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October 2022 GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral membrane and regulates epithelial apicobasal polarity "The adhesion family of G protein-coupled receptors (GPCRs GPR125 (ADGRA3), an orphan adhesion GPCR, has been shown to modulate planar cell polarity in gastrulating Thus, the basolateral protein GPR125, an autocleavable adhesion GPCR, appears to play a crucial role Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the newsletter HERE

October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system In VSMCs, stimulation of GPCRs also modulates contractile and cell growth phenotypes. We also review the hierarchy of signaling events driving the fibrotic response and the communications We discuss how such events may be distinct depending on where the GPCRs and their associated signaling Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5 homo- and hetero-dimer formation "The process of GPCR dimerization can have profound effects on GPCR activation, signaling, and intracellular trafficking. Somatostatin receptors (SSTs) are class A GPCRs abundantly expressed in pituitary tumors where they represent Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Negative Allosteric Modulator, ORG27569, and Analogs "A growing number of G-protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate Read more at the source #DrGPCR #GPCR #IndustryNews

Kenakin  highlighted a fundamental truth: GPCR systems do not offer stable, proportional input–output Teams equipped with deep GPCR pharmacology insights make different decisions. This is a core GPCR pharmacology insight:ligand → receptor → G protein is never the entire story. Common mechanistic traps: Alpha-driven effects misinterpreted as beta-driven, or vice versa. GPCR innovation is accelerating, and those who invest in deeper GPCR pharmacology insights today will

2022 Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR simulation was conducted to elucidate binding mechanisms of a middle-sized flexible molecule, bosentan, to a GPCR generalized ensemble method that produces a free-energy landscape of the ligand-receptor binding by searching Read more at the source #DrGPCR #GPCR #IndustryNews

For most researchers, that’s a dead end. For Alessandro Nicoli, it’s an opportunity. we explore how computational tools—especially AlphaFold —are helping crack the mystery of olfactory GPCRs The Problem: Hundreds of Receptors, Almost No Ligands Alessandro’s work focuses on olfactory GPCRs—nearly —Alessandro Nicoli For the first time, researchers had a reliable set of predicted structures to work —Alessandro Nicoli A New Era of GPCR Research AlphaFold didn’t just fill a gap—it shifted the focus of

September 2022 "Class A (rhodopsin-like) G protein-coupled receptors (GPCRs) are constitutive phospholipid scrambling is not detectable in the resting plasma membrane of mammalian cells that is replete with GPCRs considered whether cholesterol, a prominent component of the plasma membrane, limits the ability of GPCRs This mechanism may explain the inability of GPCRs to scramble lipids at the plasma membrane." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated reveal an interaction between the βarr2 finger loop domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin Read more at the source #DrGPCR #GPCR #IndustryNews

The Tools to Detect Them Using the multiplexed GPCR library and Luminex assay , researchers can now: antibody is activating or inhibitory Guide diagnostics or treatment research based on GPCR targets Beyond This is the future of GPCR immunology . ________________ Keyword Cloud : GPCR autoantibodies , GPCR immunology , GPCR diagnostics , Dr. GPCR ecosystem , multiplex assays

🧠Do you want to share your #GPCR knowledge? Come to Dr. GPCR Ecosystem and create a course on your favorite #GPCR research, technique and more… Available for GPCR Ecosystem paid memberships ➡️https://bit.ly/3R8ZZbo #gpcr #drgpcr

Artificial intelligence in GPCR drug discovery The use of AI in GPCR drug discovery has increased over Classification: AI models can be used to distinguish GPCRs from non-GPCRs, and to classify GPCRs into Predicting GPCR properties: AI models can predict various properties of GPCRs, such as ligand binding Automated tools for researchers: AI solutions which bring together theoretical, computational, and experimental Instead, it complements and assists researchers in the GPCR drug discovery process.

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated However, although necessary for some GPCRs, we found that distal C-tail sites might not be sufficient to specify recruitment of STAM1 to βarr1 for other GPCRs. Read more at the source #DrGPCR #GPCR #IndustryNews

For drug hunters working at the GPCR interface, the difference between a successful lead and a dead-end For GPCR drug discovery, those hidden details can determine whether a compound advances or stalls. The Hidden Lever in GPCR Research In GPCR pharmacology, the conversation often centers on ligand properties—affinity By reducing receptor density, researchers can transform full agonists into partial ones—allowing comparative In an era of accelerated GPCR-targeting innovation, these advantages define which programs advance and

Unlocking the Puzzle: The Importance of Precision in GPCR Programs and the Hidden Costs of Overlooking A GPCR program can have world-class science, top-tier talent, and millions in funding — and still fail Hiring Won’t Save Your GPCR Drug Discovery Program When a drug discovery program stalls, the default Without clear rules of engagement, communication becomes chaos, progress gets lost in Slack threads, Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn

October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical Recent advances in X-ray crystallography and cryo-EM have resulted in a wealth of GPCR structures that adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source #DrGPCR #GPCR

research community. Celtarys Research, now partnering with Dr. GPCR, is helping researchers worldwide gain access to customized, reliable assay tools without the delays drug discovery , GPCR research community , medicinal chemistry , Dr. GPCR ecosystem , GPCR online course , GPCR scientist network

The most diverse and common molecular target of drug medicines is G protein-coupled receptors (GPCRs) Fortunately, GPCR researchers have solutions at their disposal to overcome this challenge, essentially Biomedical researchers' perspectives on the reproducibility of research. G Protein-Coupled Receptors: A Century of Research and Discovery. Qualitative Research. 2015;16(4):446-467. 56.         Wilner W.

pharmacology and apply it to their research in academia and industry. Act Now and Become a Valued Member of our Learning Community! Agonist for the Treatment of Hypoparathyroidism Confo Therapeutics Announces Publication in Nature Communications Jobs HIGHLIGHT Research Associate - Professor Graeme Milligan HIGHLIGHT Postdoc in Molecular Pharmacology mechanosensing   Postdoctoral Position Postdoctoral research position Adhesion GPCRs The G Protein-Coupled

October 2022 Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of diseases, but few therapies have been directed against GPCRs in the field of cancer, partly because of the lack Here, using colorectal cancer (CRC) as a model, we explored the gene expression of a panel of GPCRs in Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR event of the year is the 3rd edition of the Summit. Come join us from October 10 to 16 to hear about exciting #GPCR research from amazing speakers. GPCR Ecosystem site member to attend the Summit, it’s free! ➡️ https://bit.ly/3SUkB8D #gpcr #drgpcr

September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular Modulating a single function of a specific aGPCR isoform while affecting no other function and no other Here, we engineered an antibody, termed LK30, that binds to the extracellular region of the aGPCR ADGRL3 Our work provides proof of concept for the modulation of isoform- and ligand specific aGPCR functions therapeutics" Read more at the source #DrGPCR #GPCR #IndustryNews

His work spans deep academic research, startup life, and the application of machine learning and pharmacology to GPCR drug discovery. Superluminal Medicines: AI/ML Meets GPCR Pharmacology As Ajay continued to explore how GPCR signaling Advice for Young Scientists For early-career researchers, Ajay’s journey offers a powerful blueprint. He also underscores the value of developing cross-functional skills — including communication, strategy

We welcome suggestions, feedback, and announcements from the community. research? If I wanted to be part of the narrative, I felt that I had to join the community. And so I did. AB: The next workshop will likely bring together some of the hottest adhesion GPCR research going on Also, seeing the expanding diversity among the aGPCR community, added to the fact that this will all

GPCR signaling almost never follows a straight path. This article is about one big idea: GPCRs don’t act in isolation—they respond to the system they’re in In this session, you’ll gain: ✅ A mental model you can trust  for predicting how GPCR ligands behave Internalized Signaling: Same Receptor, Different Story A GPCR response isn’t always over when the receptor Constitutive Activity: When Doing Nothing Still Does Something Some GPCRs simply refuse to stay quiet

GPCR Summit 2022 held between Oct. 10 - 16, it's FREE! Join the #GPCR movement by signing up now! ➡️ https://bit.ly/3cKMXlw #gpcr #drgpcr

October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered activation mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

But what are the conformation changes that drive GPCR dimerization? How dynamic are GPCRs dimer interfaces? GPCRs constantly bind to form dimers and dissociate to form monomers. But how can we target GPCR dimers? via%3Dihub #GPCR #DrGPCR#Ecosystem

GPCRs have also been identified within the mitochondria. Compartmentalized GPCR Signaling from Intracellular Membranes. Insights into Nuclear G-Protein-Coupled Receptors as Therapeutic Targets in Non-Communicable Diseases Nature communications, 8(1), 443. https://doi.org/10.1038/s41467-017-00357-2 Jong, Y. Neurochemical research, 42(1), 166–172. https://doi.org/10.1007/s11064-016-2026-6 Mendizabal-Zubiaga,