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GPCR Summit 2022 held between October 10th and 16th. Dr. GPCR Summit is FREE for all Ecosystem site members! Become a member today, it's also free! ➡️ https://bit.ly/3wKZmfR #gpcr #drgpcr

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. Finally, immunofluorescence data showed that SST2 and SST5 recruitment at the plasma membrane and internalization Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR Summit is between October 10th to the 16th! ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr

The first Nobel prize that can be attributed to work related to GPCR-mediated signaling was the 1947 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 signaling pathways with other cellular signaling pathways, as well as non-signaling roles of GPCRs, Interaction of G-Protein βγ Complex with Chromatin Modulates GPCR- Dependent Gene Regulation.

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. 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

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

2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

What does DNA Day have to do with GPCRs? GPCR biology, the development of GPCR-targeted drugs, and the exploration of GPCRs as key regulators Also, ongoing research may discover new GPCRs or refine existing data, which could lead to adjustments in the total count of GPCR genes in the human genome. Structural bioinformatics analysis of variants on GPCR function.

Add a data scientist. Surely more hands will move the needle. Bad Data Management Is Undermining Your GPCR Drug Discovery Team The real problem isn’t competence. A few familiar failure points: Fragmented Data: GPCR programs spew data across files, folders, and inboxes Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn cripples GPCR programs — and how to fix it before it sinks yours.

Classification: AI models can be used to distinguish GPCRs from non-GPCRs, and to classify GPCRs into The models use a variety of data for the input, including amino acid sequences or structural data (from GPCR-ligand interactions: ML can predict GPCR-ligand interactions based on input data of protein sequences data, to identify potential drug targets within the GPCR signaling pathways. 9. By integrating this data with GPCR-related knowledge, AI can help identify patient-specific GPCR targets

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

Hello Sweet GPCR Enthusiasts, This week at Dr. GPCR: a new podcast episode with Dr. GPCR Updates   New Podcast Episode  - When to Walk, When to Run with Dr. GPCR Store is live!   — A tale of detergent tails: GPCR activation beyond ligands .   GPCR Team

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

Watch Episode 171 What happens when your protein has no known ligands, no structure, and very little data 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 By iteratively refining the models with docking and mutagenesis data, they developed predictive pipelines computational chemistry is no longer a side tool—it’s a driver of discovery , especially when experimental data

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. For complex GPCR systems, this boundary is a strategic advantage: NAMs can only shift an agonist curve GPCR innovation is accelerating, and those who invest in deeper GPCR pharmacology insights today will

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 inverse agonism. ✅ Practical insights into designing assays that mimic pathophysiology , producing data The Hidden Lever in GPCR Research In GPCR pharmacology, the conversation often centers on ligand properties—affinity reveals drug properties earlier in the pipeline translates directly into better prioritization, cleaner data What emerges is not just more data—it’s the right data, positioned to inform strategic decision-making

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

GPCR signaling almost never follows a straight path. make course corrections before trials derail. ✅ Practical strategies  for using receptor trafficking data This lecture challenges the habit of treating in vitro data as destiny. You’ll understand why this is good news, not bad data, and how it can actually prevent harmful reflex Here’s what you’ll get: Weekly expert sessions  that turn messy data into clear decisions On-demand access

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

🧠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

Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just GPCR University Exciting news! We are pleased to announce the scheduled dates for our highly anticipated courses led by Dr. GPCR Event Highlight Get ready for the 11th Adhesion GPCR Workshop! GPCR Ecosystem

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

By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

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