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• W2137207319 endingPage "2962" @default.
• W2137207319 startingPage "2953" @default.
• W2137207319 abstract "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." @default.
• W2137207319 created "2016-06-24" @default.
• W2137207319 creator A5029049466 @default.
• W2137207319 creator A5071429090 @default.
• W2137207319 date "2012-04-11" @default.
• W2137207319 modified "2023-10-17" @default.
• W2137207319 title "Minireview: G Protein-Coupled Estrogen Receptor-1, GPER-1: Its Mechanism of Action and Role in Female Reproductive Cancer, Renal and Vascular Physiology" @default.
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• W2137207319 doi "https://doi.org/10.1210/en.2012-1061" @default.
• W2137207319 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3380306" @default.
• W2137207319 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22495674" @default.
• W2137207319 hasPublicationYear "2012" @default.
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