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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

Pancreatic ductal adenocarcinoma, β-blockers and antihistamines: A clinical trial is needed Jillian G Baker ,  Erica K Sloan ,   Kevin Pfleger ,  Peter J McCormick , Cristina Salmerón ,   Paul A Insel PGxDB Schedule a session with our Chief Match Maker. Direct line to the Dr. fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research Associate - Professor Graeme Milligan

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.

GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who

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

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

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

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

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

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

A GPCR program can have world-class science, top-tier talent, and millions in funding — and still fail Let’s build the systems now, before the next delay burns another half a million. 🚀 Book your free 30

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

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

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