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- 📢 Early Bird Registration Ends Tomorrow! | Sep 16 - 22, 2024
Ahoy, GPCR Crew! peers and explore the cutting-edge advancements in adhesion GPCR biology! using polymer-encapsulated nanodiscs Google DeepMind And Isomorphic Labs Are Making Rapid Progress In Biology Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein Biochemist/Structural Biologist
- Functional Characterization of the Venus Flytrap Domain of the Human TAS1R2 Sweet Taste Receptor
sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs The TAS1R2 and TAS1R3 subunits are members of a small family of class C GPCRs whose members share the Read more at the source #DrGPCR #GPCR #IndustryNews
- Opioid Ligands Addressing Unconventional Binding Sites and More Than One Opioid Receptor Subtype
"Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR ) drug targets and also act as prototypical models for GPCR function. Read more at the source #DrGPCR #GPCR #IndustryNews
- Regulators of G-protein signaling: essential players in GPCR signaling
components of the intracellular signaling pathways that mediate the effects of G protein-coupled receptors (GPCRs Upon activation, GPCRs have conformational changes that allow the coupling and subsequent activation Role of RGS proteins in regulating GPCR signaling: Recent studies have revealed that the interaction The interaction between RGS proteins and GPCRs is highly specific and tightly regulated; mutations in and amplitude of GPCR signaling.
- Structure of the vasopressin hormone-V2 receptor-β-arrestin1 ternary complex
October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation Recent structural studies shed light on the molecular mechanisms involved in GPCR-arrestin coupling, but whether this process is conserved among GPCRs is poorly understood. It reveals an atypical position of β-arrestin1 compared to previously described GPCR-arrestin assemblies Read more at the source #DrGPCR #GPCR #IndustryNews
- 📰 GPCR Weekly News, May 29 to June 4, 2023
Hello GPCR friends👋, Stay informed with the latest developments in GPCR research and industry news! GPCR Symposium is coming up on July 21st on Structural and Molecular Insights on GPCR Activation. Reviews, GPCRs, and more Advancements in G protein-coupled receptor biosensors to study GPCR-G protein GPCR Events, Meetings, and Webinars FREE Symposium - IPI Surfacing (June 15, 2023) GPCRs in drug discovery GPCR Ecosystem
- 🎧Episode 85 of the Dr. GPCR podcast is here!
GPCR podcast is here! 🎧Hear Dr. GPCR Ecosystem membership or listen wherever you get your podcast for free.
- Diversification of PAR signaling through receptor crosstalk
Read more at the source #DrGPCR #GPCR #IndustryNews
- Chemical Drug Matter : Rethinking the Molecules We Choose to Develop In Drug Discovery
Indoles, benzodiazepines, phenethylamines — each recurs because it “fits” biology well. GPCRs are not simple on/off switches. therapeutic windows More predictable clinical behavior Allosteric modulation allows us to work with biology Does it interact with the receptor in a way that biology can use? GPCR innovation is accelerating.
- New structural perspectives in G protein-coupled receptor-mediated Src family kinase activation
Sandra Berndt talk about new structural perspectives in GPCR-mediated Src family kinase activation. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe #drgpcr #gpcr #virtualcafe
- Orthosteric Binding Experiments: How to Avoid the Most Common Data Pitfalls
Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry Take home message: interpret orthosteric binding data only after verifying that the biology behaved as Complex Two-Stage Biology Behind Orthosteric Binding GPCR pharmacology rarely follows the neat Langmuir Clues that point to true multiple-site binding rather than two-stage GPCR biology: Disrupting G protein
- Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine..
Autoimmune Diseases "The chemokine receptor CXCR3 is a seven-transmembrane G-protein-coupled receptor (GPCR The careful structural modifications during the lead optimization phase led to a compound with high biological Read more at the source #DrGPCR #GPCR #IndustryNews
- G protein-coupled receptor 21 in macrophages: An in vitro study
orphan and constitutively active receptor belonging to the superfamily of G-Protein Coupled Receptors (GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews
- Hear the sounds: the role of G protein-coupled receptors in the cochlea
G protein-coupled receptors (GPCRs) are crucial receptors that regulate a wide range of physiological Recently, several GPCRs have been found to play important roles in the cochlea. Frizzleds and Lgrs are dominant GPCRs that regulate stem cell self-renew abilities. Here, we review the key findings of GPCR in the cochlea and discuss the role of GPCR in the cochlea, Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
in which, the allosteric nature of GPCRs must be respected. Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery. Nature chemical biology. 2020;16(8):841-849. 44. Mini-G proteins: Novel tools for studying GPCRs in their active conformation. Cryo-EM structures of GPCRs coupled to Gs, Gi and Go.
- Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture of fungi...
scoring protective hits included the complement C3a receptor (C3aR), a G-protein coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
A much smaller conformational change of helix VI upon activation than previously solved class A GPCR-Gi Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor Read more at the source #DrGPCR #GPCR #IndustryNews
- Murine bone marrow macrophages and human monocytes do not express atypical chemokine receptor 1
FAB6695 and scrutinize the apparent ACKR1 expression in BM macrophages" Read more at the source #DrGPCR #GPCR
- Emerging approaches for decoding neuropeptide transmission
processing, release from dense core vesicles, and ability to activate G-protein-coupled receptors (GPCRs Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter HERE
- Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias...
essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews
- Unlock the Hidden Lives of Receptors – Are You Ready?
Imagine you're navigating a vast terrain—not on foot, but through the shape-shifting world of GPCRs.
- Fusion protein strategies for cryo-EM study of G protein-coupled receptors
microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack In GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly The fusion strategies explored here are likely applicable to cryo-EM interrogation of other GPCRs and Read more at the source #DrGPCR #GPCR #IndustryNews
- G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions...
representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR and the multifunctional scaffolding protein β-arrestin2 are key integrated signaling nodes in various biological Read more at the source #DrGPCR #GPCR #IndustryNews
- Comparative study of neuropeptide signaling systems in Hemiptera
Here, 33 neuropeptide precursors and 48 putative neuropeptide G protein-coupled receptor (GPCR) genes Read more at the source #DrGPCR #GPCR #IndustryNews
- Arginine 125 Is an Essential Residue for the Function of MRAP2
Read more at the source #DrGPCR #GPCR #IndustryNews
- Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
Originally, β-arrestins were identified for their contribution to GPCR desensitization to agonist-mediated However, current investigations have now recognized that in addition to GPCR arresting (hence the name Read more at the source #DrGPCR #GPCR #IndustryNews
- New Resources in GPCRdb
GPCR on the 24th of June! This time, the GPCRdb team ( Dr. David Gloriam , Dr. Reserve your spot for free at: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #GPCR #GPCRs #DrGPCR
- GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting
pro-inflammatory neutrophil response, signaling downstream of an agonist-activated G protein-coupled receptor (GPCR Among the family of GPCR kinases (GRKs) that regulate receptor phosphorylation and signaling termination analysis of subcellular fractions revealed a cytosolic localization. " Read more at the source #DrGPCR #GPCR
- Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...
Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled (GPCR Here, we show that a combination of insulin and the GPCR agonist neurotensin induced rapid activation Read more at the source #DrGPCR #GPCR #IndustryNews
- Structural view of G protein-coupled receptor signaling in the retinal rod outer segment
October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews








