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Hello Readers👋, GPCR weekly newsletter is here! GPCR Symposium event held on March 24th. GPCRs in Neuroscience Physiological Condition Dependent Changes in Ciliary GPCR Localization in the Brain Structural details of a Class B GPCR-arrestin complex revealed by genetically encoded crosslinkers in GPCR Ecosystem

Hello GPCR friends👋, Stay informed with the latest developments in GPCR research and industry news! GPCR Symposium is coming up on July 21st on Structural and Molecular Insights on GPCR Activation. Reviews, GPCRs, and more Advancements in G protein-coupled receptor biosensors to study GPCR-G protein Application of computational methods for class A GPCR Ligand discovery. GPCR Ecosystem

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

GPCR activation typically occurs through the binding of agonists which stabilize receptor conformations Natural and synthetic ligands can be categorized into four distinct efficacy classes: 1) full agonists GPCR targeting drugs: orthosteric vs allosteric sites Most of the drugs targeting GPCRs bind to the orthosteric GPCRs functional selectivity Recent research has revealed a more intricate understanding of GPCR behavior selectively activate specific cellular outcomes linked to that GPCR.

Many GPCR scientists trace their origin story back to a single unexpected spark. Not a grand plan. She went from reluctant intern to global researcher shaping how we understand GPCR spatial signaling. 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.

What emerged wasn’t just another pharmacology group — it became a collaborative engine for GPCR discovery The Power of GPCR Collaboration: Funding as a Force Multiplier Collaboration sounds warm and fuzzy. This ecosystem outlasted individual PIs  and became a GPCR innovation hub  with global reach. GPCR science thrives in complexity — meaning no single lab or company can do it alone. GPCR Premium  for deep dives, strategic tools, and behind-the-scenes conversations shaping the GPCR field

That’s not a story about nostalgia — it’s a snapshot of how GPCR research was built, on technique at The Era of Cold Fingers and Patience Back then, GPCR signaling experiments weren’t elegant; they were Every step felt like it could make or break the result, The pace and precision of GPCR research today The GPCR field needs thinkers who can direct platforms, not just operate them. GPCR Podcast 🔓 Get tools, deep dives, and exclusive insights with   Dr. GPCR Premium .

Historically, ligands for GPCRs have been identified before their receptor counterparts. Orphan GPCRs have been shown to play key roles in various physiological functions, such as sensory perception Therefore, matching a ligand to an orphan GPCRs, the process of de-orphanizing, is of great importance GPR84 is a Gi‐coupled class A GPCR mainly expressed in immune cells and microglia in the brain (Wojciechowicz #GPCR #DrGPCR#Ecosystem

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

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

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.

Hello GPCR Community, Stay up-to-date with the latest GPCR research, including breakthrough studies, Lukas Grätz , Jan Voss , and Gunnar Schulte , for their study on Class-Wide Analysis of Frizzled-Dishevelled Plus, access to over 500 minutes of recorded classes of our GPCR Courses with Drs. Kenakin's upcoming classes. We’re committed to making education accessible to all! Function Delineating the stepwise millisecond allosteric activation mechanism of the class C GPCR dimer

Hello GPCR Enthusiasts, Interpreting binding data isn’t optional—it’s career-defining. GPCR Premium: Sneak Peek Every week, Premium Members get curated intelligence they won’t find in open 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. The pace of GPCR innovation is accelerating.

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.

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. shows how this plays out in model systems and clinical data—and why residence time should be a first-class GPCRs now have validated intracellular  allosteric sites.

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.

Upcoming events:  Adhesion GPCR Workshop; GRC—Transporters, Ion Channels & GPCRs; MPGPCR Joint Satellite GPCR Podcast: Chemical Probes for GPCR Imaging with Dr. GPCR Premium Membership Gives You an Edge Premium gives GPCR scientists and biotech teams a single, trusted GPCR and the offered resources in my work sphere." GPCR research and education across the global community.

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.

Following the Data Into GPCR, Metabolic Disease and GLP-1 After his PhD, Hodson entered neuroendocrinology 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?

Listen to the episode ➤ Quick Links Assess GPCR Biased Signaling of Agonist How GPCR Collaboration Built an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling GPCR Premium Membership Gives You an Edge Premium delivers a clear, noise-free stream of GPCR intelligence GPCR innovation is accelerating. GPCR Team

11] Through Nobel prize-winning research work, Wald made important discoveries on the role that the class-A archetypical GPCR rhodopsin plays in scoptic vision and night blindness. 2004 Nobel Prize in Physiology or Medicine went to Richard Axel and Linda Brown Buck for their work on Class-A These odorant receptors (ORs) now account for about 60% of all identified human GPCRs. GPCR signaling, and location bias.[68–70] Further, our understanding of cross-talk between GPCR-mediated

GPCR. Dear Dr. GPCR, it was with a simple goal: to connect people who shared a passion for GPCR science and discovery GPCR Foundry  — our R&D and biotech hub designed to bridge GPCR science with execution. The Dr. GPCR resources, connect new scientists, and earn rewards  for helping expand access to GPCR knowledge GPCR About Dr. GPCR Dr.

His work highlights how foundational GPCR science can drive therapeutic innovation. The GPCR Angle Ben sees GPCRs as untapped goldmines for drug discovery. Ready to dive deeper into GPCR drug discovery? Want to push the boundaries of GPCR drug discovery? Start learning with our GPCR University today. _______________ Keyword Cloud: GPCR research community , GPCR drug discovery, mu-opioid receptor, positive allosteric modulators, GPCR training program, GPCR

For decades, GPCRs have been the cornerstone of pharmacology. GPCR Modeling in Context: Then and Now When Carlsson entered the GPCR field in the early 2000s, structural Why Predictive GPCR Modeling Matters Now The convergence of machine learning, improved GPCR structures Want to go deeper into GPCR modeling? Dr. GPCR Podcast Push the boundaries of what's possible 👉 Join the Dr.

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

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.

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.

function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR OR51E1 and OR51E2, initially assumed to be GPCRs only expressed in prostate tissue, play a role in prostate of GPCRs. expression of ORs is generally more technically challenging compared with expression of nonolfactory GPCRs Check the original article at https://pubmed.ncbi.nlm.nih.gov/35999088/ #GPCR #DrGPCR#Ecosystem