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
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