. << 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 .

and the challenges of discovering ligands for understudied receptors like the galanin receptor family and the galanin receptor family. This illustrates how receptor pharmacology often involves complex, receptor-specific effects. 5. My favorite GPCR is not the opioid receptors. Instead, it’s the galanin receptor . Dr. There are three members of the galanin receptor family: galanin receptor 1, 2, and 3.

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 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 pharmacology versus single-receptor studies Building scientific community at the early-career stage "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.

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.

Randy Hall on the receptor tail the field ignored, the adhesion GPCR experiment that did the opposite to NMDA receptors, and asked what bound there. lab at Duke to work on adrenergic receptor regulation. focus on disease associated mutations that disturb receptor signaling or trafficking. His own case is the evidence: NMDA receptor scaffolding logic applied to beta adrenergic receptors.

Unlike class A receptors, which bind orthosteric ligands within their transmembrane domain and can function as monomers, class C receptors carry an additional extracellular domain of 500 to 600 amino acids that glutamate receptors, and the calcium-sensing receptor, the molecular mechanisms governing their activation In class C receptors, the orthosteric site sits inside a large extracellular domain that is physically A decade on one receptor: the cost and the clarity it produces Fan has worked on the GABA-B receptor

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. For example, you might take the extracellular and transmembrane domains of the beta-2 adrenergic receptor Some receptor combinations work very well, while others fail—even when the receptors are very similar

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

Paul Insel explains how unbiased GPCR expression profiling uncovered overlooked receptors in cancer — This challenges the mutation-centric framework that dominates oncology and suggests GPCRs may contribute 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

Laura Duvall's lab has traced this suppression to a specific neuropeptide Y family receptor, one she What pulls Duvall back to this receptor personally is its apparent conservation: the same NPY family receptor she found in mosquito gut tissue has a close relative in the human colon, doing a job no one A neuropeptide receptor turned up in a tissue no one expected. One receptor sits at the intersection of two very different behaviors.

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 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 Scientific Themes of the Conversation First-contact receptor characterization, what it means to study

Arun Shukla on how two beta-arrestin isoforms regulate over 800 receptors, why "non-canonical" GPCRs are nature's own biased receptors, and building a structural pharmacology lab in India. << Back to podcast How two structurally similar proteins orchestrate such functional diversity across an entire receptor cells and biosensors that visualize beta-arrestin conformations across multiple receptor systems. tail was expected to be receptor-specific.

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

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

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

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

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 The dimer interface sits on helix 1, involves a domain-swapped N-terminus and helix 7, is twice the area , and also by electron cryo-microscopy of receptors coupled to mini G protein bound to βγ subunits.

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

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 Bengtsson emphasizes the dominant role of skeletal muscle in metabolic regulation. “People think a receptor produces one signal. In reality, a receptor produces many signals.” Traditionally people thought receptor activation leads to one downstream pathway.

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

Terry Kenakin shows how tuning receptor expression separates affinity from efficacy, unmasks hidden agonism Receptor density and coupling efficiency change what a ligand appears to do, which is part of why in Glaxo, now GlaxoSmithKline, before joining UNC Chapel Hill, where he teaches and leads research in receptor His work is central to the quantitative framework used today to describe receptor signaling bias, allosteric and ortholog variants Multiple mechanisms of action: cAMP accumulation, β-arrestin recruitment, receptor

With respect to GPCRs, I'm particularly interested in peptide/small protein receptors and the mechanisms With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular motivated behavior and how these receptors can be targeted for therapeutic benefit. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor

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

Slosky’s research is focused on understanding how neuropeptide G protein-coupled receptors (GPCRs) regulate motivated behavior and how these receptors can be targeted for therapeutic benefit. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling addiction-associated behaviors in animal models without the side effects characteristic of balanced receptor Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on 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

Overview of GLP-1 physiology and receptor pharmacology, including mechanisms of GLP-1 agonists used to Its discovery and characterization have led to the development of GLP-1 receptor agonists, a therapeutic This session provides a foundational overview of GLP-1 physiology and receptor pharmacology. The session also reviews currently approved GLP-1 receptor agonists, highlighting pharmacokinetic strategies In this Masterclass, she introduces the physiological and pharmacological foundations of GLP-1 receptor

Fast, clear, live-cell receptor trafficking detection. This technology supports robust analysis even at low endogenous receptor expression levels. Internalization into acidic compartments = signal activation: Upon receptor-mediated endocytosis, the View Product pHSense Eu SNAP Labeling Reagent Can be used to label receptors and membrane proteins carrying All four formats are validated in well-established models like GLP1R and Mu opioid receptor (MOR), and