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Arrestins regulate a wide range of signaling events, most notably when bound to active G protein-coupled

GPR15 is a G protein-coupled receptor (GPCR) located on chromosome 3 and has similarity in its sequence

G protein-coupled receptors (GPCRs) are among the most promising drug targets.

They recognize two types of G protein-coupled receptors (LPARs): LPA1-3 receptors and LPA4-6 receptors

considered that TNBC is an estrogen-independent breast cancer, while a new estrogen receptor, namely G protein-coupled

conducted to elucidate binding mechanisms of a middle-sized flexible molecule, bosentan, to a GPCR protein

Alterations in the expression and/or activity of brain G-protein-coupled receptors (GPCRs) such as dopamine

G protein-coupled receptors (GPCRs) have been shown to play integral roles in Alzheimer's disease pathogenesis

Engineered G protein-coupled receptors (GPCRs) are commonly used in chemogenetics as designer receptors

the tethered agonist-dependent activities of all 33 aGPCRs in a suite of transcriptional reporter, G protein PMID: 38608683 The activation profile of different G proteins by ADGRL3 is shown using a collection of

We demonstrate that the chemoreceptor genes, srg-36 and srg-37, which encode G protein-coupled receptors

The cytoskeletal protein filamin A (FLNA) directly interacts with both somatostatin receptor type 2 (

Deadline February 12, 2023 Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology The Illuminating the Understudied Druggable Proteome Conference.

GPCR Activation and Signaling The GPCR adaptor protein Norbin regulates S1PR1 trafficking and the morphology

Molecular basis of proton-sensing by G protein-coupled receptors. bioRxiv .

is a potent neutrophil chemoattractant Methods & Updates in GPCR Research GproteinDb in 2024: new G protein-GPCR into GPCR Function Structural and signaling mechanisms of TAAR1 enabled preferential agonist design Proteome-wide

Industry News OMass Therapeutics Welcomes Melissa Faris as Chief Business Officer Septerna: Revitalizing G-Protein

Pharmacology - The Hauser Group Postdoctoral Scholar – iPSC in cardiac and endothelial cell function Protein

Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein

Odorant receptors function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled

adenosine 3’-phosphate 5’-phosphosulfate (PAPS) donor to the hydroxyl group of a tyrosine residue of the protein

August 2022 A new Kunitz-type snake toxin family associated with an original mode of interaction with the vasopressin 2 receptor "Abstract Background and purpose: Venomous animals express numerous Kunitz-type peptides. The mambaquaretin-1 (MQ1) peptide identified from the Dendroaspis angusticeps venom is the most selective antagonist of the arginine-vasopressin V2 receptor (V2R) and the only unique Kunitz-type peptide active on a GPCR. We aimed to exploit other mamba venoms to enlarge the V2R-Kunitz peptide family and gain insight into the MQ1 molecular mode of action. Experimental approach: We used a bio-guided screening assay to identify novel MQs and placed them phylogenetically. MQs were produced by solid-phase peptide synthesis and characterized in vitro by binding and functional tests and in vivo by diuresis measurement in rats. Key results: Eight additional MQs were identified with nanomolar affinities for the V2R, all antagonists. MQs form a new subgroup in the Kunitz family, close to the V2R non-active dendrotoxins and to two V2R-active cobra toxins. Sequence comparison between active and non-active V2R Kunitz peptides highlighted five positions, among which four are involved in V2R interaction and belong to the two large MQ1 loops. We finally determined that eight positions, part of these two loops, interact with the V2R. The variant MQ1-K39A showed a higher affinity for the hV2R, but not for the rat V2R. Conclusions and implications: A new function and mode of action is associated with the Kunitz peptides. The number of MQ1 residues involved in V2R binding is large and may explain its absolute selectivity. MQ1-K39A represents the first step in the improvement of the MQ1 design from a medicinal perspective." Read more at the source #DrGPCR #GPCR #IndustryNews