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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.

How receptor residence time — not affinity — rescued a CRF drug discovery program, and why a career in starts with asking what the math never captured. << Back to podcast list Strategic Partner(s) Sam Hoare: Receptor When Sam Hoare and the CRF receptor team at Neurocrin Biosciences discovered that their lead compound sat on the receptor for seven hours while a failed backup fell off in fifteen minutes, it exposed a in vivo stayed on the receptor for seven hours at room temperature.

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.

. << 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 He is the author of a 2014 book on evolutionarily conserved receptor signaling, co-written with Terry conservation of biased receptor function across receptor classes The physiologist's approach to mechanistic The same logic applies to cytokine receptors, nuclear hormone receptors, and receptor tyrosine kinases

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

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 .

. << 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.

These are questions you cannot answer in a HEK cell overexpressing a receptor it was never meant to see Working on chemokine receptor CCR1 in multiple myeloma, free fatty acid receptor FFA2 in type 2 diabetes acid receptor FFA2 in type 2 diabetes, and muscarinic M2 and M3 receptors, consistently prioritizing as a property of a compound and a receptor. receptor.

Bender uses virtual docking to find chemical probes for orphan GPCRs - receptors biology can't study Partner(s) Brian Bender: Computational Probes for Orphan GPCR The GPCR superfamily contains hundreds of receptors when one is even known - is rarely sufficient: a large peptide or lipidated compound may activate a receptor This gap is one of the defining bottlenecks in receptor pharmacology, and closing it one receptor at "I have to go into more receptors. I can't stay with just the one." About Dr. Brian Bender Dr.

Their pharmacological complexity is amplified by receptor activity modifying proteins (RAMPs), three single-pass membrane proteins that associate with these receptors to create pharmacologically distinct Hay examines the molecular pharmacology of the calcitonin receptor and calcitonin-like receptor - with and calcitonin-like receptor - and their interactions with RAMPs. - the canonical CGRP receptor in migraine.

These hybrid receptors enable researchers to probe receptor signaling, investigate G protein coupling receptors with poorly understood receptors. A hybrid GPCR is a receptor constructed by combining elements from two different receptors. Some receptor combinations work very well, while others fail—even when the receptors are very similar Some papers call them hybrid receptors, others call them chimeric receptors, and sometimes they’re just

Specifically, I am interested in understanding dysregulated G-protein coupled receptor (GPCR) signaling During my post-doctoral research, I was part of a study that identified the receptors of a novel human 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. My long-term plan is to conduct research in the field of receptor biology, with a focus on GPCRs.

Paul Insel explains how unbiased GPCR expression profiling uncovered overlooked receptors in cancer — purinergic receptors and, most recently, proton-sensing GPCRs in the tumor microenvironment. The field's reductionism may be hiding how receptors actually work Dr. And the answer was PAR1, the thrombin receptor. From that point on, Paul was hooked and has since studied receptor function in human physiology, receptor

studying GPCRs in HEK293 cells misses critical biology — and how iPSC-derived models and intracellular receptor Hebert's research focuses on the angiotensin AT1 receptor, a signaling hub coupled to Gq, Gi, G12, and Intracellular GPCRs as Drug Targets — Receptors on the nuclear and mitochondrial membranes represent The AT1 Receptor Defies Simple Classification The angiotensin AT1 receptor is not just a Gq-coupled receptor A Clinical Trial Failure That Pointed Forward The Trevena biased agonist for the AT1 receptor failed

Nivedha also reflects on broader implications for receptor subtype selectivity, peptide receptor pharmacology Simulations Provide Dynamic Views of Receptor Function Static structures capture only one moment in receptor the receptor to activate signaling? Applications to Receptor Selectivity Dr. I also worked on collaborative projects involving peptide-binding receptors, including angiotensin receptors

Beatriz Blanco-Redondo on characterizing unknown adhesion GPCRs in Drosophila - receptor discovery, nocifensive Blanco-Redondo: Adhesion GPCR Discovery in Drosophila Adhesion GPCRs are among the least characterized receptor The receptors were named after condiments, ketchup, mayo, and remulate, not out of irreverence, but because Remulate is the receptor she secured funding to study, the one her first PhD student built an entire Since returning to Europe, her research has centered on receptor biology at the intersection of basic

From the development of BRET-based biosensors that revealed receptor behavior in living cells, to the discovery of pharmacological chaperones that rescue misfolded receptors from the endoplasmic reticulum Not which receptor - but which question. That inversion - question first, receptor second - shaped a body of work that spans adrenergic receptors , chemokine receptors, vasopressin receptors, and class C GPCRs without ever being defined by any single

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. It is also a complication: a receptor that modulates so many circuits will inevitably produce wanted The question, in Johnson's framing, is not which receptor you prefer, but which receptor is correctly

Marshall on structure-based GPCR drug discovery, the GABA-B heterodimer, the acetate that rewrote a receptor The Ligand That Wasn't the Ligand Screening orphan receptors in yeast, the team chased peptide hits that The orphan was a free fatty acid receptor. These discoveries rewrote what counts as "druggable" on receptors once considered fully mapped. "We had this really cool room where you could see — you put on 3D glasses and see the receptor in three

Receptors that fell apart in any useful detergent could not be crystallized, and without crystals, there That insight led to a systematic mutation screen, a 21-degree improvement in receptor thermostability Tate's work reframed the problem: before asking what a receptor does, you first have to ask whether it from family D - turned out to be a dimer, with an architecture that breaks the rules of class A receptor , and also by electron cryo-microscopy of receptors coupled to mini G protein bound to βγ subunits.

Explore GPCR lipid rafts, bitter taste receptor pharmacology, and data integration in this expert interview construction of an open-access GPCR-lipid raft database and reviews key findings from his research on D1 receptor When you’re mapping receptor localization and need to understand the mechanistic role of microdomains 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.

The team’s projects are devoted to the activation/function of CXCR4-ACKR3 (CXCR7) receptors of the CXCL12 In particular, FB contributed to the discovery that CXCL12 is the ligand for the CXCR4 receptor and can FB’ team has identified the orphan CXCR7/ACKR3 receptor as being the 2nd receptor for CXCL12, which behaves 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

Tore Bengtsson on β₂-adrenergic receptor signaling, muscle metabolism, and how GPCR pharmacology can Tore Bengtsson , professor of physiology at Stockholm University, explores how β-adrenergic receptor “People think a receptor produces one signal. In reality, a receptor produces many signals.” That’s what we’ve now achieved with new compounds that stimulate the receptor in a novel way. Traditionally people thought receptor activation leads to one downstream pathway.

GPCR webinars are live online scientific sessions focused on G protein-coupled receptor (GPCR) biology These webinars are ideal for: GPCR pharmacologists Medicinal chemists working on receptor targets Structural Topics frequently address: Receptor efficacy and bias Allosteric modulation PK/PD relationships Irreversible These webinars are designed for scientists with foundational knowledge in receptor pharmacology, signaling Topics may include: Receptor efficacy and operational models Allosteric modulators (PAMs and NAMs) Biased

GIPR Imaging: From Cell Assays to In Vivo Systems Fluorescent tools for imaging endogenous incretin receptors across biological systems Interrogating Incretin Receptor Biology Across Biological Complexity GLP-1 and GIP receptors have emerged as central targets in metabolic medicine, yet their precise localization and dynamics in native contexts — without relying on receptor overexpression or genetic modification Enable simultaneous visualization of endogenous receptor localization and nanodomain organization in

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 By combining NanoLuc-tagged receptors with fluorescent tracers, this approach allows direct measurement GPCR, the global knowledge hub for G protein-coupled receptor (GPCR) research and education, is proud “These tools can dramatically improve how scientists measure ligand-receptor interactions, visualize

Strosberg AD in France, where he worked on the regulation of ß-adrenergic receptors. He is the Research director at INSERM with a specific interest in G protein-coupled receptors by developing He showed the formation of melatonin receptor heteromers in vitro and in vivo and their importance in He established the concept of ligand-independent functions of orphan receptors in heterodimers with other He discovered multiple rare and loss-of-function variants of the MT2 melatonin receptors that are associated

Her team at InterAx models receptor signaling pathways as systems of time-dependent equations, then runs in Graz, she spent six and a half years at Novo Nordisk in early drug discovery, focused on incretin receptors With a well-constructed computational model and a small set of kinetic assays, one compound on one receptor The next challenge is multi-receptor, multi-disease complexity. The computational tools that now describe single receptors will need to extend to how multiple receptors

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 Her research centers on developing nanobody-ligand conjugates to target GPCRs, with a focus on receptors As a young researcher fascinated by chemokine receptors, molecular pharmacology, drug discovery, and I investigated the effect of lung cancer-related mutations in the GAIN domain of the Latrophilin 3 receptor

contributed to multiple projects exploring the underlying mechanisms of biased signaling at chemokine receptor signaling profile of CXCR3’s three endogenous biased ligands, elucidating the role of site-specific receptor biased agonists, and demonstrating the ligand specificity behind GRK recruitment to endosomes upon receptor identifying the non-canonical signaling effectors involved in the activation of Atypical Chemokine Receptor 3 (ACKR3), a receptor which does not couple to G protein and has been shown to maintain its activation