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

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

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

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

The GPCR Happy Hour Room What struck me first was the range. GPCR Happy Hour is free to every scientist who walks in. GPCR YouTube channel, and I encourage you to watch it. GPCR: welcome. This is what we do. Come find us in the fall. the people https://www.ecosystem.drgpcr.com/gpcr-university

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

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

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.

Welcome to the 4th official Adhesion GPCR Consortium newsletter! de Investigación y de Estudios Avanzados del IPN (Cinvestav) How did you become involved in adhesion GPCR AB: I became aware of the existence of adhesion GPCRs while completing my graduate studies. The family of adhesion GPCRs called the Latrophilins or ADGRLs first captured my attention due to their AB: The next workshop will likely bring together some of the hottest adhesion GPCR research going on

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.

Watch Episode 167 Some GPCR-targeting antibodies don’t inhibit receptors. They activate them. GPCRs, are likely targets for antibody-based immune responses. This is the future of GPCR immunology . ________________ Keyword Cloud : GPCR autoantibodies , GPCR immunology , GPCR diagnostics , Dr. GPCR ecosystem , multiplex assays

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.

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

Welcome GPCR Fans,   Every discovery-phase decision you make shapes your entire pipeline trajectory—and Upcoming events:  5th MMCS New Trends in Drug Discovery; GPCR-UK Network Meeting; neuroGPCR Symposium Must-read publications:  GPCRchimeraDB: Database of engineered GPCR designs. GPCR University Course Attendee Dr. The pace of GPCR innovation is accelerating.

Welcome aboard, GPCR Crew! GPCR Event Spotlight 11th Adhesion GPCR Workshop    📍  Mexico City 📅 October 23 - 25, 2024 Get ready Classified GPCR News  Let’s dive into the   Classified GPCR News from September 23rd to 29th, 2024 Industry Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug

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

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.

Traditionally, GPCR signaling was believed to primarily occur at the plasma membrane. GPCRs have also been identified within the mitochondria. Compartmentalized GPCR Signaling from Intracellular Membranes. Functional selectivity of GPCR-directed drug action through location bias. GPCRomics: GPCR Expression in Cancer Cells and Tumors Identifies New, Potential Biomarkers and Therapeutic

But for Ajay Yekkirala, that closed door lit the fuse for a career that would reimagine GPCR therapeutics spans deep academic research, startup life, and the application of machine learning and pharmacology to GPCR Blue Therapeutics: Turning GPCR Biology Into a Business Ajay’s academic training planted the seeds for Superluminal Medicines: AI/ML Meets GPCR Pharmacology As Ajay continued to explore how GPCR signaling Takeaway: Ajay Yekkirala’s story is not just about GPCR science or startup success.

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

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

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 if the way we've been studying GPCRs—arguably the most important drug targets in pharmacology—has Here’s the surprising truth: up to 80% of GPCR-targeted drugs fail—not because of poor chemistry, but Join Terry’s Corner and stay updated on the latest in GPCR research—delivered in a format that’s as approachable

GPCRs in Neuroscience Role of G-Proteins and GPCR-Mediated Signalling in Neuropathophysiology. New insights into the structure and function of class B1 GPCRs. Papers GPCRs: Signal Transduction. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. 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.

G protein-coupled receptors (GPCRs) are a vast family of membrane-bound proteins crucial for transmitting Traditionally, it was believed that GPCRs selectively activate only their cognate G protein subtypes, 'unproductive coupling'[1] and a fascinating phenomenon known as GPCR priming [2]. The enhanced signalling observed in GPCR priming is attributed to the formation of temporal non-cognate-GPCR GPCR priming opens new avenues for understanding the nuanced regulatory mechanisms governing GPCR signalling

Below is your Classified GPCR News at a glance for December 12 to December 18th, 2022. 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. GPCR Ecosystem

fascinating aspect of the cellular signaling network is the crosstalk between G protein-coupled receptors (GPCRs GPCRs, known for their involvement in a myriad of physiological processes, mediate mostly signaling through The cross-talk between growth factor receptors and GPCRs is an intriguing area of study. , leading to segregation of RTK-to-Gαi pathways from canonical GPCR-to-Gαi pathways. For instance, the sequestration of G proteins from canonical GPCR-dependent pathways by growth factor

Hi GPCR Enthusiasts (and Arrestin Aficionados!)   This week at Dr. GPCR, we’re decoding arrestin-driven signaling and spotlighting the tools to match.   Check out our new on-demand course on non-canonical GPCR behaviors and a podcast episode tracing 30 years of GPCR-RAMP discovery. GPCR Updates   Advanced Methods for the Optimization of Candidate Selection  – Master GPCR behavior beyond