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G protein-coupled estrogen receptor C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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The G protein-coupled estrogen receptor (GPER, nomenclature as agreed by the NC-IUPHAR Subcommittee on the G protein-coupled estrogen receptor [12]) was identified following observations of estrogen-evoked cyclic AMP signalling in breast cancer cells [1], which mirrored the differential expression of an orphan 7-transmembrane receptor GPR30 [3]. There are observations of both cell-surface and intracellular expression of the GPER receptor [14-15]. Selective agonist/ antagonists for GPER have been characterized [12]. Antagonists of the nuclear estrogen receptor, such as fulvestrant [7], tamoxifen [14-15] and raloxifene [11], as well as the flavonoid 'phytoestrogens' genistein and quercetin [9], are agonists of GPER. Reviews of GPER pharmacology have been published [12]. The roles of GPER in (patho)physiological systems throughout the body (cardiovascular, metabolic, endocrine, immune, reproductive) and in cancer have also been reviewed [6,8,10,12-13]. The GPER-selective agonist G-1 is currently in Phase I/II clinical trials for cancer (NCT04130516).

Receptors

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Targets of relevance to immunopharmacology are highlighted in blue

GPER C Show summary » More detailed page go icon to follow link

Further reading

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. Br J Pharmacol. 176 Suppl 1:S27-S156.