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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

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 solution is captured using a tip region of the flexible N-terminal tail of hETB via nonspecific attractive interactions Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated Further molecular dynamics simulation studies reveal an interaction between the βarr2 finger loop domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin complex, which regulates γ-secretase activity Collectively, these studies provide insight into the molecular and structural determinants of the APH1A-βarr2 interaction Read more at the source #DrGPCR #GPCR #IndustryNews

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

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.

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 "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

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

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 analyzing drug-target interactions and disease pathways, AI can identify potential candidates that

David Eliezer, et al. for their research on Control of G protein-coupled receptor function via membrane-interacting Are you interested in becoming a sponsor? for obesity and metabolic health GPCRs in Neuroscience Chronic modulation of cAMP signaling elicits activation of bombesin receptor subtype-3 Control of G protein-coupled receptor function via membrane-interacting GPCR Ecosystem

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

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 In cellular-adhesion assays, LK30 specifically broke the trans-cellular interaction of ADGRL3 with teneurin therapeutics" 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

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

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 If you’re still treating orthosteric and allosteric interactions as interchangeable, you’re leaving precision

GPCRs, are likely targets for antibody-based immune responses. Sakmar and Kotliar’s system is multiplexed and scalable , able to test hundreds of interactions from This is the future of GPCR immunology . ________________ Keyword Cloud : GPCR autoantibodies , GPCR immunology , GPCR diagnostics , Dr. GPCR ecosystem , multiplex assays

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 mouse versus human GPR116 and recapitulate these findings in a model supporting tethered agonist:ECL2 interactions 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

The interaction between two receptors in a dimer involves a conformational change in the transmembrane How dynamic are GPCRs dimer interfaces? GPCRs dimers exist in a transient state however they are still able to be activated and interact with What is the potential of targeting GPCR dimer interface in drug discovery? via%3Dihub #GPCR #DrGPCR#Ecosystem

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

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

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

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

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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

July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators The grant should help expand Confo Therapeutic’s research on G protein-coupled receptor (GPCR) drug candidates . " Read more at the source #DrGPCR #GPCR #IndustryNews

Welcome to the 4th official Adhesion GPCR Consortium newsletter! AB: I became aware of the existence of adhesion GPCRs while completing my graduate studies. Transitioning to study Latrophilins, I decided to test the interaction of neurexins with Latrophilins New Insights Members Torsten Schöneberg and Ines Liebscher present an interactive browser-based application PMID: 38311610 Member Dimitris Placantonakis’s identifies extended synaptotagmin 1 as an intracellular interaction

In the endosomes, sustained G protein signaling has been associated with prolonged interactions between GPCRs, G proteins, and arrestins on endosomal membranes3,4. GPCRs have also been identified within the mitochondria. Sustained cyclic AMP production by parathyroid hormone receptor endocytosis. Persistent cAMP Signaling by Internalized LH Receptors in Ovarian Follicles.