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G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements

August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily, have gradually entered the field of vision of

particle cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs) in complex with G proteins or arrestins.

Masterclass on GPCR Allostery: Unveiling Techniques to Decode Drug Behavior – July 31st, 2025. Welcome back GPCR fans, If your drug discovery strategy still relies on static GPCR models, you’re already behind. Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor behavior in real-world systems. That’s exactly what Terry’s Corner delivers this week: high-impact insight into GPCR allostery, crafted for pharmacologists and biotech scientists who need to translate mechanistic nuance into better decision-making. 🔍 This Week in Premium: Sneak Peek Industry insights:  Strategic biotech alliances (Chemspace/Enamine, Superluminal Medicines), Novartis financial leadership shakeup, and next-gen GPCR targeting platforms reshaping immunotherapy pipelines. Upcoming events:  GPCR-UK Network Meeting, neuroGPCR symposium, and Transatlantic ECI GPCR event—where discovery and collaboration intersect. Career opportunities:  Exclusive pharma and academic listings you won’t find on job boards—curated for translational scientists and GPCR specialists. Must-read publications:  CXCL12 dimer impact on AML migration, mechanosensitive behavior in GPCRs, and in vivo APLNR biosensor imaging. Terry's Corner : Stop Chasing Affinity and Start Reading the System In this week’s cornerstone Terry’s Corner lecture, Dr. Terry Kenakin reframes GPCRs as dynamic, allosteric sensors—far from static binding sites. This is the lens that lets scientists anticipate drug effects, decode kinetic behavior, and optimize probe-dependent signaling. What you’ll learn: Reveal cryptic binding sites and time-dependent interactions.  Some drugs take hours to reach equilibrium—not because of poor design, but because the system is fluid. Learn how to decode that fluidity. Exploit probe dependence to shape precision pharmacology.  Want to avoid off-target effects? Understand how GPCRs react differently depending on the probe. Map dynamic receptor behavior to real-time decision-making.  Allostery is not passive—it’s predictive. Leverage this model to stay ahead of therapeutic complexity. To stay in the know on upcoming courses and AMA session, get the complementary Kenakin Brief , the weekly newsletter delivered directly to your inbox. Sharpen your discovery decisions ➤ GPCR Signal Transduction Call for Papers: Define What Comes Next Volume I was just the beginning with over 28K reads. As the GPCR field surges forward—from ligand bias to signaling diversity—the guest editors Dr. Lauren Slosky, Stuart Maudsley and Yamina Berchiche invite your insights for Volume II. This is a chance to shape the next scientific consensus on how GPCRs work, signal, and fail. Why this matters: Secure your voice in the next chapter of GPCR science.  Your work belongs in the core conversation—not buried in supplementary files. Position your research for maximum visibility.  This is where funders, peers, and biotech scouts are watching. Contribute to an evolving field still rich with firsts.  Volume II isn’t about repetition—it’s about redefining signal transduction. 📝 Manuscript summary deadline: 23 Sept 2025 📄 Submission deadline: 11 Jan 2026 Submit to Volume II ➤ Discovery On Target: Where the Next Decade of GPCR Drugs Begins If you’re not attending the GPCR-focused sessions at Discovery On Target 2025, you’re missing where the field is headed. It’s the 20th anniversary—and the spotlight is squarely on kinetic modeling, allosteric frameworks, and targeting the “undruggable.” 🔥 Featured:  Dr. Terry Kenakin on “The Kinetics of Allostery: The Added Benefits of Allosteric Function.” Why you need to be there: Learn how kinetic nuance shapes ligand design.  Don’t just measure residence—understand it. Access peer insights on allosteric modulators and biased ligands. Join the conversation on computational targeting and next-gen selectivity. Register for Discovery On Target ➤ What our community is saying “I enjoy the breadth of questioning that goes beyond just the science, and reveals a bit about the scientists as individuals/mentors/people.” — Dr. GPCR Podcast Listener Why Dr. GPCR Premium Membership Gives You an Edge Premium delivers curated, noise-free intelligence every week: deep-dive expert lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—designed to help you move faster, smarter. If you work on GPCRs across translational pharmacology, drug development, or molecular pharmacology, this is your decision advantage. Our Premium Members don’t have to chase signals—they act on them. FAQ: What You Get with Dr. GPCR Premium 🔹 What’s included? The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive on-demand expert frameworks, and member-only discounts. 🔹 Who is it for? GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who need fast, curated, career-relevant intelligence to stay ahead. 🔹 Why now? The pace of GPCR innovation is accelerating. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming. 👉 Access all the news and upcoming events ➤ 👉 Already a Premium Member?  Read the Full Edition here ➤

This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

Engineered G protein-coupled receptors (GPCRs) are commonly used in chemogenetics as designer receptors

October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental G protein-coupled receptors, the largest family of membrane proteins in eukaryotes and the largest drug Among them, the secretin/adhesion (Class B) G protein-coupled receptors are essential drug targets for Given the great value of the secretin/adhesion (Class B) G protein-coupled receptors in the regulation

October 2022 "Adhesion G protein-coupled receptors (aGPCRs) are keys of many physiological events and A comparison of Gq, Gs, Gi, G12 and G13 engagements with GPR110 reveals details of G-protein engagement Taken together, our study fills the missing information of GPCR/G-protein engagement and provides a framework

The company has long-standing expertise in G protein–coupled receptor (GPCR) biology—one of the most

August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing using ligands with differing levels of selectivity and affinity as GPR84 antagonists. Although blockade of GPR84 may potentially prove effective also in diseases associated with inflammation of the lower gut there is emerging interest in defining if agonists of GPR84 might find utility in conditions in which regulation of metabolism or energy sensing is compromised. Here, we consider the physiological and pathological expression profile of GPR84 and, in the absence of direct structural information, recent developments and use of GPR84 pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Proton-sensing G-protein coupled receptors are activated by acidic environments, but their role in fibrosis Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in

this review, we will discuss the regulation of mTORC1 by upstream stimuli, with a specific focus on G-protein

Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled

Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination type depends on the molecular recognition of two peptidyl mating pheromones by their corresponding G-protein

September 2022 Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epithelium That Directs P-Glycoprotein Expression "P-glycoprotein (P-gp) is a key component of the intestinal epithelium playing a pivotal role in removal of toxins and efflux of endocannabinoids to prevent excessive inflammation and sustain homeostasis. Recent studies revealed butyrate and secondary bile acids, produced by the intestinal microbiome, potentiate the induction of functional P-gp expression. We now aim to determine the molecular mechanism by which this functional microbiome output regulates P-gp. RNA sequencing of intestinal epithelial cells responding to butyrate and secondary bile acids in combination discovered a unique transcriptional program involving multiple pathways that converge on P-gp induction. Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the RNA sequencing findings and discovered a role for intestinal HNF4α in P-gp regulation. These findings shed light on a sophisticated signaling network directed by intestinal microbial metabolites that orchestrate P-gp expression and highlight unappreciated connections between multiple pathways linked to colonic health." Read more at the source #DrGPCR #GPCR #IndustryNews

Unlocking the Puzzle: The Importance of Precision in GPCR Programs and the Hidden Costs of Overlooking Details. A GPCR program can have world-class science, top-tier talent, and millions in funding — and still fail. Not because the science is wrong. Not because the people aren’t brilliant. But because the program is run on duct tape and heroics instead of precision. Your program isn’t slipping because of bad science — it’s bleeding money because your systems were broken before the first experiment ran. And every time your Head of Biology spends each night copy-pasting data instead of thinking about the next experiment, your program is bleeding six figures in lost time and wasted salaries. Brilliant minds doing low impact work is not a strategy. It’s a slow-motion car crash. Hiring Won’t Save Your GPCR Drug Discovery Program When a drug discovery program stalls, the default reflex is always the same: hire more people. Bring in a computational chemist. Add a data scientist. Surely more hands will move the needle. But here’s the reality: even ultra-specialized experts can’t fix systemic dysfunction in their spare time. They’re hired for science, not for building operational scaffolding. And when you chain your highest-paid scientists to repetitive admin work, you’re not solving problems — you’re multiplying them. Every two-week delay in a DMTA cycle can burn through hundreds of thousands in salaries and overhead. That’s not a hiccup. That’s a hemorrhage. Bad Data Management Is Undermining Your GPCR Drug Discovery Team The real problem isn’t competence. It’s the absence of operational precision. Even flawless experiments collapse under sloppy systems. A few familiar failure points: Fragmented Data: GPCR programs spew data across files, folders, and inboxes. Without a unified drug discovery data management  pipeline, teams waste hours cleaning, reconciling, and integrating before they can even think about analysis. A good ELN that pipes instrument outputs into a central hub — where QC, analysis, consumption and consolidation across assays — isn’t a luxury. It’s oxygen. Undefined Protocols: “We’ll figure it out” is not a workflow. Without clear rules of engagement, communication becomes chaos, progress gets lost in Slack threads, and insights die in inboxes. Ambiguous Decision Gates: Molecules advance or stall based on vibes, not criteria. That leads to premature investment in weak scaffolds or endless tinkering with dead ends. These aren’t minor oversights. They’re cracks in the foundation. And cracks don’t stay small for long. Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn’t more people or shinier assays. It’s a deliberate blueprint for precision. This doesn’t mean an overnight overhaul. It means a commitment to continuous improvement — starting with the highest-friction gaps and working upward. Plan, fix at the root, and stop fighting the same fire every week. The payoff? Progress that’s predictable, not reactive. The Hidden Costs of Poor Drug Discovery Data Management Stop pretending more hires or new assays will save you. They won’t. Every DMTA cycle lost to fragmented data and sloppy processes costs your company hundreds of thousands of dollars. That’s not “part of the process.” That’s a chaos tax — and you’re paying it in cash, time, and morale. If you want your program to survive, you need a Blueprint for Precision. Not next quarter. Not after the next fire drill. Now. Because the truth is harsh: in drug discovery, you don’t run out of science. You run out of money. And if your systems aren’t built for precision, you’ll run out fast. 👉 In Part 2, we’ll expose exactly how fragmented data cripples GPCR programs — and how to fix it before it sinks yours. And if you’re already seeing the cracks? Don’t wait for Part 2. Reach out. Let’s build the systems now, before the next delay burns another half a million. 🚀 Book your free 30-minute precision audit — before your next DMTA cycle costs another $200K Let’s unlock the momentum your GPCR program needs. 👉 https://calendly.com/drgpcr/yamina-corner Or explore how we can work together: 👉   Yamina.org

Ca2+ In combination these pathways allow complex presynaptic integration.SIGNIFICANCE STATEMENTTwo G

Are you ready to truly understand how pharmacologists predict whole-body drug response from a single experiment?   Terry Kenakin’s newest foundational lesson in Terry's Corner  cuts straight to it:   Why models are vital for translating lab data into clinical forecasts The 4 types of pharmacologic models (and when to use each) The truth about linear models: useful or misleading? How the Mass Action Law underpins nearly every model Future of Receptor Theory: Linkage vs. Probability Models   This is practical drug development expertise from Terry’s 40+ years of experience.   Beyond the lessons, Terry's Corner  is your exclusive gateway. Ecosystem Premium Members: Look for significant savings on this and other resources in your weekly Dr. GPCR News.   Elevate your pharmacology expertise. Unlock "Pharmacologic Models" now

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs

The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo signalling repertoire Common to all cytomegalovirus (CMV) genomes analysed to date is the presence of G Constitutive G protein-coupled M33 signalling is required for these phenotypes, although the contribution IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR) signaling

Join Dr. GPCR and global experts at the GPCR Drug Discovery session during Discovery on Target 2025—where groundbreaking collaborations begin. GPCR Drug Discovery at Discovery on Target 2025 — The Track You Can’t Miss If you work in drug discovery  or biotech , this is your moment. Mark your calendar, it's happening September 22-25, 2025. From obesity and diabetes to cancer, fibrosis, and CNS disorders — GPCRs  are at the heart of the world’s most pressing therapeutic challenges. And at this year’s Discovery on Target  meeting in Boston, the GPCR Drug Discovery track will deliver breakthroughs, bold ideas, and the strategies shaping the next wave of medicines . I’m honored to be chairing a session  in this track — with none other than Terry Kenakin  on the speaker lineup. 🌟 Speaker Spotlight In the run-up to the conference, our founder Yamina Berchiche is speaking with some of the brilliant minds presenting in the GPCR track. Here’s who we've talked to so far: 🎥 Check out the interview with Dr. Aaron McGrath from Takeda   🎥 Interview with Kris Borzilleri & Alison Heick Varghese from Pfizer 🎥 Interview with Terry Kenakin from UNC and Terry's Corner We'll continue to update this section as new videos are released — so check back before the meeting for fresh insights and behind-the-scenes perspectives from our speakers. 🌐 Why Dr. GPCR Is in This Conversation At Dr. GPCR , our mission is simple: connect the GPCR community, share knowledge, and accelerate innovation . At Yamina's Corner , our founder Yamina Berchiche works closely with organizations to help them navigate receptor pharmacology, identify opportunities, and move their programs forward effectively. Over the years, we’ve built a global network of researchers, biotech leaders, and pharma innovators who believe that GPCR science is one of the most powerful tools we have to address urgent health challenges. Chairing this session isn’t just another speaking engagement — it’s an extension of what we do every day: Spotlight innovation  across academia and industry. Foster collaboration  through our platform and events. Push the boundaries  of receptor pharmacology and its real-world applications. When we step into the GPCR track at Discovery on Target, we’re not just participating. We’re helping shape the conversation. 🚀 Why GPCRs Are Still the Hottest Target Class in Drug Discovery GPCRs regulate countless physiological processes, making them a goldmine for therapeutic breakthroughs. They’re already behind blockbuster drugs: GLP-1 receptor agonists  – reshaping obesity & type 2 diabetes care. CCR5 antagonists  – fighting HIV and certain cancers. Dopamine D2 receptor modulators  – transforming treatment for Parkinson’s & schizophrenia. PAR1 antagonists  – protecting cardiovascular health. But the real  excitement is in what’s next: Biased signaling  for selective therapeutic effects. Allosteric modulation  for unprecedented precision. Structure-based design  powered by cryo-EM and AI. 🔬 Inside the GPCR Track Agenda Expect deep dives into: CXCR4  in oncology and immune regulation. GIPR/GLP-1R co-agonists  in metabolic diseases. Serotonin & dopamine receptor modulation  for neuropsychiatric disorders. Orphan GPCRs  with untapped therapeutic potential. These sessions bridge structural biology , computational modeling , and clinical translation  — with tangible takeaways for programs from discovery through late-stage development. 🗝️  Highlight: Terry Kenakin at Discovery on Target Terry Kenakin’s work on functional selectivity  has transformed GPCR drug discovery, showing how to bias receptor signaling toward beneficial outcomes and away from side effects. Hearing Terry speak is more than an academic experience — it’s like being handed a new set of tools to rethink your drug design strategy. Having him in the session I’m chairing is not just an honor — it’s a highlight of the year.   📚 Terry’s Corner — The Only On-Demand Pharmacology Hub with Dr. Kenakin Himself If you’re part of the Dr. GPCR  community, you already know about Terry’s Corner  — our exclusive, on-demand pharmacology series where Terry Kenakin breaks down receptor pharmacology, functional selectivity, and ligand bias in a way you can apply directly to your work. It’s the only  resource of its kind — part masterclass, part fireside chat — available anytime to our members. For those who can’t get enough of Terry’s insights at Discovery on Target, Terry’s Corner  keeps the learning going long after the conference ends. 💡 Why This Matters — Even If You’re Not a GPCR Scientist GPCR pathways intersect with oncology, CNS, metabolic, cardiovascular, immunology, and fibrosis research . Whether you’re in early discovery or clinical development, the strategies here could open doors in your own therapeutic area. 🧭  Join Us in Boston 🗓 Discovery on Target  — Boston, MA 📅 September 23-25, 2025 🎯 Track:   GPCR Drug Discovery Let’s connect. Let’s debate. Let’s move GPCR drug discovery forward — together. 🚨 Mark your calendar for the GPCR Happy Hour Join us at GPCR Happy Hour , where scientists, biotech leaders, CRO professionals, and investors from around the globe meet Boston’s vibrant life sciences hub. ✨ Spark collaborations. ✨ Strengthen the GPCR community. ✨ Be part of Dr. GPCR’s nonprofit mission to connect and empower the global GPCR ecosystem. 📅 September 24, 2025 📍 Pressed Café, Huntington Ave, Boston ⏰ 6–8 PM EST ⚠️ Space is limited — Secure your spot now

Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle production and circulation of vasoconstrictors, resulting in enhanced signalling through their cognate G In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of a great variety

Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic analysis and review Odorant receptors (ORs) account for about 60% of all human G protein-coupled receptors

Why I Started GPCR Consulting You've got great data. You've got brilliant scientists. But your GPCR program still isn't moving at the pace it should. I've seen this pattern unfold across biotech, academia, and nonprofits. The assays are running, data is flowing in from your CROs or your internal labs , yet progress stalls. Decisions are slow, crucial data is siloed, and despite everyone working hard, programs drift. For over two decades, my work has centered on GPCR pharmacology . In every role and sector, I found myself drawn to the same critical challenges: missed opportunities, misaligned systems, and promising programs stalling despite strong science. I was always the one identifying what could be improved: The essential structure that was missing. The clarity that was desperately lacking. The unnecessary friction that slowed everything down. Traditional roles rarely gave me the freedom to implement these changes at the scale needed. So, I created a new path—one that allows me to embed, optimize, and accelerate GPCR programs from the inside out. The GPCR Data Dilemma: The Lego Bucket Problem I've seen promising GPCR programs generate massive volumes of high-quality data. But without structure, it's just a messy pile of colored blocks. I call this the Lego Bucket Problem . You have the data, but not the definitive direction. This disconnect frequently leads to: Underperforming assays. Internal data and CRO outputs  misaligned with strategic goals. Delays in critical go/no-go decisions. Frustrated teams and slipping timelines. It's not just a scientific issue—it's an operational one. You can't move fast without clarity, and you can't make confident decisions without robust structure. My Approach: Biology, Execution, Systems My consulting approach uniquely blends deep pharmacology expertise with the operational discipline required to make that expertise actionable. Here's how I bring a fresh perspective: Biology-First, Data-Driven Strategy:  I help you focus on the science that truly matters. We cut through the noise, elevate what's working, and strategically solve what's not, ensuring your GPCR program stays on target. Embedded Execution:  I work alongside your team—not above it. I'll help write CRO scopes, meticulously review assay data, flag risks early, and keep your programs relentlessly on track. Systems That Drive Progress:  From assay tracking to data workflows, I design simple, scalable tools that surface insights early and dramatically reduce delays, transforming your data into actionable intelligence. A Broader Lens: Dr. GPCR As the co-founder of Dr. GPCR, we've built a global hub connecting over 1,300 GPCR scientists dedicated to this field. These ongoing conversations keep me on the front lines, sharpening my understanding of the common bottlenecks and evolving needs across the entire GPCR community. My Consulting Philosophy This practice is built on three core values: Scientific Integrity:  Every recommendation is grounded in real-world evidence and extensive experience. Operational Discipline:  Robust systems and clear structure aren't "nice to have"—they are absolutely essential for efficient progress. Collaborative Partnership:  I embed, contribute, and build solutions hand-in-hand with your team. Ready to Move Your GPCR Program Forward? If you're navigating a stuck GPCR program, planning your next crucial milestone, or struggling to gain clarity from complex data, I'd love to help. 📌 Learn more about my services: Yamina.org 📅 Book a 30-minute strategy call: https://calendly.com/drgpcr/yamina-corner