to achieve safer, on-target therapeutics. One example of our recent work surrounds a structure-based effort to develop ligands that specifically target the beta2AR above all other adrenergic receptor isoforms. Our goal is to develop safer beta2AR-selective ligands for the treatment of asthma and acute rescue therapy for anaphylaxis. We also study non-canonical sites, those outside of the native hormone, or orthosteric, binding sites. We have identified several GPCR ligands that allosterically modulate orthosteric ligand binding and target sites that are often located in regions that display higher sequence variability among receptor subtypes. Again, our intention is to target specific receptor subtypes. The structural work on the GPCR-G protein complexes have also revealed some unprecedented conformational changes in G protein structure. Some of these changes are associated with G protein activation while the functional consequences of other structural changes remain elusive. More recently we have have been heavily engaged in studies to address the functional role of these dramatic conformational changes and the relationship to disease. Some of these studies resolved a major question regarding the signaling differences in G protein splice forms, specifically the short and long forms of the stimulatory G protein, Galpha-s(s) and Galpha-s(l), respectively. We demonstrated that Galpha-s(l), but not Galpha-s(s), regulates extracellularly regulated kinases (ERK), and that this long isoform is tied to a devastating blood disorder, myelodysplastic syndrome (MDS). We speculate that these aberrations in Galpha-s(l), specifically, may be involved in other pathologies such as cancer. The Sunahara lab has also been developing protein-based therapeutics using structure-guided design and validation. A notable therapeutic is an enzyme that hydrolyzes cocaine. Through structural and computational approaches the Sunahara lab and collaborators developed a thermostable form of the enzyme that has recently progressed through Phase II clinical trials as an antidote for cocaine overdose. The laboratory continues to engineer the enzyme to optimize its potential as a treatment for cocaine abuse, a debilitating disease that would require long-term and sustained therapeutic actions. Dr. Roger Sunahara on the web UCSD Profile Google Scholar ResearchGate LinkedIn Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Brendan Wilkins About Brendan Wilkins "Brendan completed his undergraduate training at the University of New South Wales (UNSW) Sydney, Australia in 2016 with first class Honours in Pharmacology. In his Honours year, Brendan explored small molecule allosteric modulators of the β2-adrenoceptor under the tutelage of Dr Angela Finch. Since then, Brendan worked as a research assistant at the Victor Chang Cardiac Research Institute where he investigated the orphan G protein-coupled receptor (GPCR), GPR37L1. Brendan is now a final year PhD candidate in the Orphan Receptor Laboratory headed by Associate Professor Nicola J Smith at UNSW Sydney, Australia. Brendan’s PhD project focuses on the orphan GPCR GPR146. This project aims to characterise the molecular pharmacology of GPR146 and to validate the proposed ligands of GPR146 in line with IUPHAR-NC guidelines on deorphanisation of orphan GPCRs. Brendan is currently looking for post-doctoral positions to begin in mid-2024" Brendan Wilkins on the web UNSW Sydney Google Scholar ResearchGate LinkedIn Twitter Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Discover how Celtarys Research is transforming GPCR assay development with fluorescent ligands in this episode featuring CSO Dr. Maria Majellaro—and learn what their new partnership with Dr. GPCR means for the global research community. << Back to podcast list Strategic Partner(s) Custom Molecules, Fluorescent Probes: When Chemists Think Like Biologists with Dr. Maria Majellaro from Celtarys A Partnership Rooted in Scientific Innovation In this episode, Dr. Maria Majellaro, CSO of Celtarys Research, shares the story behind the company’s journey from academic curiosity to biotech force. But this conversation also marks something new: a strategic partnership between Dr. GPCR and Celtarys, built on a shared commitment to empowering the GPCR research community. At Celtarys, the focus is on enabling fast, customizable development of fluorescent ligands and chemical probes for GPCR assays. What started as a PhD project has grown into a commercial technology that helps scientists interrogate receptor pharmacology with greater speed and flexibility. “We started with GPCRs, but now we’re expanding to many new targets. Every time, it’s a new world—and we’re still learning.” — Maria Majellaro Through this partnership, Celtarys becomes an integral part of the Dr. GPCR ecosystem, contributing both expertise and tools that align directly with the needs of scientists at the bench and in translational drug discovery. Decision-Making: From Researcher to Scientific Leader Maria’s story is one of trusting her instincts while embracing change. She began as a medicinal chemist in Italy, but a postdoc opportunity in Santiago de Compostela—and a mentor’s timely suggestion—changed her trajectory. When the time came to decide whether to leave the lab and lead Celtarys into biotech, she took the leap. “It was my shift from the lab to leadership. I wasn’t sure at first, but I realized I could do this too.” — Maria Majellaro Her decisions, often made intuitively rather than analytically, have led to key inflection points—including Celtarys’ formal launch in 2021, just as the world was emerging from the pandemic. Now, she leads a team of six scientists and continues to build momentum through collaborations like the one with Dr. GPCR. Translating Science into Business Like many scientists-turned-entrepreneurs, Maria faced the challenge of learning the business side of biotech on the fly. Celtarys had the technology—but not the roadmap for commercialization. That changed with support from Galicia’s robust biotech network, and the company quickly defined its value: building better tools for drug discovery assays. “As scientists, we know how to make molecules. But we had to learn everything else—IP, market positioning, customer discovery.” — Maria Majellaro This year, as part of its partnership with Dr. GPCR, Celtarys will bring those lessons to the broader community, providing insight into assay development, probe design, and the realities of scaling innovation from lab bench to product launch. The Complexity Behind Every “Successful” Probe Maria is candid about the technical challenges behind fluorescent ligand development. “It’s not just attaching a fluorophore,” she says. Each probe must retain activity, remain soluble, and be compatible with a given assay format. There were moments of doubt and repeated optimization. The payoff? Enabling companies and academic labs to avoid the costly dead ends often associated with probe development. “You can have a great ligand—but if you can’t solubilize it, it’s useless.” — Maria Majellaro Celtarys’ unique chemical platform shortens development timelines and allows tailored modifications—critical for labs starting new GPCR-related projects. Their work directly supports the tool-building mission that aligns with the Dr. GPCR ecosystem. Pivoting: From Chemistry Company to Discovery Partner Initially focused on tool production, Celtarys has evolved into something more: a scientific collaborator. Their approach is highly consultative—they don’t just sell ligands, they co-develop solutions. The company works with clients from pharma, CROs, and academia, including MD Anderson and several leading GPCR labs. “We always start with the problem, then generate the right compound using our chemistry. It’s about enabling biology.” — Maria Majellaro Through its partnership with Dr. GPCR, Celtarys will expand its visibility and impact—offering its expertise, tools, and real-world insight to researchers tackling today’s most pressing GPCR-related questions. Key Takeaway This episode is more than a conversation—it’s the official kickoff of a one-year partnership between Dr. GPCR and Celtarys. Together, we’re combining chemistry, biology, and business insight to empower the GPCR research community like never before. Whether you're designing assays, developing probes, or seeking better tools for GPCR drug discovery, Celtarys and Dr. GPCR are now working hand-in-hand to help you do it faster, better, and more reproducibly. About Maria Majellaro Dr. Maria Majellaro obtained her PhD with the distinction of Doctor Europeus from the Department of Pharmacy at the University of Bari (Italy) in 2018. During her doctoral studies, she spent one year as a predoctoral visiting student at the CIQUS Research Center—Campus of International Excellence—in Santiago de Compostela (Spain). In 2018, she returned to CIQUS to work as a Postdoctoral Research Associate in the group of Prof. Eddy Sotelo, where together with Dr. Jhonny Azuaje they laid the groundwork for the future creation of Celtarys Research. Since the founding of Celtarys in 2021, she has served as the company’s Chief Scientific Officer, leading all scientific activities—from the development of Celtarys’ proprietary products to the ideation and execution of custom research projects. She also oversees the company’s scientific collaborations across Europe and beyond, being responsible for securing and managing national and international research grants. To date, she has successfully led seven funded projects. Her scientific expertise is rooted in organic synthesis and medicinal chemistry, with a particular focus on GPCR modulators. She has played a central role in the development and validation of Celtarys’ proprietary synthetic technology and is both a co-author of the related patent and a co-founder of the company. Maria Majellaro on the web LinkedIn ResearchGate Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Alessandro Nicoli shares how he models olfactory GPCRs with AlphaFold, mentors students, and builds science from scratch in a new lab. A fresh look at computational GPCR research. << Back to podcast list Strategic Partner(s) Smells Like GPCR Spirit: Cracking Olfactory Codes with Alessandro Nicoli The Accidental Path to Science Alessandro Nicoli didn’t grow up knowing he’d be a scientist. Like many, his path to GPCR research wasn’t linear—it evolved through academic exploration and mentorship. “I think I don’t have a linear trajectory… the beauty of seeing molecule design and reactions—thinking you can create molecules—was really exciting.” – Alessandro Nicoli He studied pharmaceutical chemistry in Padua, where his fascination with molecular design first took shape. But it wasn’t until meeting an inspiring professor, Prof. Moro, that he truly saw how molecules could go beyond the bench and interact with biology in powerful ways. The Moment Chemistry Met Biology Nicoli’s turning point came when he realized that molecules weren’t static—they could act , bind , and modulate biological targets. “It was not just a molecule—it was a partner that goes to interact with something else… a protein, DNA, RNA. That opened up a new world.” – Alessandro Nicoli That early spark led him to discover the role of medicinal chemistry and, eventually, molecular modeling. For Nicoli, chemistry became more than reactions—it became a bridge to biological insight. Falling for Computational Chemistry The "second academic love" arrived during his master’s thesis, where Nicoli dove into computational chemistry. “I got to know computational chemistry through a project on BCL2 proteins and drug discovery… I was in love with the topic.” – Alessandro Nicoli Working on docking and NMR studies for cancer-related proteins, he discovered the power of simulation in revealing molecular interactions. That experience convinced him to pursue a PhD and deepen his computational skills—eventually leading him to GPCRs. Finding the Right Mentor and Lab A birthday email changed everything. Professor Moro forwarded a PhD opening from Prof. Antonella Di Pizio’s lab in Munich. It felt serendipitous—and it was. “We had a super match… and after a month, I was already in Germany. I was her first PhD student.” – Alessandro Nicoli Starting from scratch in a young lab wasn’t easy, but it created a unique bond between PI and student. Nicoli thrived in this setting—helping shape the lab and its direction, particularly in computational studies of olfactory GPCRs . GPCRs, Receptors of Infinite Variety When asked about his favorite GPCR, Nicoli refused to pick. “Let’s embrace the challenge to study all of them… they’re unique in how they bind ligands, how selective they are.” – Alessandro Nicoli He emphasized that olfactory receptors , while underexplored, present an incredible challenge. With hundreds of subtypes and very few known ligands, the structure–function relationships remain largely mysterious—and incredibly exciting for a computational chemist. AlphaFold: A Turning Point in GPCR Research When Nicoli began his PhD, AlphaFold hadn’t yet revolutionized the field. But once released, it changed everything. “AlphaFold gave us a face to those proteins… now we have 400 models to start with.” – Alessandro Nicoli He explained how AlphaFold’s predictions, surprisingly close to experimental structures, provided a powerful starting point for docking, dynamics, and ligand design—especially for receptors previously “invisible” to structural biology. Modeling the Invisible: Olfactory Receptors Nicoli’s work centers on predicting ligand binding and receptor behavior for olfactory GPCRs. “The main challenge was: how do we get a face for these proteins when we don’t have ligands?” – Alessandro Nicoli He shared a detailed case study of working on a specific odorant receptor (R5VK1), where they leveraged known active/inactive ligands to validate models through iterative refinement , molecular docking , and mutagenesis-guided optimization . The goal? Build predictive models to discover new ligands . Why Molecular Dynamics Matters For Nicoli, molecular dynamics is more than simulation—it’s how we watch biology move . “You simulate over time… see how receptors move in physiological conditions, with water, membranes, ligands.” – Alessandro Nicoli He emphasized that MD allows researchers to observe allosteric changes , mutation effects , and even ligand entry/exit paths , offering dynamic insights that static structures cannot. It’s a critical complement to experimental work. From Researcher to Mentor: Growing Together Outside his research, Nicoli mentors students, manages interns, and even lectures. Balancing this with a PhD isn't easy, but it’s deeply rewarding. “You have people that rely on you… but you grow together, and that’s the most powerful thing.” – Alessandro Nicoli He reflected on learning to delegate—how hard it was initially to hand over tasks—but how vital it is for team science. He now sees mentoring as a way to shape the next generation while evolving himself as a scientist. Advice, Tools, and the Future of GPCR Research Nicoli offered advice to wet-lab scientists curious about computational work: Start with passion. Learn Python. Explore online resources like “Talktorials.” “We’re living in a golden era for computational chemistry… the tools are out there. You just need the motivation to explore.” – Alessandro Nicoli As for what’s next? More structures, better tools, and deeper insights into the elegant, complex world of GPCRs. He sees a future where wet and dry labs converge , and where computational methods are fully integrated into GPCR drug discovery pipelines. Key Takeaway Alessandro Nicoli’s journey is a compelling example of how computational chemistry can unlock new frontiers in GPCR research , especially in complex areas like olfactory receptors. By bridging structural prediction, molecular dynamics, and ligand discovery, his work not only deciphers biological mysteries but also inspires a new generation of scientists to think computationally. About Alessandro Nicoli Alessandro Nicoli is currently a PhD student in the Molecular Modeling group led by Prof. Dr. Antonella Di Pizio at the Leibniz Institute for Food Systems Biology at the Technical University of Munich (Germany). He obtained an MSc degree in Chemistry and Pharmaceutical Technology from the University of Padua (Italy). His training and passion for computational chemistry started in 2019 during his time at the Molecular Modeling Section (MMS) under the supervision of Prof. Stefano Moro, where he worked on integrated Nuclear magnetic resonance (NMR) and computational modeling strategies to target the antiapoptotic BCL-2 protein family, key regulators of cell survival, using small molecules. He then moved to Germany in 2019 to pursue his PhD. His research focuses on a group of 400 transmembrane proteins known as olfactory receptors, which mediate the sense of smell. Beyond the olfactory epithelium, these receptors are expressed in various tissues, where they play important but not yet fully understood roles in various physiological and pathological processes. Despite their relevance, they remain understudied due to the limited knowledge of their ligands and the lack of experimental structures. Alessandro PhD work aims to fill these gaps by leveraging computational structure-based tools and develop specific protocols to accelerate OR ligand discovery and improve our understanding of olfactory function at the molecular level. Alessandro Nicoli on the web Leibniz Institute for Food Systems Biology at the Technical University of Munich Technical University of Munich Google Scholar Pubmed ORCID ResearchGate X Bluesky Github Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Oliver Hartley About Dr. Oliver Hartley Oliver Hartley is VP for Drug Discovery at Orion Biotechnology . He is the inventor of OB-002 as well as the key technology underlying Orion’s discovery platform. Trained as a biochemist, he completed a PhD in protein engineering (Cambridge, UK) with Sir Gregory Winter (Nobel Prize for Chemistry, 2018). Since then Oliver has worked at the University of Geneva, where his research on peptide engineering and GPCR pharmacology has led to a series of high-profile publications and new intellectual property, and at the Mintaka Foundation for Medical Research with a role as co-founder and Chief Scientific Officer. Dr. Oliver Hartley on the web LinkedIn Orion Biotechnology Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Françoise Bachelerie About Dr. Françoise Bachelerie " FB leads a team at Paris-Saclay University with expertise in immunology and virology related to Host/Virus interactions and GPCR function. The team’s projects are devoted to the activation/function of CXCR4-ACKR3 (CXCR7) receptors of the CXCL12 chemokine, key effectors of the immune system, including their role in immunological disorders (e.g. WHIM syndrome) and in the innate control of the life cycle of papillomavirus, which are commensal inhabiting the healthy human epithelium (virome) while presenting an oncogenic potential that remains a major health concern. FB is recognized for her expertise and pioneering works in the field of biological and pathological functions of chemokines and their receptors, for which she made important breakthroughs regarding the CXCL12/CXCR4/ACKR3 trio. In particular, FB contributed to the discovery that CXCL12 is the ligand for the CXCR4 receptor and can therefore prevent infection by the Human Immunodeficiency Virus (HIV). FB’ team has identified the orphan CXCR7/ACKR3 receptor as being the 2nd receptor for CXCL12, which behaves as a modulator of CXCL12/CXCR4 functions. FB is a member of various international committees in the field, including the one that reviewed the standard nomenclature for chemokine receptors that are categorized into a large subgroup of G protein–coupled (GPCR) leukocyte chemotactic receptors (including CXCR4), and a smaller subgroup of atypical chemokine receptors (including the CXCR7/ACKR3). " Dr. Françoise Bachelerie on the web INSERM ResearchGate SciSpace Loop LinkedIn Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Stuart Maudsley About Dr. Stuart Maudsley Stuart graduated from the University of Leeds in the U.K. with a First Class Honors degree in Pharmacology. At the end of his studies, he was awarded the Pfizer Prize for undergraduate research. He then completed his Ph.D. at Leeds as well as the University’s Ackroyd, Brotherton, and Brown Scholar. Following his Ph.D., Dr. Maudsley was awarded a Howard Hughes Medical Institute Fellowship to train with Professor Robert Lefkowitz at Duke University. Following this tremendous experience, he was recruited to be the Principal Investigator of the Receptor Biology Section at the Medical Research Council (MRC) -Human Reproductive Sciences Unit within the University of Edinburgh. At the MRC he developed novel prostate cancer therapeutics based upon his research into GPCR pluridimensional signaling. To broaden his biomedical skill-set Stuart next accepted the position of Head of the Receptor Pharmacology Unit at the National Institutes of Health – National Institute on Aging at the Johns Hopkins University Medical Center. At the NIH he was the recipient of the coveted NIH ‘Bench-to-Bedside’ Translational Research Grant Award, one of the few awards available within the intramural NIH program. Upon starting a new family, and returning to Europe, Dr. Maudsley continued his scientific journey with the award of the highly-valued Odysseus Program Type I Program Grant to work as both the Adjunct Director of the VIB Center for Molecular Neurology and also Vice-Chair of the Department of Biomedical Sciences at the University of Antwerp. Stuart’s current research, in the Receptor Biology Lab, focuses on the development of novel GPCR-based therapeutics that interdict diseases based on their gerontological underpinnings. This research stream is now forming the basis of a new technology-based start-up company, HeptOME , to help screen and develop novel longevity/disease-regulating compounds with multidimensional disease efficacy profiles. Dr. Stuart Maudsley on the web Maudsley Lab LinkedIn Google Scholar ResearchGate Maudsley Lab on Facebook Receptor Biology Lab Facebook Group Twitter Semantic Scholar Instagram Neurotree Dimensions Reddit Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Dr. Foord reflects on discovering RAMPs, deorphanizing GPCRs, and navigating industrial GPCR pharmacology, target validation, and drug discovery strategy. << Back to podcast list Strategic Partner(s) Dr. Foord: Serendipity, RAMPs, And Industrial GPCR Pharmacology Scientific Abstract This conversation traces how GPCR pharmacology, receptor signaling, and drug discovery evolved inside one of the world’s largest pharmaceutical organizations. Dr. Foord reflects on his path from academic neuroendocrinology to introducing molecular biology and molecular pharmacology into Glaxo’s GPCR programs, and on the combination of rigor, bioinformatics, and serendipity that led to several influential discoveries. He describes the purification and cloning of the CGRP receptor, the identification of receptor activity-modifying proteins (RAMPs), and the realization that CGRP signaling required receptor complexes rather than a single seven-transmembrane protein, reshaping thinking about peptide receptor activation and ligand binding. Dr. Foord also discusses work on angiotensin, GABA B, free fatty acid, nicotinic acid, and prostaglandin EP4 receptors, showing how orphan receptors were deorphanized using expression systems, electrophysiology in Xenopus oocytes, and early bioinformatics. The discussion highlights the gap between identifying a target and delivering a drug, the challenges of target validation, and the realities of industrial decision-making around receptor selectivity, safety, and market focus. Along the way, Dr. Foord reflects on the limits and promise of human genetics, the underexploited potential of GPCR antibodies, and the importance of team composition, negative data, and scientific community in navigating complex receptor biology. About the Guest Dr. Foord is a physiologist and pharmacologist who spent more than two decades at Glaxo, Glaxo Wellcome, and GlaxoSmithKline working on GPCR pharmacology and drug discovery. Trained in neuroendocrinology, he helped bring molecular biology into traditionally pharmacology-driven GPCR programs and worked across migraine, cardiovascular, pain, and inflammation projects. His work contributed to the identification of RAMPs in the CGRP receptor system, deorphanization of several GPCRs including GABA B and carboxylic acid receptors, and discovery of a prostaglandin EP4 modulator that advanced as a drug candidate. Later in his career, Dr. Foord led bioinformatics for neuroscience and played a central role in GSK’s early large-scale genetics initiative, integrating GPCR targets, ion channels, transporters, and ligands into association studies. His experience spans receptor cloning, expression systems such as Xenopus oocytes, electrophysiology, molecular pharmacology, and the use of informatics to mine sequence, structural, and genetic data for new receptor targets. Key Insights from the Conversation RAMPs Reframed Peptide GPCR Pharmacology . Dr. Foord explains how attempts to clone the CGRP receptor from SK-N-MC cells, combined with highly sensitive cAMP readouts in Xenopus oocytes, unexpectedly pulled out RAMP1 rather than a conventional seven-transmembrane receptor. The realization that RAMPs co-assemble with CRLR to form CGRP and related receptors forced a reconceptualization of peptide receptor activation and made clear that receptor complexes, not single proteins, could underlie pharmacological specificity. Serendipity Depends on Experimental Design and System Choice . The discovery of RAMPs was only possible because the assay tied receptor signaling to a highly amplified electrophysiological readout, revealing dramatic effects that might have been lost in noisier systems. Similarly, placental tissue became the source for CGRP receptor purification simply because binding studies showed it combined high receptor density with practical availability, illustrating how pragmatic choices in model systems can open unexpected paths in GPCR pharmacology. Deorphanizing Receptors Blends Bioinformatics and Bench Work . Dr. Foord describes a period where his group repeatedly identified ligands for orphan receptors: the second GABA B subunit via yeast two-hybrid, a carboxylic acid receptor when the solvent turned out to be the real agonist, and a nicotinic acid receptor by intersecting tissue expression data with orphan GPCRs. These stories show how careful pharmacology, informed sequence analysis, and attention to apparent artifacts can reveal new receptor signaling pathways relevant for metabolism and cardiovascular disease. Target Validation Is Harder Than Cloning a Receptor . From the non-existent second AT1 angiotensin receptor to the MAS oncogene as a poor angiotensin responder, Dr. Foord emphasizes how easy it is to be misled by overexpressed systems and noisy orphan receptor data. Southern blotting, cross-hybridization, and later genetic analyses ultimately showed that some hypothesized subtypes were artifacts, underscoring that robust target validation is a distinct and often more challenging problem than receptor cloning or initial ligand binding assays. Drug Discovery Is Constrained by Selectivity, Safety, and Strategy . The CGRP story illustrates how structural biology and pharmacology intersect with corporate decisions: once it became clear that the CRLR binding pocket is shared across CGRP, amylin, and adrenomedullin receptors, small-molecule selectivity looked problematic. Later hepatotoxicity concerns and the success of antibody therapeutics further shifted strategy. Similar strategic considerations shaped the fate of the EP4 partial agonist that ultimately found a niche in veterinary medicine rather than human rheumatoid arthritis. Genetics and Informatics Offer Power but Not Simple Answers . As Head of Bioinformatics for Neuroscience, Dr. Foord participated in GSK’s early large-scale association genetics effort, feeding GPCRs, ion channels, and transporters into case–control studies. Apart from APOE4 in Alzheimer’s disease, most signals failed to reach robustness with available cohort sizes, tempering expectations that genetics alone would deliver pipelines of GPCR targets. He argues that integrating structural biology, computational pharmacology, and genetics may still be key to understanding receptor activation in patients, but requires realistic views of effect sizes and trial design. Scientific Careers Depend on Teams, Mentors, and Community . Reflecting on his path from physiology to molecular pharmacology to bioinformatics, Dr. Foord highlights how good mentors, diverse teams, and open sharing of reagents and ideas enabled progress. He stresses the value of lab “optimists and cynics,” the importance of talking about negative results, and the role of informal networks in preventing wasted effort. For younger scientists, his advice centers on doing work you genuinely enjoy, finding supervisors who connect you to the broader GPCR community, and being willing to pivot as new methods and questions emerge. Episode Timeline 00:00 — Early academic work in neuroendocrinology, self-experimentation with TRH and somatostatin, and first encounters with hormones and GPCRs. 02:00 — Move to Roger Craig’s lab, purification of the CGRP receptor from human placenta, and practical considerations in choosing receptor-rich tissues. 05:00 — Transition from academia to Glaxo, early HIV TAT work in Xenopus oocytes, and the emergence of molecular pharmacology within a pharmacology-led organization. 10:30 — Expression cloning of the CGRP system, discovery of RAMP1, and how oocyte electrophysiology revealed a massive potentiation of endogenous CRLR signaling. 18:00 — Industrial migraine programs, small-molecule CGRP antagonists, challenges with selectivity and liver toxicity, and the later success of CGRP antibodies. 20:00 — Angiotensin receptor work, using Southern blots to hunt for a non-existent AT1 subtype, and the MAS oncogene as a cautionary tale in receptor signaling artifacts. 30:00 — Discovery of the prostaglandin EP4 receptor while searching for angiotensin-related sequences, development of an EP4 partial agonist, and its path into veterinary medicine. 34:00 — GABA B receptor complex, identification of the second subunit via yeast two-hybrid, and closing the chapter on proposed additional GABA B subtypes. 39:00 — Large-scale genetics and bioinformatics at GSK, expectations for GPCR target discovery from association studies, and reflections on why many signals remained elusive. 52:00 — Career advice on doing work you enjoy, the importance of mentors and connectedness, and how team composition and negative data shape GPCR research and drug discovery. Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Kaavya Krishna Kumar About Dr. Kaavya Krishna Kumar "I am a postdoc in Prof. Brian Kobilka's lab at Stanford University, USA. I work on understanding the activation mechanism of different Families of GPCRs." Dr. Kaavya Krishna Kumar on the web Journal of Biology Chemistry Stanford University Google Scholar LinkedIn Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) You never know where your GPCR takes you with Dr. Brian Hudson About Brian Hudson Brian is a lecturer in the School of Molecular Biosciences at the University of Glasgow. He has more than 20 years of experience in GPCR, primarily focused on drug discovery and developing new tools to study this receptor family. He leads a research group that is focused on understanding the pharmacology and function of a group a GPCRs that are activated by metabolic intermediates. Brian Hudson on the web University of Glasgow Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

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

<< Back to podcast list Strategic Partner(s) Dr. Ross Cheloha About this episode Dr. Ross Cheloha is an Investigator at the National Institutes of Health in the Laboratory of Bioorganic Chemistry in Bethesda, MD, where he started in October 2020. He completed his postdoctoral training at MIT and Harvard Med School in the lab of Hidde Ploegh , where he developed new applications of single-domain antibodies (nanobodies). He earned his Ph.D. in Chemistry at the University of Wisconsin-Madison in the lab of Sam Gellman on the study of analogs of the GPCR peptide ligand parathyroid hormone. Work in his independent laboratory is focused on developing new pharmacological tools via chemistry and protein engineering to interrogate GPCR signaling. Ross and I chatted about his work and transition to an independent investigator; join me to learn more about class B GPCRs and Dr. Cheloha’s work. Dr. Ross Cheloha on the web NIDDK Cheloha Lab Google Scholar LinkedIn Twitter ResearchGate Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Yao Lu (Jackie) About Yao Lu (Jackie) "Jackie is a Ph.D. student, at Monash University, Australia, investigating the role of functional selectivity in a novel class of potential antipsychotics for the treatment of schizophrenia. Her work involves the pharmacological and structural characterisation of novel putative antipsychotic small molecules. Her research aims to provide a molecular explanation of small molecules for their pre-clinical efficacy and to support the design of novel therapeutics. " Yao Lu (Jackie) on the web Monash University Georgina Sweet Fellowship Authorea Dr. GPCR Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

<< Back to podcast list Strategic Partner(s) Dr. Stephen Ferguson The History of the Great Lakes GPCR Retreat with Dr. Stephen Ferguson About Dr. Stephen Ferguson Dr. Stephen Ferguson is a Professor in the Department of Cellular and Molecular Medicine at the University of Ottawa. He did B.Sc. in biology at McGill University and received his Ph.D. under the mentorship of Dr. Brian Collier in the Department of Pharmacology and Therapeutics at McGill University (1994). He did his postdoctoral training with Dr. Marc G. Caron at Duke University (1994-1997), where he and his colleagues investigated the role of G protein-coupled receptor kinases and beta-arrestin in regulating G protein-coupled receptor endocytosis, trafficking, and signaling. He has held four Canada Research Chairs since 2001 and was previously a Heart and Stroke Foundation of Canada MacDonald Scholar (1998-2003) and Heart and Stroke Foundation of Ontario Career Investigator (2003-2016). He was a recipient of Canada's Top 40 under 40 award in 2004 and received Queen Elizabeth II, Diamond Jubilee Medal, in 2012. He has also received both Junior (2001) and Senior (2005) investigator awards from the Pharmacological Society of Canada. Most recently, in 2021, he was elected as a Fellow of the Canadian Academy of Health Science (FCAHS). His research career has focused on the investigation of the regulation of G protein-coupled receptors signaling mechanisms in health and disease. He currently holds multiple research grants from the Canadian Institutes of Health Research (CIHR) for his research investigating the role of metabotropic glutamate receptor signaling in Huntington’s and Alzheimer’s disease. Dr. Stephen Ferguson on the web Carlton University Canada Research Chairs Twitter ResearchGate LinkedIn Dr. GPCR Ecosystem Great Lakes GPCR Retreat on the web 21st Great Lakes GPCR Retreat More about previous GPCR Retreat meetings Dr. GPCR Ecosystem Upcoming Live Expert Sessions ➚ 🔒Explore the Full Masterclass ➚ Unlock the Full Dr. GPCR Learning Ecosystem ✔ Full Masterclass library ✔ Terry's Pharmacology Corner ✔ Advanced GPCR courses ✔ Scientific discussions → Become Premium 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 Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>