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HERO ID
2735080
Reference Type
Journal Article
Subtype
Review
Title
The G-protein-coupled estrogen receptor GPER in health and disease
Author(s)
Prossnitz, ER; Barton, M
Year
2011
Is Peer Reviewed?
1
Journal
Nature Reviews. Endocrinology
ISSN:
1759-5029
EISSN:
1759-5037
Volume
7
Issue
12
Page Numbers
715-726
Language
English
PMID
21844907
DOI
10.1038/nrendo.2011.122
Web of Science Id
WOS:000297685100006
Abstract
Estrogens mediate profound effects throughout the body and regulate physiological and pathological processes in both women and men. The low prevalence of many diseases in premenopausal women is attributed to the presence of 17β-estradiol, the predominant and most potent endogenous estrogen. In addition to endogenous estrogens, several man-made and plant-derived molecules, such as bisphenol A and genistein, also exhibit estrogenic activity. Traditionally, the actions of 17β-estradiol are ascribed to two nuclear estrogen receptors (ERs), ERα and ERβ, which function as ligand-activated transcription factors. However, 17β-estradiol also mediates rapid signaling events via pathways that involve transmembrane ERs, such as G-protein-coupled ER 1 (GPER; formerly known as GPR30). In the past 10 years, GPER has been implicated in both rapid signaling and transcriptional regulation. With the discovery of GPER-selective ligands that can selectively modulate GPER function in vitro and in preclinical studies and with the use of Gper knockout mice, many more potential roles for GPER are being elucidated. This Review highlights the physiological roles of GPER in the reproductive, nervous, endocrine, immune and cardiovascular systems, as well as its pathological roles in a diverse array of disorders including cancer, for which GPER is emerging as a novel therapeutic target and prognostic indicator.
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