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G-protein coupled estrogen receptor 1

Definition:

G-protein coupled estrogen receptor that binds to 17-beta-estradiol (E2) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways. Stimulates cAMP production, calcium mobilization and tyrosine kinase Src inducing the release of heparin-bound epidermal growth factor (HB-EGF) and subsequent transactivation of the epidermal growth factor receptor (EGFR), activating downstream signaling pathways such as PI3K/Akt and ERK/MAPK. Mediates pleiotropic functions among others in the cardiovascular, endocrine, reproductive, immune and central nervous systems. Has a role in cardioprotection by reducing cardiac hypertrophy and perivascular fibrosis in a RAMP3-dependent manner. Regulates arterial blood pressure by stimulating vasodilation and reducing vascular smooth muscle and microvascular endothelial cell proliferation. Plays a role in blood glucose homeostasis contributing to the insulin secretion response by pancreatic beta cells. Triggers mitochondrial apoptosis during pachytene spermatocyte differentiation. Stimulates uterine epithelial cell proliferation. Enhances uterine contractility in response to oxytocin. Contributes to thymic atrophy by inducing apoptosis. Attenuates TNF-mediated endothelial expression of leukocyte adhesion molecules. Promotes neuritogenesis in developing hippocampal neurons. Plays a role in acute neuroprotection against NMDA-induced excitotoxic neuronal death. Increases firing activity and intracellular calcium oscillations in luteinizing hormone-releasing hormone (LHRH) neurons. Inhibits early osteoblast proliferation at growth plate during skeletal development. Inhibits mature adipocyte differentiation and lipid accumulation. Involved in the recruitment of beta-arrestin 2 ARRB2 at the plasma membrane in epithelial cells. Functions also as a receptor for aldosterone mediating rapid regulation of vascular contractibility through the PI3K/ERK signaling pathway. Involved in cancer progression regulation. Stimulates cancer-associated fibroblast (CAF) proliferation by a rapid genomic response through the EGFR/ERK transduction pathway. Associated with EGFR, may act as a transcription factor activating growth regulatory genes (c-fos, cyclin D1). Promotes integrin alpha-5/beta-1 and fibronectin (FN) matrix assembly in breast cancer cells.

References:

[1]. E J Filardo, et al. Estrogen-induced activation of Erk-1 and Erk-2 requires the G protein-coupled receptor homolog, GPR30, and occurs via trans-activation of the epidermal growth factor receptor through release of HB-EGF. Mol Endocrinol. 2000 Oct;14(10):1649-60. [Content Brief]

[2]. Subhadeep Chakrabarti, et al. G-protein coupled receptor 30 (GPR30): a novel regulator of endothelial inflammation. PLoS One. 2012;7(12):e52357. [Content Brief]

[3]. Chetana M Revankar, et al. A transmembrane intracellular estrogen receptor mediates rapid cell signaling. Science. 2005 Mar 11;307(5715):1625-30. [Content Brief]

[4]. Elvira Haas, et al. Regulatory role of G protein-coupled estrogen receptor for vascular function and obesity. Circ Res. 2009 Feb 13;104(3):288-91. [Content Brief]

[5]. P Thomas, et al. Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology. 2005 Feb;146(2):624-32. [Content Brief]

[6]. K Maiti, et al. G-1-activated membrane estrogen receptors mediate increased contractility of the human myometrium. Endocrinology. 2011 Jun;152(6):2448-55. [Content Brief]

[7]. Robert Gros, et al. Aldosterone mediates its rapid effects in vascular endothelial cells through GPER activation. Am J Physiol Cell Physiol. 2013 Mar;304(6):C532-40. [Content Brief]

[8]. Robert Gros, et al. GPR30 expression is required for the mineralocorticoid receptor-independent rapid vascular effects of aldosterone. Hypertension. 2011 Mar;57(3):442-51. [Content Brief]

[9]. Patricia M Lenhart, et al. G-protein-coupled receptor 30 interacts with receptor activity-modifying protein 3 and confers sex-dependent cardioprotection. J Mol Endocrinol. 2013 Jul 3;51(1):191-202. [Content Brief]

[10]. Antonio Madeo, et al. Nuclear alternate estrogen receptor GPR30 mediates 17beta-estradiol-induced gene expression and migration in breast cancer-associated fibroblasts. Cancer Res. 2010 Jul 15;70(14):6036-46. [Content Brief]

[11]. Jeffrey A Quinn, et al. Coordinate regulation of estrogen-mediated fibronectin matrix assembly and epidermal growth factor receptor transactivation by the G protein-coupled receptor, GPR30. Mol Endocrinol. 2009 Jul;23(7):1052-64. [Content Brief]

[12]. Caroline Sandén, et al. G protein-coupled estrogen receptor 1/G protein-coupled receptor 30 localizes in the plasma membrane and traffics intracellularly on cytokeratin intermediate filaments. Mol Pharmacol. 2011 Mar;79(3):400-10. [Content Brief]

[13]. Maria Francesca Santolla, et al. G protein-coupled estrogen receptor mediates the up-regulation of fatty acid synthase induced by 17β-estradiol in cancer cells and cancer-associated fibroblasts. J Biol Chem. 2012 Dec 21;287(52):43234-45. [Content Brief]

[14]. Q K Y Chan, et al. Activation of GPR30 inhibits the growth of prostate cancer cells through sustained activation of Erk1/2, c-jun/c-fos-dependent upregulation of p21, and induction of G(2) cell-cycle arrest. Cell Death Differ. 2010 Sep;17(9):1511-23. [Content Brief]

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