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Could reorganizing the cell membrane redefine how we target GPCRs? Explore how lipid rafts shape receptor signaling, why targeting compartmentalization is advancing drug discovery tools, and what happens when conventional paradigms are challenged. Go behind the scenes of receptor desensitization—from deletion mutants to the promise and challenge of next-generation assays. About Keyvan Sedaghat Keyvan Sedaghat is an accomplished lecturer in pharmacology and biomedical science with extensive experience developing scientific tools and teaching advanced pharmacology in Canada and internationally. His research spans GPCR signaling regulation, assay development, and knowledge sharing, notably leading the creation of an open-access GPCR lipid raft database. Sedaghat’s global perspective and practical work at the bench and in curriculum design offer unique insights into GPCR structural pharmacology and the translation of research into innovative drug discovery resources for the field. What You’ll Learn How receptor compartmentalization within lipid rafts impacts GPCR signaling and why it matters for pharmacology research. Why deletion mutants of D1 dopamine receptors reveal unexpected mechanisms of desensitization—challenging classical signaling models. What drove the creation of a freely available GPCR lipid raft database, and how scientists are using it for experimental design. How molecular modeling and simulation complement wet-lab assays to probe GPCR function and accelerate assay development. Why bitter taste receptors are increasingly seen as targets for non-taste therapeutic pathways, including cancer and cardiovascular disease. What leadership lessons shape the next generation of GPCR scientists and the importance of focus, discipline, and curiosity in research. Episode link: https://www.ecosystem.drgpcr.com/dr-g... Keywords: gpcr podcast, gpcr internalization, drug discovery tools, fluorescence-based assays, receptor signaling, snap-tag, assay development, biased agonism, dr gpcr premium, pharmacology research Timestamps: 00:00 Intro 02:10 Keyvan Sedaghat’s Scientific Journey: From Pharmacy to GPCR Research 04:39 Choosing Pharmacology & Discovering Molecular Drug Mechanisms 08:37 D1 Dopamine Receptor Desensitization & GRK2/3 Signaling 10:24 Challenging Classical GPCR Paradigms 13:00 Building the 7TMR-Lipid Raft Database (7tmr-raft.org) 14:21 GPCR Compartmentalization & Lipid Rafts in Depression 16:32 Membrane Organization & Single Molecule Imaging (GPCR Retreat Insights) 19:17 Cholesterol Depletion Experiments & Membrane Lipid Composition 21:26 Molecular Dynamics & Modeling GPCRs in Different Lipid Environments 22:42 AlphaFold, AI & the Future of GPCR Structural Biology 24:28 Teaching Pharmacology in Canada & Supporting International Pharmacists 26:00 Bitter Taste Receptors Beyond Taste: Cancer, Asthma & Cardiovascular Disease 27:52 Apoptosis, Herbal Medicine & Bitter Compounds 29:54 Nobel Prize Moment: GPCR Field Recognition 31:07 Mentorship & Scientific Identity 32:25 Advice for Young Scientists: Focus, Discipline & Lifelong Learning 35:12 Naming the Episode – “A Fun Chat with a GPCR Guy” 37:05 Outro _____ 🧠 Want more like this? Join the Dr. GPCR Premium Ecosystem to unlock exclusive episodes, practical toolkits, and early access to GPCR University content. 👉 https://www.ecosystem.drgpcr.com/gpcr... _____ Join Terry’s Corner today! Visit https://www.terrykenakin.com for expert-led, on-demand pharmacology courses, and join us at the monthly AMAs with Dr. Terry Kenakin. https://www.ecosystem.drgpcr.com/terr... _____ Get to know our Partners: 👉 Celtarys Research • Company Page: https://www.ecosystem.drgpcr.com/celt... • Press Release: https://www.ecosystem.drgpcr.com/post... • Celtarys News: https://www.ecosystem.drgpcr.com/gpcr... 👉 Eurofins DiscoverX • Company Page: https://www.ecosystem.drgpcr.com/euro... • Press Release: https://www.ecosystem.drgpcr.com/post... • Celtarys News: https://www.ecosystem.drgpcr.com/gpcr... _____ Dr. GPCR is dedicated to fostering a collaborative ecosystem focused on GPCRs. By connecting researchers, sharing knowledge, and facilitating partnerships, the #DrGPCR Ecosystem provides resources to advance GPCR drug discovery. The ecosystem encompasses a range of initiatives to inform and engage the scientific community, including courses, news updates, and networking opportunities.