| 词条 | GPR75 |
| 释义 |
FunctionGPR75 is a member of the G protein-coupled receptor family. GPRs are cell surface receptors that activate guanine-nucleotide binding proteins upon the binding of a ligand.[2] GPR75 is currently classified as an orphan GPCR and several studies are underway to identify its ligand. In one study, the chemokine CCL5 (RANTES) has been shown to stimulate calcium mobilization and inositol triphosphate formation in GPR75-transfected cells.[3] Recently, 20-hydroxyeicosatetraenoic acid (20-HETE), a bioactive eicosanoid formed by ω-hydroxylation of arachidonic acid has been shown to mediate its prohypertensive effects on the vasculature through activation of GPR75 (Gq) signalling.[4] This study by Dr. Schwartzman's laboratory at New York Medical college, one of the pioneers in study of 20-HETE biology, has opened new insights into the field of GPR75 pharmacology. References1. ^{{cite journal | vauthors = Tarttelin EE, Kirschner LS, Bellingham J, Baffi J, Taymans SE, Gregory-Evans K, Csaky K, Stratakis CA, Gregory-Evans CY | title = Cloning and characterization of a novel orphan G-protein-coupled receptor localized to human chromosome 2p16 | journal = Biochemical and Biophysical Research Communications | volume = 260 | issue = 1 | pages = 174–80 | date = June 1999 | pmid = 10381362 | pmc = | doi = 10.1006/bbrc.1999.0753 }} {{G protein-coupled receptors}}{{transmembranereceptor-stub}}2. ^1 {{cite web | title = Entrez Gene: GPR75 G protein-coupled receptor 75 | url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=10936}} 3. ^{{cite journal | vauthors = Ignatov A, Robert J, Gregory-Evans C, Schaller HC | title = RANTES stimulates Ca2+ mobilization and inositol trisphosphate (IP3) formation in cells transfected with G protein-coupled receptor 75 | journal = British Journal of Pharmacology | volume = 149 | issue = 5 | pages = 490–7 | date = November 2006 | pmid = 17001303 | pmc = 2014681 | doi = 10.1038/sj.bjp.0706909 }} 4. ^{{cite journal | vauthors = Garcia V, Gilani A, Shkolnik B, Pandey V, Zhang FF, Dakarapu R, Gandham SK, Reddy NR, Graves JP, Gruzdev A, Zeldin DC, Capdevila JH, Falck JR, Schwartzman ML | title = 20-HETE Signals Through G-Protein-Coupled Receptor GPR75 (Gq) to Affect Vascular Function and Trigger Hypertension | journal = Circulation Research | volume = 120 | issue = 11 | pages = 1776–1788 | date = May 2017 | pmid = 28325781 | pmc = 5446268 | doi = 10.1161/CIRCRESAHA.116.310525 }} 1 : G protein-coupled receptors |
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