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  • Subscribe to Dr. GPCR Newsletter Today!

    Did you know that each month we collect the most recent #GPCR publications and the newest Biotech/Pharma GPCR-related news? GPCR monthly newsletter for FREE! ➡️ https://bit.ly/3cCI4em #gpcr #drgpcr

  • Learn about Dr. GPCR Ecosystem!

    GPCR is much more than a podcast? Come check out the brand new Dr. GPCR Ecosystem and explore its benefits! We have #GPCR News, Learning Center, Events, and more to discover! Learn More HERE ➡️ https://www.ecosystem.drgpcr.com/learning-center #gpcr #drgpcr

  • Integrating Fluorescent Ligands into Flow Cytometry: Enhancing GPCR Analysis Beyond Traditional Antibody Staining

    In order to expand its role in GPCRs, which antibodies tend to have more trouble binding to. How Fluorescent Ligands Transform Flow Cytometry in GPCR Analysis GPCRs are a tough target in traditional ligands provide new capabilities: -            Real time tracking they allow continuous observation of GPCR conjunction with fluorescent tags to study biased signaling pathways, improving our understanding of GPCR Illuminating the life of GPCRs.

  • Structural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling

    However, the detailed mechanism of aGPCR activation remains elusive. The structures also unveil the rarely explored GPCR/G12 and GPCR/G13 engagements. Taken together, our study fills the missing information of GPCR/G-protein engagement and provides a framework for understanding aGPCR activation and GPR110 signaling." Read more at the source #DrGPCR #GPCR #IndustryNews

  • Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling

    August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases, and arrestins - preferentially bind active GPCRs. Our analysis suggests that the structures of GPCRs bound to these interaction partners available today In view of this, three possibilities are conceivable: (i) there are no generalizable GPCR conformations Read more at the source #DrGPCR #GPCR #IndustryNews

  • GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for...

    October 2022 GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches Read more at the source #DrGPCR #GPCR #IndustryNews

  • High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands

    High-content screening (HCS) has become a cornerstone in GPCR and phenotypic drug discovery, enabling For GPCR-focused programs, the ability to visualize receptor localization, internalization kinetics, In this blog, you’ll learn:  How HCS works and why it is increasingly central to GPCR-based drug discovery The resulting multiparametric datasets are well-suited for GPCR research, where receptor trafficking, For GPCR assay developers, HCS supports:  Quantitative visualization of receptor internalization and

  • GPCR Drug Discovery at Discovery on Target: Why This Track Is About More Than Receptors

    GPCR and global experts at the GPCR Drug Discovery session during Discovery on Target 2025—where groundbreaking GPCR Is in This Conversation At Dr. GPCR , our mission is simple: connect the GPCR community, share knowledge, and accelerate innovation . 🚀 Why GPCRs Are Still the Hottest Target Class in Drug Discovery GPCRs regulate countless physiological Let’s move GPCR drug discovery forward — together. 🚨 Mark your calendar for the GPCR Happy Hour Join

  • Dr. GPCR Virtual Cafe - Postponed

    GPCR Virtual Cafe with Matthew Eddy scheduled for tomorrow (Sep 29th, 2022) due to Hurricane Ian that #gpcr #drgpcr

  • Automated micro-plate-based methods for quantifying GPCR activation

    Joe Clayton from BioTek Instruments talk about automated micro-plate-based methods for quantifying #GPCR activation. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #drgpcr #gpcr #virtualcafe

  • Lysosomal GPCR-like protein LYCHOS signals cholesterol sufficiency to mTORC1

    Read more at the source #DrGPCR #GPCR #IndustryNews

  • Dr. GPCR Summit 2022 is coming!

    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

  • Ode to GPCRs

    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.

  • 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

  • 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

  • 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

  • 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

  • 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

  • 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.

  • 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

  • Molecular creativity in drug discovery

    Innovative Approaches in GPCR Drug Discovery: Designing Precise Solutions for GPCR Challenges. GPCR Podcast: Leadership, Impact, and GPCR Signaling with Dr. GPCR evolved from a grassroots effort to a global force in GPCR science—one rooted in connection, sustainability The pace of GPCR innovation is accelerating. No matter where you are in your GPCR journey, Dr.

  • 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 Pharmacology Insights That Prevent Real Drug Discovery Failures

    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

  • 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

  • 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

  • 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

  • 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

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