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G protein-coupled estrogen receptor 1: a novel target to treat cardiovascular disease in a sex-specific manner?

Authors
  • Dinh, Quynh Nhu1
  • Vinh, Antony1
  • Arumugam, Thiruma V1
  • Drummond, Grant R1
  • Sobey, Christopher G1
  • 1 Department of Physiology, Anatomy and Microbiology and Centre for Cardiovascular Biology and Disease Research, School of Life Sciences, La Trobe University, Bundoora, Victoria, Australia. , (Australia)
Type
Published Article
Journal
British Journal of Pharmacology
Publisher
Wiley (Blackwell Publishing)
Publication Date
Oct 01, 2021
Volume
178
Issue
19
Pages
3849–3863
Identifiers
DOI: 10.1111/bph.15521
PMID: 33948934
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

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. © 2021 The British Pharmacological Society.

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