G protein-coupled estrogen receptor (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
The G protein-coupled estrogen receptor (GPER, nomenclature as agreed by the NC-IUPHAR Subcommittee on the G protein-coupled estrogen receptor ) was identified following observations of estrogen-evoked cyclic AMP signalling in breast cancer cells , which mirrored the differential expression of an orphan 7-transmembrane receptor GPR30 . There are observations of both cell-surface and intracellular expression of the GPER receptor [27, 32]. Selective agonist/ antagonists for GPER have been characterized . Antagonists of the nuclear estrogen receptor, such as fulvestrant , tamoxifen [27, 32] and raloxifene , as well as the flavonoid 'phytoestrogens' genistein and quercetin , are agonists of GPER. A complete review of GPER pharmacology has been recently published . The roles of GPER in physiological systems throughout the body (cardiovascular, metabolic, endocrine, immune, reproductive) and in cancer have also been reviewed [24, 25, 18, 15, 8].
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License.