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PMID: 21844907 Published · epublish English Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't Review

The G-protein-coupled estrogen receptor GPER in health and disease.

Nature reviews. Endocrinology ·Vol. 7 ·No. 12 ·2011-08-16 ·Pages 715-26

Prossnitz ER, Barton M

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.

MeSH Terms
Animals Benzhydryl Compounds Cardiovascular System Endocrine System Estradiol/physiology Female Genistein Humans Immune System Male Neoplasms Nervous System Phenols Premenopause Receptors, Estrogen/physiology Receptors, G-Protein-Coupled/physiology Signal Transduction
Chemicals
Benzhydryl Compounds Phenols Receptors, Estrogen Receptors, G-Protein-Coupled Estradiol Genistein bisphenol A
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Prossnitz Eric R
Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA. [email protected]
Barton Matthias
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Article Info
Journal
Nature reviews. Endocrinology
Abbr.
Nat Rev Endocrinol
ISSN
1759-5037
DOI
10.1038/nrendo.2011.122
Email
[email protected]
Published
2011-08-16
Epub
2011-00-16
Pages
715-26
Language
English
Region
England
NLM ID
101500078
PMCID
PMC3474542
Subset
IM
Grants
NCI NIH HHS · CA118743 · United States
NCI NIH HHS · R01 CA118743 · United States
NCI NIH HHS · R01 CA127731 · United States
NCI NIH HHS · CA116662 · United States
NCI NIH HHS · R01 CA116662 · United States
NCI NIH HHS · CA127731 · United States
External Links
PubMed source DOI: 10.1038/nrendo.2011.122 PMC Full Text View journal details
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