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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 SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.