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- Dr. GPCR Summit 2022 is coming!
GPCR Summit is between October 10th to the 16th! ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr
- GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...
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
- The complicated lives of GPCRs in cardiac fibroblasts
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. Here, we will focus on the relatively less well-studied effects of GPCRs in cardiac fibroblasts, focusing 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
- Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5...
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
- A cryptic mode of GPCR regulation revealed
2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of...
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
- From DNA day to GPCR genomics
What does DNA Day have to do with GPCRs? This intersection of genomics and GPCR research sparked a new era of a comprehensive understanding of GPCR biology, the development of GPCR-targeted drugs, and the exploration of GPCRs as key regulators in the total count of GPCR genes in the human genome. Structural bioinformatics analysis of variants on GPCR function.
- Aβ peptides stabilize GPCRs in inactive form and trigger inverse agonism in Alzheimer's disease
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
- Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR..
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 Read more at the source #DrGPCR #GPCR #IndustryNews
- Cholesterol occupies the lipid translocation pathway to block phospholipid scrambling by a GPCR
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
- GPCR kinases generate an APH1A phosphorylation barcode to regulate amyloid-β generation
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
- GPCR kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by...
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
- Unlocking the Future of Medicine: Advancements in GPCR Research
Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just GPCR University Exciting news! GPCR Event Highlight Get ready for the 11th Adhesion GPCR Workshop! GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs GPCR Ecosystem
- Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures
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
- The Imprecision Problem: Why Your GPCR Drug Discovery Program Is Off-Track Before It Even Starts
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 Bad Data Management Is Undermining Your GPCR Drug Discovery Team The real problem isn’t competence. Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn
- Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR...
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
- The Chemistry of Confidence: Aha Moments That Shape Scientific Careers
GPCR Podcast, is filled with such moments, from bombing her first high school chemistry test to co-founding a startup delivering tools for GPCR drug discovery. GPCR on the company page . _______________ Keyword Cloud: GPCR scientist network , career development , fluorescent ligands , GPCR training program , Dr. GPCR ecosystem , GPCR podcast
- Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
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 GPCR-ligand interactions: ML can predict GPCR-ligand interactions based on input data of protein sequences Predicting GPCR properties: AI models can predict various properties of GPCRs, such as ligand binding By integrating this data with GPCR-related knowledge, AI can help identify patient-specific GPCR targets
- Isoform-and ligand-specific modulation of adhesion GPCR ADGRL3/Latrophilin3 by a synthetic binder
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
- Decoding Olfactory GPCRs: How AlphaFold and AI Are Changing the Game
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 : Predicting the “Face” of a Receptor When Alessandro began his PhD, structural models of olfactory GPCRs —Alessandro Nicoli A New Era of GPCR Research AlphaFold didn’t just fill a gap—it shifted the focus of Start with our GPCR training program and get hands-on with virtual tools shaping the future of drug discovery
- Assay Sensitivity: The Hidden Lever Driving GPCR Drug Discovery
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 In an era of accelerated GPCR-targeting innovation, these advantages define which programs advance and GPCR members save 50%+ with your Weekly News code) 👉 Explore Trailers & Join Today Why Terry’s Corner
- 🧠Do you want to share your #GPCR knowledge?
🧠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
- Antibodies That Don’t Block, They Activate: A New Angle on Autoimmunity and GPCRs
Watch Episode 167 Some GPCR-targeting antibodies don’t inhibit receptors. They activate them. GPCRs, are likely targets for antibody-based immune responses. This is the future of GPCR immunology . ________________ Keyword Cloud : GPCR autoantibodies , GPCR immunology , GPCR diagnostics , Dr. GPCR ecosystem , multiplex assays
- Why Opposing Processes Matter for Your Next GPCR Drug
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
- In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors
By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling Read more at the source #DrGPCR #GPCR #IndustryNews
- Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist...
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
- GPCR Buzz of the Week | Sep 23 - 29, 2024
Welcome aboard, GPCR Crew! GPCR Event Spotlight 11th Adhesion GPCR Workshop 📍 Mexico City 📅 October 23 - 25, 2024 Get ready Classified GPCR News Let’s dive into the Classified GPCR News from September 23rd to 29th, 2024 Industry Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug
- Don't miss the chance to be part of the Dr. GPCR Summit 2022!
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
- Join Dr. GPCR Summit 2022 in 3 simple steps!
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
- Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery
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












