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GPER: A Novel Target To Treat Cardiovascular Disease In A Sex‐Specific Manner?

journal contribution
posted on 01.06.2021, 01:38 by Quynh Nhu Dinh, Antony VinhAntony Vinh, Thiruma ArumugamThiruma Arumugam, Grant R Drummond, Christopher G Sobey
As an agonist of the classical nuclear receptors, ERα and ERβ, estrogen has been understood to inhibit the development of cardiovascular disease in pre-menopausal 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 post-menopausal women that include increased serious adverse events. Interestingly, pre-clinical studies have shown that selective activation of the novel membrane-associated G protein-coupled estrogen receptor 1, 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 post-menopausal women could provide cardiovascular protection with fewer adverse effects than 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.

History

Publication Date

04/05/2021

Journal

British Journal of Pharmacology

Article Number

bph.15521

Publisher

Wiley

ISSN

0007-1188

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The Author reserves all moral rights over the deposited text and must be credited if any re-use occurs. Documents deposited in OPAL are the Open Access versions of outputs published elsewhere. Changes resulting from the publishing process may therefore not be reflected in this document. The final published version may be obtained via the publisher’s DOI. Please note that additional copyright and access restrictions may apply to the published version.

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