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  • Inside the New Dr. GPCR Ecosystem: Learning, Insight, and Momentum for 2026

    GPCR Ecosystem: sharper programming, deeper expertise, and renewed momentum across everything we publish We have shifted to continuous, coordinated programming  across Weekly News, Terry’s Corner, the Podcast Pharmacokinetics isn’t a late-stage checkbox—it’s a decision framework that shapes every viable drug discovery program With new courses, expanded programming, upcoming partnerships, and deeper community engagement ahead, GPCR Team

  • GPCR Drug Discovery Summit 2026: What to Expect in Boston — and How to Register

    New structural tools, AI-driven design pipelines, and a growing number of programs moving into the clinic This year's program reflects where science is actually heading. Dr. GPCR founder Dr. from biotech and pharma to advance GPCR programmes from discovery through translation — experts in GPCR Alphamol on Phase 1 results from an orphan GPCR program pursued against industry skepticism. 🎥 Speaker program in every chapter of it.

  • GPCR Allosteric Modulation: Why Allostery is the Engine of Drug Discovery

    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 You’ll see how this manifests in real data from muscarinic receptors, CCR5 chemokine programs, and NMDA 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.

  • Allosteric Binding Demystified: Smarter GPCR Drug Discovery

    traditional displacement logic breaks down in allosteric systems, and how overlooking this can derail entire programs Sharpen your discovery decisions ➤ Yamina’s Corner - The Hidden Cost of Busy A GPCR program can collapse—not Read the article now ➤ Discovery on Target - The Next Wave of GPCR Drug Discovery The 20th Annual GPCR-Based GPCR Premium Membership Gives You an Edge The GPCR field is advancing at breakneck speed. a masterful teacher and communicator." — DrGPCR University Attendee The difference between stalled programs

  • The Boston Happy Hour: What Happens When GPCR Scientists Enter the Cafe

    The GPCR Happy Hour Room What struck me first was the range. We had trainees and CSOs standing next to each other, talking like peers. GPCR Happy Hour is free to every scientist who walks in. GPCR YouTube channel, and I encourage you to watch it. the people https://www.ecosystem.drgpcr.com/gpcr-university

  • How GPCR Spatial Signaling Sparked a Scientific Journey

    Many GPCR scientists trace their origin story back to a single unexpected spark. Not a grand plan. early curiosity led her to pursue a PhD in Molecular Pharmacology at Monash University, and later to train Luck, Leadership & GPCR Signaling Michelle is clear: luck played a role. But so did choice. GPCR Podcast 🔓 Want to go deeper? Join   Dr. GPCR Premium  for exclusive tools, deep dives, and expert access.

  • Targeting GPCRs in the CNS: Advances in Drug Discovery Strategies

    The central role of GPCRs in Neurological Disorders GPCRs are the largest family of membrane receptors Over 30% of FDA-approved drugs target GPCRs, with many targeting CNS located GPCRs. GPCR Structure, Activation, and Signaling Pathways in the Brain An understanding of GPCR structure is GPCR signaling: (A) an orthosteric ligand (orange) binds an inactive GPCR, the β2 adrenergic receptor Emerging GPCR Therapeutic Targets in CNS Drug Discovery GPCRs have been studied for decades, but there

  • How Understanding Intracellular Drug Access Can Transform Your GPCR Drug Discovery Program

    Welcome back GPCR fans, The pace of GPCR innovation is accelerating at a rate that can be difficult to Terry's Corner : Unlock the Power of Intracellular GPCR Drugs For years, GPCR drug discovery has focused GPCR Podcast : The Future of GPCR Drug Discovery with Molecular Modeling The field of GPCR research is Kenakin) teaming up with the best GPCR community platform to help train and inspire the next generation GPCR Course Attendee FAQ: What You Get with Dr. GPCR Premium What’s included?  

  • Assay Volume Control: Your GPCR Drug Discovery Power Lever

    This week Terry's Corner unlocks a simple lever that separates signal from storytelling, moving programs Breakthroughs this week: C. elegans avoids EGCG via SRXA-7 GPCR; a bidirectional GPCR switch modulates drug discovery program. Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters 7-day free trial to explore the corner   💎 $2999/year — one conference cost = 12 months of expert training

  • Exciting GPCR Events for Next Year! + GPCR Weekly Rocket Launch ⌿ Oct 28 - Nov 3, 2024

    Get your space suits on, GPCR cadets! up with a series of cosmic GPCR events for the year ahead. Exclusive access to private groups  Over 30 recorded talks from Symposia - that's a lot of brain food Classified GPCR News  Let’s dive into the   Classified GPCR News from October 28th to November 3rd, 2024 - Targeted Antibody Therapeutics Using Generative AI Zombie Fungi Hijack Hosts’ Brains GPCR Therapeutics

  • From Switches to Microcircuits: GPCR Biased Signaling and the Future of Drug Discovery

    Why GPCR Drug Discovery Is More Complex Than It Looks G protein-coupled receptors (GPCRs) have long occupied Emerging Families and Orphan GPCRs: Expanding the Drug Discovery Target Space Family A and B GPCRs — CONCLUSION: What the Switch-to-Microcircuit Shift Means for Drug Discovery Programs The shift from viewing phenotypic integration, and rigorous pharmacokinetic correlation are now increasingly accessible to programs , the answers will emerge from programs that take receptor signaling seriously at every stage of the

  • GPCR Internalization: When the Signal Moves Inside the Cell

    The Cell Surface Is Only Part of the Story For decades, GPCR pharmacology centered on events at the cell Work on receptors such as GLP-1R and MC4R has demonstrated that internalized GPCRs can continue to signal Measuring GPCR Internalization: Assay Strategies Beyond Imaging The classical approach to detecting internalization Terry Kenakin’s session on measuring GPCR internalization walks through the assay logic, the mechanistic

  • Why Kinetics Matter More Than Kd in GPCR Drug Discovery

    Welcome GPCR Fans,   Every discovery-phase decision you make shapes your entire pipeline trajectory—and Must-read publications:  GPCRchimeraDB: Database of engineered GPCR designs. Yet too many programs rely solely on affinity metrics—Kd—as proxies for in vivo behavior, missing a critical GPCR University Course Attendee Dr. The pace of GPCR innovation is accelerating.

  • Enzyme Inhibition Pharmacology: The Hidden Gatekeepers of GPCR Drug Discovery

    The Overlooked Step in Every Discovery Program So what does that mean for discovery scientists designing the next generation of GPCR ligands? Your Membership Includes: Frameworks proven in real discovery programs On-demand lessons  designed for trusted by biotech, pharma, and academia 💎 $2999/year — one conference cost = a full year of expert training Kenakin with your own enzyme or GPCR interaction puzzles.

  • From Failed Experiments to Predictive GPCR Models

    Watch Episode 175 From failed assays to breakthroughs in GPCR modeling , Dr. At that point, very few GPCR crystal structures had been determined. For Carlsson, this marked a shift in how his lab approached GPCR research. This perspective influences how his lab trains students. protein sequences, small molecule data are often fragmented, inconsistent, or unavailable, making model training

  • How Breakthroughs Happen: Eric Trinquet on Innovation, Serendipity & GPCRs

    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

  • Dr. GPCR Spotlights Revvity’s pHSense™ Internalization Tools

    GPCR Ecosystem. GPCR Podcast To mark the spotlight, Dr. GPCR  invited Dr. Eric Trinquet  to the Dr. GPCR. GPCR Dr. Through our podcast, training programs, and partner content, we help scientists connect, collaborate,

  • Four Reasons to Measure GPCR Signaling Bias in Drug Discovery

    Drug discovery programs that do not consider investigating for signaling bias often fail to fully understand How GPCR Signaling Bias Strengthens Drug Discovery Programs There are four distinct reasons why bias Programs that characterize signaling bias early — across G protein, β-arrestin, and second messenger For further reading on GPCR biased signaling and assay methodologies, explore the ‘Insights into GPCR Visit Eurofins DiscoverX GPCR Products and Solutions to explore the full portfolio of GPCR assays from

  • How Schild Analysis Protects Your Conclusions in GPCR Research

    GPCR Podcast: Visualizing GLP-1 & GIP Receptors in Islets and Brain Understanding incretin biology depends Listen to the episode ➤ Quick Links Assess GPCR Biased Signaling of Agonist How GPCR Collaboration Built GPCR Premium Membership Gives You an Edge Premium delivers a clear, noise-free stream of GPCR intelligence GPCR innovation is accelerating. GPCR Team

  • A Note from Yamina: Building the Next Chapter of Dr. GPCR

    We’re also reopening our instructor program  — welcoming scientists from across the community to teach Our access program for researchers in developing countries  continues as well: eligible scientists can GPCR Ambassador Program As we grow, we want the community to grow with us. Our Ambassador Program empowers community members to share Dr. GPCR About Dr. GPCR Dr.

  • GPCR Selectivity Beyond the Receptor — Live April 9th with Bryan Roth

    GPCR community live this week to examine what happens when GPCR selectivity is encoded not at the receptor GPCR University iPSC-Derived Systems for GPCR Signaling and Translation HEK293 systems are powerful tools differentiate these binding modes and why this distinction carries practical consequences for drug discovery programs interactions — and with it, how we think about drug discovery at GPCRs. GPCR Dr. GPCR is the intelligence and community platform for GPCR scientists.

  • Beyond HEK293 — Terry HĂŠbert on iPSC-Derived GPCR Models, Live April 16,

    pharmacology into disease-relevant environments, and what the implications are for translational pharmacology programs modes, and why establishing that distinction early carries immense practical value for drug discovery programs GPCR at the GPCRs Targeted Drug Discovery Summit — Boston, April 28-30 The GPCRs Targeted Drug Discovery What draws me to this meeting is not just the science on the program, but the conversations that happen GPCR University Learner About Dr. GPCR Dr.

  • Choosing the Right GPCR Calcium Assay Readout for Measuring Receptor Activation

    Introduction G protein-coupled receptors (GPCRs) remain one of the most important classes of drug targets Among the many signaling pathways activated by GPCRs, calcium mobilization is one of the most widely Why GPCR Calcium Assays Remain Valuable A GPCR calcium assay offers several advantages that have made Important Considerations When Selecting a GPCR Calcium Assay Despite their versatility, GPCR calcium biology and accelerate drug discovery programs.

  • How Collaboration Sparked a GPCR Imaging Breakthrough in Chemical Biology

    partnership built on trust and curiosity — reshaped both careers and helped unlock a new generation of GPCR How a Collaboration Led to a GPCR Imaging Breakthrough JB didn’t set out to contribute to a GPCR imaging It was the start of a scientific partnership with the potential to shift how GPCRs could be visualized How Chemical Probes Transformed GPCR Imaging and Outperformed Antibodies As JB continued exploring the Designing Reliable GPCR Imaging Tools for Real Biological Systems Success brought new challenges.

  • The Imprecision Problem: Why Your GPCR Drug Discovery Program Is Off-Track Before It Even Starts

    Unlocking the Puzzle: The Importance of Precision in GPCR Programs and the Hidden Costs of Overlooking A GPCR program can have world-class science, top-tier talent, and millions in funding — and still fail Hiring Won’t Save Your GPCR Drug Discovery Program When a drug discovery program stalls, the default A few familiar failure points: Fragmented Data: GPCR programs spew data across files, folders, and inboxes Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn

  • When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue

    Johannes “JB” Broichhagen trained as a synthetic chemist — someone who trusted carbon–carbon bonds far 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

  • Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal

    Why Speed Matters in GPCR Drug Discovery Nine out of ten GPCR programs stall  not because the target Programs stall. Timelines stretch. programs to advance or kill. Program Kill vs. Advance: What Real Teams Do How do large pharma teams decide whether to advance or pause a GPCR program

  • Mechanism vs. Assumption: A Model-First Path to Getting GPCR MoA Right

    Hi GPCR Community, If you work on GPCR discovery, you already know: early signals can mislead, and timing across oncology, metabolic, CNS, and fibrosis programs. Track, GPCR Happy Hour, and more! GPCR innovation is accelerating. community platform to help train and inspire the next generation of scientists.

  • Competitive vs Non-Competitive GPCR Antagonists: How to Interpret Pharmacology Data with Confidence

    your conclusions, your experiments, and even your program’s credibility. clear framework for distinguishing these mechanisms and avoiding common pitfalls that can derail a program data interpretations that can lead to costly dead ends and missed opportunities in your drug discovery program Sharpen your discovery decisions ➤ Yamina's Consulting Corner - Building Your GPCR Program for Breakthroughs Learn how to transform your program from a series of disconnected efforts into a predictable, de-risked

  • From Farm Fields to GPCR Discovery, GLP-1 and GIP

    Later, exposure to veterinarians working in agricultural settings inspired him to train in veterinary — the “interface” between brain and body. GPCRs Re-Enter the Story — Not as Theory, but as Tools GPCRs have always been powerful drug targets — That partnership eventually produced fluorescent GPCR tools  that allow researchers to visualize GPCR Can GPCRs act as “delivery ZIP codes” for targeted therapies?

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