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G protein‐coupled estrogen receptor 1: a novel target to treat cardiovascular disease in a sex‐specific manner?
Author(s) -
Dinh Quynh Nhu,
Vinh Antony,
Arumugam Thiruma V.,
Drummond Grant R.,
Sobey Christopher G.
Publication year - 2021
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.15521
Subject(s) - gper , estrogen , estrogen receptor , menopause , disease , medicine , selective estrogen receptor modulator , endocrinology , adverse effect , agonist , estrogen receptor beta , receptor , estrogen receptor alpha , bioinformatics , biology , breast cancer , cancer
As an agonist of the classical nuclear receptors, estrogen receptor‐α and ‐β (NR3A1/2), estrogen has been assumed to inhibit the development of cardiovascular disease in premenopausal women. Indeed, reduced levels of estrogen after menopause are believed to contribute to accelerated morbidity and mortality rates in women. However, estrogen replacement therapy has variable effects on cardiovascular risk in postmenopausal women, including increased serious adverse events. Interestingly, preclinical studies have shown that selective activation of the novel membrane‐associated G protein‐coupled estrogen receptor, GPER, can promote cardiovascular protection. These benefits are more evident in ovariectomised than intact females or in males. It is therefore possible that selective targeting of the GPER in postmenopausal women could provide cardiovascular protection with fewer adverse effects that are caused by conventional ‘receptor non‐specific’ estrogen replacement therapy. This review describes new data regarding the merits of targeting GPER to treat cardiovascular disease with a focus on sex differences.