Must-read publications:  GPCRs in neurological disorders; OSTα-OSTβ structure; GPCR–G protein–β-arrestin GPCR Podcast—GPCR Assay Strategy, Bias, and Translational Drug Discovery In this episode of the Dr. GPCR podcast , Dr. GPCR innovation is accelerating. GPCR Team

In the high-stakes world of GPCR drug discovery , breakthrough science isn't enough. GPCR, we recognized this core problem. This is the essence of de-risking GPCR programs through operational excellence. the entire GPCR program as a single, interconnected entity. The GPCR Precision Blueprint is more than a concept.

we explore how computational tools—especially AlphaFold —are helping crack the mystery of olfactory GPCRs The Problem: Hundreds of Receptors, Almost No Ligands Alessandro’s work focuses on olfactory GPCRs—nearly : Predicting the “Face” of a Receptor When Alessandro began his PhD, structural models of olfactory GPCRs —Alessandro Nicoli A New Era of GPCR Research AlphaFold didn’t just fill a gap—it shifted the focus of Start with our GPCR training program and get hands-on with virtual tools shaping the future of drug discovery

of how residence time—not potency—predicts therapeutic coverage ✅ Insight into cryptic intracellular GPCR evaluating scaffold permeability using modern, cost-effective pharmacokinetic assays   Why Intracellular GPCR Drugs Change the Game For decades, drug design has treated GPCRs as surface targets. GPCRs now have validated intracellular  allosteric sites. Subscribe to The Kenakin Brief today  ➤ #GPCRs #IntracellularDrugs #DiffusionBarriers #DrugResidenceTime

A single successful GPCR imaging experiment can transform a project’s trajectory. Interdisciplinary design isn’t optional in GPCR imaging. It’s the catalyst. And the most striking validation came from in vivo GPCR imaging. Strong GPCR imaging tools come from strong interdisciplinary relationships.  🎧 Listen to the full episode https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/chemical-probes-for-gpcr-imaging-and-internalization

GPCR is proud to partner with the 5th Annual GPCRs-Targeted Drug Discovery Summit. Why the GPCR Drug Discovery Field Is Converging in Boston The GPCR field is in a genuinely exciting moment from biotech and pharma to advance GPCR programmes from discovery through translation — experts in GPCR structural modeling for GPCR drug discovery. signaling, and GPCR oligomerization.

Why Speed Matters in GPCR Drug Discovery Nine out of ten GPCR programs stall  not because the target In accelerating GPCR drug discovery, the bottleneck isn’t target identification — it’s turning validated GPCR Kinetics: The Critical Data You Can’t Afford to Skip Equilibrium potency data only tells part of “GPCRs are nature’s prototype allosteric proteins. Everything they do is allosteric.” Kenakin with your own enzyme or GPCR interaction puzzles.

Enhance your GPCR research with deeper assay insights for more effective results. This Week’s GPCR Intelligence: If you want cleaner decisions, start with the system—then the ligand. Breakthroughs this week: C. elegans avoids EGCG via SRXA-7 GPCR; a bidirectional GPCR switch modulates allosteric site on an orphan GPCR. 🔍 This Week in Dr. GPCR innovation is accelerating.

Kenakin  highlighted a fundamental truth: GPCR systems do not offer stable, proportional input–output Teams equipped with deep GPCR pharmacology insights make different decisions. The sections below synthesize the key topics addressed during the AMA and highlight the GPCR pharmacology This is a core GPCR pharmacology insight:ligand → receptor → G protein is never the entire story. GPCR innovation is accelerating, and those who invest in deeper GPCR pharmacology insights today will

The first Nobel prize that can be attributed to work related to GPCR-mediated signaling was the 1947 These odorant receptors (ORs) now account for about 60% of all identified human GPCRs. GPCR signaling, and location bias.[68–70] Further, our understanding of cross-talk between GPCR-mediated signaling pathways with other cellular signaling pathways, as well as non-signaling roles of GPCRs, Interaction of G-Protein βγ Complex with Chromatin Modulates GPCR- Dependent Gene Regulation.

GPCR Premium: Sneak Peek Want the full classified brief? GPCR , our mission is simple but urgent: Accelerate GPCR biology and drug discovery by connecting scientists GPCR Podcast, the Revvity team built pHSense™ from the ground up by listening to what GPCR scientists GPCR innovation is accelerating. GPCR and the offered resources in my work sphere." — DrGPCR University Attendee GPCR innovation doesn

As GPCR science and pharmacological innovation accelerate, timely guidance from foundational to advanced

Hello Sweet GPCR Enthusiasts, This week at Dr. GPCR: a new podcast episode with Dr. GPCR Updates   New Podcast Episode  - When to Walk, When to Run with Dr. GPCR Store is live!   — A tale of detergent tails: GPCR activation beyond ligands .   GPCR Team

Welcome back GPCR fans, If your drug discovery strategy still relies on static GPCR models, you’re already Upcoming events:  GPCR-UK Network Meeting, neuroGPCR symposium, and Transatlantic ECI GPCR event—where GPCR Podcast Listener Why Dr. GPCR Premium 🔹 What’s included? The pace of GPCR innovation is accelerating.

For drug hunters working at the GPCR interface, the difference between a successful lead and a dead-end For GPCR drug discovery, those hidden details can determine whether a compound advances or stalls. The Hidden Lever in GPCR Research In GPCR pharmacology, the conversation often centers on ligand properties—affinity In an era of accelerated GPCR-targeting innovation, these advantages define which programs advance and GPCR members save 50%+ with your Weekly News code) 👉   Explore Trailers & Join Today Why Terry’s Corner

Not a General Verdict A pharmacologist designing an orthosteric small-molecule agonist for a family B GPCR What GPCR Biologic Drugs Reveal About the Active-State Problem Family B GPCRs are conformationally malleable GPCR biologic drugs, peptides in particular, achieve this through a mechanism worth naming carefully. Family B GPCRs have a rich history of allosteric ligands that produce activation. The orthosteric site at a family B GPCR is not closed to small molecules.

What does DNA Day have to do with GPCRs? GPCR biology, the development of GPCR-targeted drugs, and the exploration of GPCRs as key regulators in the total count of GPCR genes in the human genome. The genetic variation in GPCRs is extensive; databases like GPCRdb provide a large database of genetic Structural bioinformatics analysis of variants on GPCR function.

Terry’s Corner: GPCR Binding Affinity Experiments That Hold Up Orthosteric GPCR binding affinity experiments GPCR Podcast: When GPCR Tools Scale Even the most elegant tools only matter when they scale beyond a GPCR Year in Review: Carrying Better Experiments Into 2026 As 2025 closes, the Dr. GPCR offers a clear signal of where the field is heading. GPCR Premium Member And Lock in The Current Rate➤ https://www.ecosystem.drgpcr.com/gpcr-university-pricing

GPCR signaling almost never follows a straight path. This article is about one big idea: GPCRs don’t act in isolation—they respond to the system they’re in In this session, you’ll gain: ✅ A mental model you can trust  for predicting how GPCR ligands behave Internalized Signaling: Same Receptor, Different Story A GPCR response isn’t always over when the receptor Constitutive Activity: When Doing Nothing Still Does Something Some GPCRs simply refuse to stay quiet

Exploring the intracellular allosteric site GPCRs represent one of the largest and most vital families For this reason, GPCRs have been a focus of drug development for decades due to their role in regulating Conventional GPCR drug discovery has largely focused on orthosteric sites, but recent breakthroughs in GPCR activity, enabling greater specificity and fewer side effects. allosteric site common in class A and class B GPCRs, particularly in chemokine receptors.

High-content screening (HCS) has become a cornerstone in GPCR and phenotypic drug discovery, enabling For GPCR-focused programs, the ability to visualize receptor localization, internalization kinetics, In this blog, you’ll learn:  How HCS works and why it is increasingly central to GPCR-based drug discovery The resulting multiparametric datasets are well-suited for GPCR research, where receptor trafficking, For GPCR assay developers, HCS supports:  Quantitative visualization of receptor internalization and

, and more Life, death and resurrection of plant GPCRs Structural and Molecular Insights into GPCR Function Papers GPCRs: Signal Transduction. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. The Illuminating the Understudied Druggable Proteome Conference. GPCR Ecosystem

GPCR community live on April 16 — one of 12+ Masterclasses planned for 2026, all included in Premium. April 29, and the GPCRs Drug Discovery Summit April 28-30. iPSC-Derived GPCR Models: Beyond HEK293 for GPCR at the GPCRs Targeted Drug Discovery Summit — Boston, April 28-30 The GPCRs Targeted Drug Discovery GPCR University Learner About Dr. GPCR Dr. GPCR is the intelligence and community platform for GPCR scientists.

Elevate Your GPCR Science with Essential Frameworks for Precision Drug Discovery: An Insight into Advanced GPCR-Based Drug Discovery conference is where the future of GPCR therapies will be defined. GPCR Premium Membership Gives You an Edge In a world filled with noise, Dr. GPCR Premium Membership delivers curated, noise-free intelligence every week. The pace of GPCR innovation is accelerating.

GPCR Activation and Signaling Molecular Mechanisms of PTH/PTHrP class B GPCR Signaling and Pharmacological Papers GPCRs: Signal Transduction. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. The Illuminating the Understudied Druggable Proteome Conference. GPCR Ecosystem

Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just GPCR University Exciting news! GPCR Event Highlight Get ready for the 11th Adhesion GPCR Workshop! GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs GPCR Ecosystem

Exploring the Hidden Dynamics: How Kinetics Reveals What Equilibrium Conceals in GPCR Research. Hi GPCR Community, If equilibrium curves are your comfort zone, this week’s feature will challenge (and GPCR Premium: Sneak Peek Here’s a fast, high-level preview of what Premium Members are unpacking this We’ve got your GPCR Track, Happy Hour, and sessions mapped so you can extract maximum value. GPCR innovation is accelerating.

GPCR research requires turning data into insights for drug discovery Hi GPCR Friends, Every week, critical decisions in GPCR research hinge on subtle shifts in data. GPCR Podcast – Ajay Yekkirala on GPCR Innovation In this episode, Dr. Be part of the nonprofit mission to unite the GPCR community. The pace of GPCR innovation is accelerating.

This is the kinetic detection problem in multi-target GPCR activity, and it has consequences for how

GPCRs in Neuroscience Role of G-Proteins and GPCR-Mediated Signalling in Neuropathophysiology. Papers GPCRs: Signal Transduction. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. The Illuminating the Understudied Druggable Proteome Conference. GPCR Ecosystem