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Eric Trinquet, a veteran innovator behind functional GPCR assays like HTRF and IP-One, believes rigid If you’re building tools or careers in GPCR science, this is your playbook. It began with an unmet need: how to track Gq-coupled GPCR activity without the mess of calcium flux or GPCR   Dr. GPCR X Revvity Collaboration ⸻ Want more like this? 👉 Join the Dr. GPCR Premium Ecosystem  for behind-the-scenes access to GPCR innovators, exclusive deep-dives, and practical

Before your GPCR ligand ever meets its receptor, it meets the enzymes that determine whether it survives Discovery Program So what does that mean for discovery scientists designing the next generation of GPCR Even the most elegant GPCR ligand can fail if it never reaches its receptor. GPCR members save 50%+  with your Weekly News code. 👉 Join Terry’s Corner & Secure Your Spot for the Kenakin with your own enzyme or GPCR interaction puzzles.

In GPCR drug discovery, a single mistaken assumption can derail an entire program. Why Misreading Antagonism Delays GPCR Drug Discovery If a dose-response curve shifts to the right, you Why now:  GPCR research is accelerating—and the projects that succeed will be those built on clear, accurate Subscribe to The Kenakin Brief today  ➤   #GPCRantagonism #CompetitiveAntagonists #NonCompetitiveAntagonists DoseResponseCurve #Pharmacology #SchildEquation #AntagonistAffinity #Kinetics #DrugReceptorInteractions #GPCRblockade

s latest lecture delivers high-impact insight crafted for teams navigating the complex behaviors of GPCR-targeting As Kenakin explains, all GPCR signaling is allosteric , and pretending otherwise introduces risk at every If you’re still treating GPCRs as passive targets, your screening filters may be blind to key liabilities But without understanding how GPCR state changes  influence that affinity—or vice versa—drug discovery Corner  is your trusted, expert-led guide through the evolving landscape of GPCR science.

Welcome GPCR Fans,   In GPCR-targeted drug discovery, precision isn’t optional—it’s a requirement. GPCR Premium Members this week gain curated, early access to: Industry insights : GPCRs and mRNA in drug The interpretation of high and low affinity binding sites on GPCRs. GPCR Premium Membership Gives You an Edge Dr. GPCR Premium gives you an edge in a fast-moving field.

GPCR , the global nonprofit platform dedicated to advancing GPCR science through education, community GPCR Ecosystem. GPCR Podcast To mark the spotlight, Dr. GPCR  invited Dr. Eric Trinquet  to the Dr. GPCR. GPCR Dr.

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.

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

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

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

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.

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

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

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.

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

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

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

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

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.

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

Below is your Classified GPCR News at a glance for December 5 to December 11th, 2022. , 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. GPCR Ecosystem

GPCR Latrophilin1 in neurons. GPCR Activation and Signaling Biased Activation Mechanism Induced by GPCR Heterodimerization: Observations GPCR Signal Transduction. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. GPCR Ecosystem

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.

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.

August 2022 "G protein-coupled receptors (GPCRs) are the largest family of membrane receptors that serve Classically, GPCR internalization has been considered to lead to receptor desensitization. Here, this review summarizes different PTMs in GPCR internalization and analyzes their significance in , which will offer new insights into the regulatory mechanism of GPCR signaling and novel drug targets Read more at the source #DrGPCR #GPCR #IndustryNews

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

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