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  • Better GPCR Drug Discovery Decisions Start With Structured Learning

    You can now search courses by level, topic, or instructor. Legacy courses will migrate into this format over the coming weeks, with live courses returning in March In the meantime, Premium members continue to have full access to the legacy course pages. All courses remain included in Premium Membership. GPCR University courses — now included in Premium.

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

    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 The human genome encodes ~800 GPCRs, yet only around 15% are currently targeted by approved drugs — leaving from biotech and pharma to advance GPCR programmes from discovery through translation — experts in GPCR signaling, and GPCR oligomerization.

  • 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. Luck, Leadership & GPCR Signaling Michelle is clear: luck played a role. But so did choice. But luck only works if you say yes when the door opens. GPCR Podcast 🔓 Want to go deeper? Join   Dr. GPCR Premium  for exclusive tools, deep dives, and expert access.

  • 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. GPCR University Course Attendee Dr. Exclusive discounts on Terry’s Corner  digital pharmacology courses Priority access to insights from The pace of GPCR innovation is accelerating.

  • 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 rapidly internalizes CCR5, but the receptor recycles back to the surface just as quickly — offering only 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

  • 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 Allosteric Modulation and the Microcircuit Model of GPCR Pharmacology Understanding GPCRs as allosteric Emerging Families and Orphan GPCRs: Expanding the Drug Discovery Target Space Family A and B GPCRs — But the GPCR superfamily is considerably broader. Related Resources eBook: Insights into GPCR Drug Discovery and Development: Exploring GPCR-Ligand Interactions

  • Assay Volume Control: Your GPCR Drug Discovery Power Lever

    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. of Discovery Shaped pHSense From HTRF to pHSense: The Long Game of GPCR Innovation Most scientists only GPCR innovation is accelerating. Access this week’s full Premium Edition here ➀ What our members say "Thank you for bringing this course

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

    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. in real discovery programs On-demand lessons  designed for busy scientists Direct input  on future course Kenakin with your own enzyme or GPCR interaction puzzles.

  • 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 âž» Want more like this? 👉 Join the Dr. GPCR Premium Ecosystem  for behind-the-scenes access to GPCR innovators, exclusive deep-dives, and practical

  • 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. Predictive GPCR-Ligand Modeling Carlsson's work quickly shifted from curiosity to impact. For Carlsson, this marked a shift in how his lab approached GPCR research. He came to see that effective GPCR research requires true interdisciplinary integration.

  • How Schild Analysis Protects Your Conclusions in GPCR Research

    Listen to the episode ➀ Quick Links Assess GPCR Biased Signaling of Agonist How GPCR Collaboration Built With live GPCR University courses returning next year and platform capabilities expanding, Premium pricing You also gain access to member-only discounts, full GPCR University content, and an integrated view of GPCR innovation is accelerating. GPCR Team

  • Four Reasons to Measure GPCR Signaling Bias in Drug Discovery

    Introduction G protein-coupled receptors (GPCRs) don't simply switch on or off. at the same receptor can produce fundamentally different cellular outcomes, a phenomenon known as GPCR Measuring GPCR signaling bias in drug discovery is critical, as it forms a selection criterion for agonism 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

  • Dr. GPCR Spotlights Revvity’s pHSenseℱ Internalization Tools

    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.

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

    GPCR University  next year — with new courses and instructors. For the first time, University courses will be included in Premium Membership , giving members full access courses. researcher, you and your lab will receive a complimentary one-year Premium Membership  when you lead a course GPCR University course reserves five complimentary seats for students from developing countries — no

  • 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 From the Masterclass Library This week's featured course from the Masterclass Library: Unconventional GPCR Ligands with Terry Kenakin . This course examines prodrugs, biologics, irreversible inhibitors, and molecular glues — and how these GPCR Dr. GPCR is the intelligence and community platform for GPCR scientists.

  • Beyond HEK293 — Terry HĂ©bert on iPSC-Derived GPCR Models, Live April 16,

    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 Read the paper ➀ From the Masterclass Library This week's featured course from the Masterclass Library GPCR University Learner About Dr. GPCR Dr. GPCR is the intelligence and community platform for GPCR scientists.

  • 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 In this article, you'll learn: How GPCR calcium signaling assays work The advantages and limitations 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

  • 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 David Hodson needed molecules that were only one synthetic step beyond what JB was already making. It was the start of a scientific partnership with the potential to shift how GPCRs could be visualized Designing Reliable GPCR Imaging Tools for Real Biological Systems Success brought new challenges.

  • Is Your GPCR Drug Discovery Program Built for Breakthroughs or Breakdowns?

    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.

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

    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

  • 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 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.

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

    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. on-demand expert frameworks, and member-only discounts The pace of GPCR innovation is accelerating. ” - DrGPCR University Course Attendee Get a competitive advantage—Join Dr.

  • Enhancing GPCR Research Outreach | Dr GPCR University early-bird registration ends soon!

    We've got 11 GPCR papers, seven industry news pieces, a new GPCR event, and even a job ad.   Unlock a 25% exclusive discount on these courses with Dr. Courses Schedule and  Benefits Every Thursday at 10 am EST Online Lectures 1:1 meeting with Dr. with real-time kinetics Discovering new ligands and GPCR behaviors for unique drug profiles   GPCR Event GPCR Ecosystem

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

    Fluorescent probes illuminate the mysteries of GPCRs in cutting-edge research. Hi GPCR Community, If you work on GPCR discovery, you already know: early signals can mislead, and timing Track, GPCR Happy Hour, and more! The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, and member-only GPCR innovation is accelerating.

  • Illuminating C5aR Biology: The Role of Fluorescent Ligands in GPCR Research

    GPCRs are one of the most important families of therapeutic targets in the pharmaceutical industry Approximately one-third of the drugs currently in clinical use are GPCR ligands. The C5a anaphylatoxin chemotactic receptor 1, also known as CD88, is part of the rhodopsin family of GPCRs and C5aR-Chem1 (DiscoverX) transfected cell lines, along with the cAMP HunterTM eXpress C5aR CHO-K1 GPCR Trends in GPCR Drug Discovery: New Agents, Targets and Indications.

  • How a Failed Experiment Created a Powerful GPCR Imaging Tool

    Broichhagen aka JB, the goal was bold and elegant: Create a photo-switchable ligand to remotely control GPCR They had a tool that did bind the GPCR
 but not in the light-controlled way they wanted. The Moment a Failed Tool Became a GPCR Imaging Breakthrough What the compound did reliably do was label This solved a long-standing problem in GPCR biology: You can't understand signaling if you can’t see  The Larger Lesson for Scientists and Innovators This story isn’t just about a GPCR imaging tool.

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

    Those courses didn’t feel like career-defining moments at the time — just requirements to pass. 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 Emerging direction: Multi-target GPCR + myostatin-pathway combinations. Can GPCRs act as “delivery ZIP codes” for targeted therapies?

  • Posttranslational modifications in GPCR internalization

    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

  • GPCR Binding Affinity Experiments: Interpreting Data With Confidence as We Head Into 2026

    Terry’s Corner: GPCR Binding Affinity Experiments That Hold Up Orthosteric GPCR binding affinity experiments More new courses arrive weekly in 2026, expanding coverage across GPCR pharmacology fundamentals. GPCR Podcast: When GPCR Tools Scale Even the most elegant tools only matter when they scale beyond a id1514231064 YouTube: https://www.youtube.com/@DrGPCR Looking ahead to 2026: Live and on-demand University courses GPCR Premium Member And Lock in The Current Rate➀ https://www.ecosystem.drgpcr.com/gpcr-university-pricing

  • The Quiet Power of RGS Proteins: Rethinking Pain Pathways through GPCR Biology

    explicitly interested in GPCR signaling... but the thing about GPCRs... is you always kind of end up landing at a GPCR as a major target." GPCRs in the Background, But Always Present Even though his primary focus wasn’t GPCRs themselves, Serafini Takeaway Forget what you think you know about GPCR drug targets. data platform , GPCR training program , pain research , opioid signaling .

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