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Journal of Endocrinology (2010) 204, 105-114       DOI: 10.1677/JOE-09-0242
© 2010 Society for Endocrinology
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REVIEW

The unfolding stories of GPR30, a new membrane-bound estrogen receptor

Marcello Maggiolini and Didier Picard1

Department of Pharmaco-Biology, University of Calabria, 87030 Rende, Italy
1 Département de Biologie Cellulaire, Université de Genève, Sciences III, 30, quai Ernest-Ansermet, CH - 1211 Genève 4, Switzerland

(Correspondence should be addressed to M Maggiolini; Email: marcellomaggiolini{at}yahoo.it; D Picard; Email: didier.picard{at}unige.ch)

Steroid hormones such as estrogens are known to signal through ligand-regulated transcription factors of the nuclear receptor superfamily. In addition, they elicit rapid nongenomic responses from membrane-associated receptors. One of these receptors belongs to an entirely different family of proteins. The G protein-coupled and seven-transmembrane receptor, GPR30, is now widely recognized as an estrogen receptor (ER), hence its official new acronym GPER. It appears to mediate a wide range of responses to estrogen in a large variety of cell types. Its functions are clearly distinct from those of the classical nuclear ERs, although these pathways may overlap and interact in some cases. Here, we review the history of the discovery of this new ER, the evidence for the claim that it is an ER, its signal transduction, and its potential functions in physiology and disease.




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Mol. Endocrinol.Home page
Y. Li, L. Birnbaumer, and C. T. Teng
Regulation of ERR{alpha} Gene Expression by Estrogen Receptor Agonists and Antagonists in SKBR3 Breast Cancer Cells: Differential Molecular Mechanisms Mediated by G Protein-Coupled Receptor GPR30/GPER-1
Mol. Endocrinol., May 1, 2010; 24(5): 969 - 980.
[Abstract] [Full Text] [PDF]




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