G protein-coupled estrogen receptor in GtoPdb v.2023.1

The G protein-coupled estrogen receptor (GPER, nomenclature as agreed by the NC-IUPHAR Subcommittee on [26]) was identified following observations of estrogen-evoked cyclic AMP signalling in breast cancer cells [2], which mirrored differential expression an orphan 7-transmembrane GPR30 [6]. There are both cell-surface and intracellular GPER [29, 34]. Selective agonist/ antagonists for have been characterized [26]. Antagonists nuclear receptor, such fulvestrant [11], tamoxifen 34] raloxifene [25], well flavonoid 'phytoestrogens' genistein quercetin [18], agonists GPER. Reviews pharmacology published roles (patho)physiological systems throughout body (cardiovascular, metabolic, endocrine, immune, reproductive) also reviewed [26, 27, 20, 17, 9]. GPER-selective agonist G-1 is currently Phase I/II clinical trials (NCT04130516).