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- Why Intracellular Drugs May Hold the Key to GPCR Therapeutics
diffusion, offset kinetics, and rebinding ✅ Real-world examples of how residence time—not potency—predicts therapeutic coverage ✅ Insight into cryptic intracellular GPCR sites, including allosteric modulators only accessible Drugs Change the Game For decades, drug design has treated GPCRs as surface targets. The slow-offset compound stays on target longer, maintains therapeutic effect as concentrations drop, GPCRs now have validated intracellular  allosteric sites.
- GPCR Therapeutics Expands Scientific Advisory Board
May 2022 "Seoul, South Korea, 28 April 2022 – GPCR therapeutics, Inc., a venture-backed clinical stage company with an innovative approach to drug discovery based on targeting G Protein Coupled Receptors (GPCR GPCR just had a very successful first meeting including all the Scientific Advisory Board." Read more at the source #DrGPCR #GPCR #IndustryNews
- GPCR Therapeutics welcomes Dr. Ed Brennan as their new Vice President, Head of Clinical Development
Dr Brennan has extensive experience across all phases of clinical development, and across multiple therapeutic #biotech #lifesciences #appointment #GPCR #Oncology" Read more at the source #DrGPCR #GPCR #IndustryNews
- Dr. GPCR Updates
GPCR – Precision Tools for GPCR Assays Dr. GPCR and Celtarys Research have teamed up. features a discussion about a scalable GPCR-RAMP assay. Their global resource is now helping labs decode GPCR biology at scale. It’s exciting to see how the GPCR field is evolving. GPCR Team
- Dr. GPCR and GeneTex Partner to Engage the Community on Anti-GPCR Antibody Challenges
GPCR, a nonprofit organization serving the global G protein-coupled receptor (GPCR) research community research and GPCR drug discovery. GPCR. GPCR Dr. GPCR supports scientists and organizations advancing GPCR biology and GPCR-targeted drug discovery.
- Dr. GPCR and Eurofins DiscoverX Join Forces to Accelerate GPCR Drug Discovery
GPCR , the global knowledge hub for G protein-coupled receptor (GPCR) research and education, today announced GPCR . GPCR Dr. GPCR is a nonprofit organization connecting the global GPCR community through training, curated news GPCR empowers scientists and organizations advancing GPCR biology and GPCR-targeted drug discovery.
- GPCR Happy Hour Boston 2026 — April 29 | Dr. GPCR Community Event
That's why we created GPCR Happy Hour. On April 29th, the Dr. Who's making the GPCR Happy Hour evening possible GPCR Happy Hour is made possible by four companies Whether you're decoding signaling pathways or designing the next generation of therapeutics, Revvity The first company to offer access to recombinant GPCR assays. targets, trusted by therapeutic developers worldwide for affinity, potency, efficacy, and functional
- Targeting GPCRs in the CNS: Advances in Drug Discovery Strategies
and the complexity of the central nervous system (CNS) pose a challenge for developing successful therapeutics Emerging GPCR Therapeutic Targets in CNS Drug Discovery GPCRs have been studied for decades, but there Of the traditional GPCRs, CBRs are gaining ground as potential therapeutic targets in several CNS diseases One of the best tools to study therapeutic targets are fluorescent ligands , which are very useful in G-Protein-Coupled Receptors in CNS: A Potential Therapeutic Target for Intervention in Neurodegenerative
- Accelerating GPCR Drug Discovery
But your GPCR program still isn't moving at the pace it should. The GPCR Data Dilemma: The Lego Bucket Problem I've seen promising GPCR programs generate massive volumes GPCR As the co-founder of Dr. GPCR, we've built a global hub connecting over 1,300 GPCR scientists dedicated to this field. Ready to Move Your GPCR Program Forward?
- Exciting GPCR Events for Next Year! + GPCR Weekly Rocket Launch ⦿ Oct 28 - Nov 3, 2024
Get your space suits on, GPCR cadets! et al. for their fantastic review on Molecular and structural insights into the 5-HT2C receptor as a therapeutic - Targeted Antibody Therapeutics Using Generative AI Zombie Fungi Hijack Hosts’ Brains GPCR Therapeutics Jobs Scientist I Cell Biology - Tectonic Therapeutic PhD fellowship in GPCR mechanosensing Senior Scientist proteins in obesity and diabetes mellitus Molecular and structural insights into the 5-HT2C receptor as a therapeutic
- GPCR Selectivity Beyond the Receptor
GPCR Allosteric Modulators as Intracellular Molecular Glues Standard models attribute signaling specificity Examples spanning GPCR families A, B, and T suggest that interface-directed modulation may represent From the Masterclass Library This week's featured course from the Masterclass Library: GPCR Projects: GPCR Course Attendee About Dr. GPCR Dr. GPCR is the intelligence and community platform for GPCR scientists.
- Fluorescence Polarization in GPCR Research
compounds that interact with molecular targets involved in disease pathways is where the development of new therapeutics Target-based screening is now a fundamental pillar of drug development, and GPCRs are key targets for How Fluorescence Polarization Assays Work: Principles and Applications in GPCR Research FP assays work Compatible with various sources of GPCRs. Contact us  to drive further advancements in GPCR drug discovery! Â
- GPCR Drug Discovery Summit 2026: What to Expect in Boston — and How to Register
an enormous and largely untapped therapeutic opportunity. · OMass Therapeutics · Superluminal Medicines · Tectonic Therapeutics · and many more. , Biagon, Iambic Therapeutics, Lembas, and Eli Lilly. , and Abilita Therapeutics. Will Barnes is Executive Director and Head of GPCR Biology at Iambic Therapeutics, where he leads AI-driven
- Understanding Biased Signaling in GPCRs
GPCR Allosteric Modulators as Novel Intracellular Molecular Glues Classic models explain biased signaling Reserve your spot ➤ iPSC-Derived Systems for GPCR Signaling and Translation Heterologous systems such Key implications: iPSC-derived cardiomyocytes reveal GPCR signaling behaviors that differ from HEK293 GPCR Dr. GPCR brings together scientists working across GPCR biology, pharmacology, and drug discovery to examine
- From Farm Fields to GPCR Discovery, GLP-1 and GIP
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 The Future of GPCR Therapeutics in Metabolic Disease Even with GLP-1 and GIP agonists reshaping diabetes Emerging direction: Multi-target GPCR + myostatin-pathway combinations. Can GPCRs act as “delivery ZIP codes” for targeted therapies?
- Dr. Juan José Fung - Dr. GPCR Podcast
GPCR Podcast is back this week with a brand new episode. Our guest is none other than Dr. Juan Jose Fung, Principal Scientist, at GPCR Therapeutics. https://buff.ly/32fzGbO #gpcr #drgpcr #podcast
- Four Reasons to Measure GPCR Signaling Bias in Drug Discovery
Measuring and quantifying signaling bias reveals which candidates emphasize therapeutically beneficial Pathway Pharmacological Fingerprint To obtain a pharmacological fingerprint (or profile) for GPCR therapeutics Both assays provide unique profiles and a preferred receptor signaling bias for the therapeutics tested Once a favorable efficacy fingerprint is identified in therapeutic cells (through cell-based assays), Journal of Pharmacology and Experimental Therapeutics, 344 (3), 708–717. https://doi.org/10.1124/jpet
- Five GPCR Masterclasses Before The Summer
Sam Hoare  — How Signaling Kinetics Shapes GPCR Drug Action. May 14. Sudarshan Rajagopal  — The Spatiotemporal Revolution in GPCR Biology. May 21. Andrew Tobin  — How to Build Breakthrough GPCR Programs. June 4. GPCR community gathers in person next week. GPCRs Targeted Drug Discovery Summit  — April 28–30. GPCR Dr. GPCR is the intelligence and community for GPCR scientists.
- GPCR Collaboration: From Models to Medicine
That perspective changed the moment he entered GPCR research . The GPCR Challenge What makes collaboration non-negotiable in GPCR research is the biology itself. They offer extraordinary therapeutic promise —but their complexity makes them one of the hardest targets GPCR Models Don’t Discover Drugs—People Do In GPCR research, the biggest breakthroughs won’t come from GPCR Podcast 🌱 Build a career with purpose, not just papers The Dr.
- Advantages of Fluorescent Probes in GPCR Assays
GPCRs pose a critical challenge in drug discovery: a vast therapeutic potential with many targets yet However, over half of non-sensory GPCRs do not have drugs available in the clinic, opening the door to This means fluorescent probes enable a dynamic observation of GPCRs. common starting point for employing fluorescent probes in GPCR assays. Fluorescent ligands: Bringing light to emerging GPCR paradigms.
- How Collaboration Drives GPCR Discoveries
GPCR signaling wasn’t linear. It wasn’t clean. For years, the GPCR community wrestled with unreliable antibodies. Why GPCR Collaboration Is Essential for Modern Science Hodson makes the point bluntly: modern GPCR science Together, they push GPCR science faster. biggest opportunities will emerge: Building receptor-specific delivery systems for gene or peptide therapeutics
- Targeting Intracellular Allosteric Sites in GPCRs
GPCR activity, enabling greater specificity and fewer side effects. systems such as free fatty acid receptors (FFARs), now regarded as targets for therapeutic intervention and β-arrestin coupling, enabling the development of biased agonists and antagonists with distinct therapeutic Allosteric modulation is gaining prominence in GPCR therapeutics, with the discovery of an intracellular Biased allosteric modulators can enhance the safety and efficacy of GPCR-targeted therapeutics by selectively
- Integrated GPCR Drug Discovery: A Structured Framework for Modern Programs
GPCR University Masterclass — Integrated GPCR Discovery in Practice Dr. GPCR Masterclass ➤ Eurofins DiscoverX Partnership — Tools and Insight for GPCR Drug Discovery Modern and the expanding therapeutic landscape of extra-oral bitter taste receptors, including oncology implications GPCR Premium Membership Gives You an Edge GPCR drug discovery is accelerating — across obesity, CNS, GPCR operates as a membership-based, nonprofit initiative — built to strengthen the GPCR field through
- GPCR Happy Hour – Boston, Sept 2025
GPCR’s nonprofit mission to unite and empower the GPCR community worldwide FOMO is real: if you’re not Be Part of the GPCR Community Dr. GPCR is a nonprofit global community  dedicated to building a strong, connected GPCR ecosystem. delivers cutting-edge imaging and analysis that accelerates the discovery of new and life-changing therapeutics comprehensive approach enables Axxam to support clients worldwide in identifying and optimizing new therapeutic
- From GPCR Data Chaos to Decisive Action
Is Your GPCR Program Slowing Down—Even With Good Data? You’re not alone. GPCR Ecosystem. Strong science. Promising data. But no systems to turn it into momentum. GPCR, I’m connected to 1,300+ scientists and decision-makers worldwide. Who I Work With ✅ Biotech Teams  – Especially those lacking in-house GPCR leads or overwhelmed by CRO data chaos. ✅ Venture Capital Firms  – Looking to accelerate, troubleshoot, or validate GPCR assets
- Better GPCR Drug Discovery Decisions Start With Structured Learning
If you work in GPCR research, clarity is leverage. Upcoming events: 12th Adhesion GPCR Workshop; GPCRnet International Symposium; 5th GPCRs Targeted Drug GPCR University has undergone a structural redesign. GPCR Premium Membership Gives You an Edge GPCR science is accelerating across obesity, CNS, oncology, GPCR University courses — now included in Premium.
- Understanding Enzyme Inhibition In GPCR Discovery Programs
Enhancing scientific exploration by concentrating on understanding inhibition to advance GPCR drug discovery mutated GPCRs. , and concise reads on β-agonists, phospho-barcodes, and GPCR allostery. When “inhibition” becomes activation—and how that insight fuels next-gen therapeutic design. The pace of GPCR innovation is accelerating.
- Terry’s Corner, Celtarys' Leap, and the $7B GPCR Horizon
space focused on GPCR pharmacology. – GPCR mutations in cancer—drivers, passengers, or both? – CXCR4 oligomer disruption boosts therapeutic response in lymphoid neoplasms Dr. GPCR Podcast appearance. GPCR Team
- The Truth About GPCR Product Launches: Years in the Making
GPCR and Revvity. But there was a pivot: the tech had untapped potential for GPCRs. GPCR internalization isn’t just a trafficking readout—it’s pharmacology. 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
- Why GPCR Biologic Drugs Stabilize Active States Small Molecules Struggle to Reach
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.



























