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One reason is that selectivity in this family is not just a matter of receptor subtype. dimerization - from A2A/dopamine D2 in Parkinson's to A1/A2A in cardio protection, and what remains transfected receptor signal from endogenous background. receptors form both homodimers and heterodimers with other GPCRs, including A2A with dopamine D2 (a miss 42:42 Advice for PhD students - resilience, collaboration, and not fearing the unknown 54:44 The dopamine

After a PhD on allosteric modulation of dopamine receptors in Philip Strange's UK lab and a postdoc at in vivo stayed on the receptor for seven hours at room temperature. calculation that first connected math to biology 06:16 PhD with Philip Strange: allosteric modulation of dopamine receptors and the first aha moment 16:53 Why GPCRs? Samuel Hoare Sam completed his Ph.D. in biochemistry, studying allosteric modulation of dopamine receptors

establishing a role for Beta-arrestin signaling in the brain in vivo and has established its importance in D2 dopamine receptors (D2R) functions. These receptors belong to the super-family of G-protein coupled receptors (GPCR), the major molecular stabilizer drugs (e.g. lithium) used for bipolar disorder therapy target signaling mechanisms regulated by dopamine receptors, thus providing a framework to understand how different drug classes can engage overlapping

. << Back to podcast list Strategic Partner(s) Brian Arey: Discovering Signaling Bias at the FSH Receptor Biased signaling - the idea that a single receptor can preferentially activate one downstream pathway conservation of biased receptor function across receptor classes The physiologist's approach to mechanistic It took a pertussis toxin experiment, borrowed conceptually from Tom Burris's dopamine receptor work, The same logic applies to cytokine receptors, nuclear hormone receptors, and receptor tyrosine kinases

GPCR, an ecosystem designed to bring together stakeholders interested in using G-Protein Coupled Receptors Her work focused on chemokine receptors, members of the GPCR family that control cell movement in the Latrophilin 3 receptor. free energy landscape analysis to understand the signaling pathways and activation mechanisms of the Dopamine D3 receptor and the CXCR4-CXCL12 complex.

retired at the end of 2014 and since then has been writing papers on his final major project at Lilly, a dopamine doctoral dissertation was the first large-scale study of structure-activity relationships for adenosine receptors postdoc with John W Daly at NIH and Solomon Snyder at Johns Hopkins, he developed the first adenosine receptor He then joined WL/PD, where his lab demonstrated the existence of two subtypes of the adenosine A2 receptor In 1988, he joined Lilly as a receptor biologist in charge of a high-throughput screening lab.

have a catalogue of over 30 fluorescent ligands for different families of GPCRs, including adenosine, dopamine , serotonin, cannabinoid and muscarinic receptors. NanoBRET® competitive binding assay enables real-time quantification of ligand–receptor interactions GPCR, the global knowledge hub for G protein-coupled receptor (GPCR) research and education, is proud GPCR Expertise Specialized knowledge in adenosine, dopamine, serotonin, cannabinoid and muscarinic receptors

same university in 2005 by investigating the molecular mechanisms involved in the angiotensin type 2 receptor She identified the molecular mechanisms involved in the opposite regulation of dopamine D1 and D5 receptors She identified the structural determinant controlling biased signaling of melatonin type 2 receptors Award, she investigated biased and compartmentalized G protein signaling by the vasopressin type 2 receptor understanding the role of compartmentalized Gq signaling by the cytomegalovirus-encoded chemokine US28 receptor

Gunnar Schulte of Karolinska Institute makes the case that frizzled receptors are GPCRs — through G-protein The biggest question is how we don't understand how the ligand interacts with the receptor, how the receptor That is my strongest argument for the GPCR nature of these receptors." section Receptor Biology and Signaling at the Department of Physiology and Pharmacology. , the relevance of receptor dynamics, and receptor complex composition for signal initiation and specification

the INSERM Laboratory directed by Jean-Charles Schwartz in Paris, where he cloned and characterized dopamine D2 and D3 receptor subtypes.

, odorant receptors, and the trace amine-associated receptors that may one day treat depression. << Back Chemosensory receptors — bitter taste receptors (TAS2Rs), odorant receptors, and trace amine-associated Bitter taste receptors have been identified in the heart and intestine, olfactory receptors in the brain Her group now studies taste receptors, odorant receptors, and trace amine-associated receptors using olfactory system 19:03 Inside a computational workflow for orphan receptors 29:14 Bitter receptors in

and chemokine receptor systems, including CCR2. Receptors in Complexes Behave Differently Than Receptors in Isolation Standard drug screens present a receptor as a discrete, isolated target. In the body, that receptor is complexing with other receptors, scaffold proteins, and cytoskeletal elements receptors are complexing.

Pluznick explores what changes when olfactory receptors are treated not as smell receptors but as general-purpose Her lab studies the role of understudied GPCRs — olfactory receptors, taste receptors, and orphan GPRs Reframing olfactory receptors as chemosensors. Pluznick argues they are better understood as chemical sensors that happen to dominate the nose. Mice have ~1,000 olfactory receptors; humans have ~350.

. << Back to podcast list Strategic Partner(s) Amynah Pradhan: The Delta Opioid Receptor and the Migraine Paradox Chronic migraine sits at a peculiar crossroads in opioid pharmacology: sustained mu opioid receptor For her, this line of work is also personal — the delta opioid receptor has been her scientific focus Paul Clarck , where she studied opioid receptors. Brigitte Kieffer , where she studied ligand-directed signaling at the delta-opioid receptor.

matchmaking - applying recommendation system logic to the bitter taste receptor family Sweet taste receptor receptor inhibitor suppresses the sweetness of heavy water. Taste receptor expression throughout the body reshapes the meaning of drug off-targets Bitter taste receptors properties of both - that can suggest candidate receptors for any new compound. - bitter taste receptors in the airways, gut, heart, and cancer tissues 19:37 - Sweet taste receptors

Livingston on allosteric opioid modulators, receptor internalization, and navigating the transition from Signaling Beyond the Membrane Opioid receptors belong to a class of GPCRs where the pharmacology extends internalization using live-cell imaging approaches that track receptor dynamics in real time. Internalized receptors don't stop working The membrane-centric view of receptor pharmacology assumes signaling ends when a receptor is endocytosed.

David Hodson on visualizing GLP-1 and GIP receptors in pancreatic islets and brain circuits to advance therapies for diabetes and obesity. << Back to podcast list Strategic Partner(s) Visualizing GLP-1 & GIP Receptors in Islets and Brain In this episode, Professor David Hodson discusses how GLP-1 and GIP receptors regulate metabolism across the pancreas and brain, and why visualizing receptor localization and signaling in Why this matters How receptor distribution in islets and brain circuits shapes incretin hormone drug

Cheloha builds nanobody-GPCR ligand conjugates that rescue weak peptides, engineer receptor selectivity to podcast list Strategic Partner(s) Ross Cheloha: Nanobody-GPCR Conjugates and the Engineering of Receptor Selectivity The parathyroid hormone receptor sits at the intersection of calcium homeostasis, bone metabolism How does receptor conformation shape the duration of downstream signaling? And can selectivity for one receptor subtype be engineered without redesigning the ligand from scratch

Graciela Piñeyro on what happened when her lab tested biased agonism at the μ-opioid receptor across 25 ligands, why δ-opioid receptors recycle from the lysosome, and the quantitative pharmacology that turned an early artifact into a career of receptor work. << Back to podcast list Strategic Partner(s) Her lab now studies δ- and μ-opioid receptor signaling, biased agonism, receptor trafficking and recycling Long treated as a non-recycling receptor destined for degradation, the δ-opioid receptor can in fact

Terry Kenakin on detecting, quantifying, and applying receptor signaling bias in GPCR drug discovery. This phenomenon, receptor signaling bias or functional selectivity, is now recognized as a meaningful It is a consequence of ligand-dependent receptor conformations and allosteric probe dependence, and it The Biology Behind Bias Ligands produce differential pathway engagement at a single receptor because they stabilize distinct receptor conformations.

Since 2013, he has been elected Chair of the subcommittee for the Dopamine receptors of the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification

Elva Zhao on biased agonism at the GLP-1 receptor, G protein regulation, and building a mechanistic picture podcast list Strategic Partner(s) Elva Zhao: G Protein Regulation and Biased Signaling at the GLP-1 Receptor The GLP-1 receptor is among the most clinically validated targets in metabolic disease - yet the signaling Her PhD at Western University focused not on receptors but on G protein cycle regulation - RGS proteins Nigel Bennett on biased signaling at the PAR2 receptor, then with Profs.

From chemokine receptors at Rockefeller to founding Dr. GPCR during COVID — the career arc behind the ecosystem built for the field's unreached receptors. << multiple chemokines bind multiple receptors. The 250-receptor problem sits in plain sight. Without that tissue, GPCRs stay siloed by receptor family and by lab.

Nobel laureate Robert Lefkowitz traces the accidental origins of his receptor research — from a Vietnam receptors are discrete molecular entities. Receptors were an unproven concept when Lefkowitz chose to study them When Dr. existence of receptors. There's no such thing as a receptor.

on orphan GPCR biology, GPCRDB, biased signaling, and how the data analysis bottleneck is reshaping receptor pharmacology and drug discovery. << Back to podcast list Strategic Partner(s) David Gloriam: Orphan Receptors GPCR Pharmacology GPCRs represent the largest and most pharmacologically important family of membrane receptors evolution as a framework for engineering receptor-ligand interactions at the residue level. probes for a range of receptors.

whether opioid receptors were even proteins, to the cryo-EM-driven structure-function loops that now His lab works on serotonin, dopamine, and opioid receptor structure, function, and drug discovery, with The bet is that biased ligands at the serotonin 2A receptor can separate the two. Roth's lab identified salvinorin A as a kappa opioid receptor agonist. reserve and capture coupling close to the receptor.

Johnson explains why the circuit matters more than the receptor. << Back to podcast list Strategic Partner Kari Johnson's research follows this receptor from the bench to the behaving animal, using optogenetics That breadth is a signal of the receptor's centrality in CNS function. The question, in Johnson's framing, is not which receptor you prefer, but which receptor is correctly preclinical evidence across alcohol, cocaine, methamphetamine, and heroin 13:28 How mGlu2 modulates dopamine

John Streicher: Reorganizing Opioid Signaling Beyond the Receptor The dominant strategy for improving opioid therapy has been to engineer new ligands at the receptor itself — biased agonists, partial agonists In the brain, HSP90 promotes ERK activation downstream of the mu opioid receptor and is required for Receptor signaling assays showed efficacy shifts in the spinal cord and tolerance attenuation in the John Streicher 01:49 From heart failure to opioids — a path through signaling 07:49 Why the mu receptor

. << Back to podcast list Strategic Partner(s) Scaling GLP 1 Receptor Tools Through Academia Industry access aren’t planned from the start Why fluorescence-based assays outperform antibodies for studying receptor combining fluorophore design, ligand chemistry, and pharmacology, his work enables precise visualization of receptor His research focuses on class B GPCRs, including the GLP-1 and GIP receptors, with an emphasis on understanding how these receptors operate within complex tissues such as the pancreas and brain.

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 of peptide receptor activation and made clear that receptor complexes, not single proteins, could underlie Deorphanizing Receptors Blends Bioinformatics and Bench Work . Dr. Target Validation Is Harder Than Cloning a Receptor .