| Minireview: G protein-coupled estrogen receptor-1, GPER-1: its mechanism of action and role in female reproductive cancer, renal and vascular physiology. | |
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MedLine Citation:
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PMID: 22495674 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Using cDNA cloning strategies commonly employed for G protein-coupled receptors (GPCR), GPCR-30 (GPR30), was isolated from mammalian cells before knowledge of its cognate ligand. GPR30 is evolutionarily conserved throughout the vertebrates. A broad literature suggests that GPR30 is a Gs-coupled heptahelical transmembrane receptor that promotes specific binding of naturally occurring and man-made estrogens but not cortisol, progesterone, or testosterone. Its "pregenomic" signaling actions are manifested by plasma membrane-associated actions familiar to GPCR, namely, stimulation of adenylyl cyclase and Gβγ-subunit protein-dependent release of membrane-tethered heparan bound epidermal growth factor. These facts regarding its mechanism of action have led to the formal renaming of this receptor to its current functional designate, G protein-coupled estrogen receptor (ER) (GPER)-1. Further insight regarding its biochemical action and physiological functions in vertebrates is derived from receptor knockdown studies and the use of selective agonists/antagonists that discriminate GPER-1 from the nuclear steroid hormone receptors, ERα and ERβ. GPER-1-selective agents have linked GPER-1 to physiological and pathological events regulated by estrogen action, including, but not limited to, the central nervous, immune, renal, reproductive, and cardiovascular systems. Moreover, immunohistochemical studies have shown a positive association between GPER-1 expression and progression of female reproductive cancer, a relationship that is diametrically opposed from ER. Unlike ER knockout mice, GPER-1 knockout mice are fertile and show no overt reproductive anomalies. However, they do exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. Here, we discuss the role of GPER-1 in female reproductive cancers as well as renal and vascular physiology. |
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Authors:
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Edward J Filardo; Peter Thomas |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural; Review Date: 2012-04-11 |
Journal Detail:
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Title: Endocrinology Volume: 153 ISSN: 1945-7170 ISO Abbreviation: Endocrinology Publication Date: 2012 Jul |
Date Detail:
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Created Date: 2012-06-25 Completed Date: 2012-09-20 Revised Date: 2013-04-16 |
Medline Journal Info:
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Nlm Unique ID: 0375040 Medline TA: Endocrinology Country: United States |
Other Details:
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Languages: eng Pagination: 2953-62 Citation Subset: AIM; IM |
Affiliation:
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Department of Medicine, Rhode Island Hospital and Brown University Medical School, 593 Eddy Street, Aldrich Building Room 708, Providence, Rhode Island 02903, USA. edward_filardo@brown.edu |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Biopsy Female Gene Expression Regulation, Neoplastic* Genital Neoplasms, Female / metabolism* Humans Kidney / blood supply*, metabolism* Ligands Mice Models, Biological Models, Genetic Receptor, Epidermal Growth Factor / metabolism Receptors, Estrogen / metabolism* Receptors, G-Protein-Coupled / metabolism* Transcriptional Activation |
| Grant Support | |
ID/Acronym/Agency:
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R01 CA119165/CA/NCI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/GPER protein, human; 0/Ligands; 0/Receptors, Estrogen; 0/Receptors, G-Protein-Coupled; EC 2.7.10.1/Receptor, Epidermal Growth Factor |
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