GPER1: Polycystic Ovarian Syndrome Database

Gene Information

Gene Symbol

GPER1

Aliases

CEPR, CMKRL2, DRY12, FEG-1, GPCR-Br, GPER, GPR30, LERGU, LERGU2, LyGPR, mER

Entrez Gene ID

2852

Gene Name

G protein-coupled estrogen receptor 1

Chromosomal Location

7p22.3

HGNC ID

HGNC:4485

Summary

This gene encodes a multi-pass membrane protein that localizes to the endoplasmic reticulum and a member of the G-protein coupled receptor 1 family. This receptor binds estrogen and activates multiple downstream signaling pathways, leading to stimulation of adenylate cyclase and an increase in cyclic AMP levels, while also promoting intracellular calcium mobilization and synthesis of phosphatidylinositol 3,4,5-trisphosphate in the nucleus. This protein therefore plays a role in the rapid nongenomic signaling events widely observed following stimulation of cells and tissues with estrogen. This receptor has been shown to play a role in diverse biological processes, including bone and nervous system development, metabolism, cognition, male fertility and uterine function. [provided by RefSeq, Aug 2017]

e!Ensembl

Gene	ENSG00000164850
Transcript	ENST00000401670, ENST00000413368, ENST00000297469, ENST00000397088, ENST00000397092, ENST00000619052, ENST00000617001
Protein	ENSP00000385151, ENSP00000410487, ENSP00000297469, ENSP00000380277, ENSP00000380281, ENSP00000483756, ENSP00000479553

Gene Ontology (GO)

Show/Hide all(50 )

GO ID	Ontology	Function	Evidence	Reference
GO:0001934	Biological process	Positive regulation of protein phosphorylation	IDA	20551055, 21427217
GO:0002695	Biological process	Negative regulation of leukocyte activation	IDA	23285008
GO:0007186	Biological process	G protein-coupled receptor signaling pathway	IMP	23840305
GO:0007189	Biological process	Adenylate cyclase-activating G protein-coupled receptor signaling pathway	IDA	15539556
GO:0008284	Biological process	Positive regulation of cell proliferation	IMP	20551055
GO:0010628	Biological process	Positive regulation of gene expression	IMP	23840305
GO:0010629	Biological process	Negative regulation of gene expression	IMP	23840305
GO:0010948	Biological process	Negative regulation of cell cycle process	IMP	23840305
GO:0014068	Biological process	Positive regulation of phosphatidylinositol 3-kinase signaling	IDA	15705806
GO:0030335	Biological process	Positive regulation of cell migration	IMP	20551055
GO:0030518	Biological process	Intracellular steroid hormone receptor signaling pathway	IBA	21873635
GO:0030518	Biological process	Intracellular steroid hormone receptor signaling pathway	IDA	15705806
GO:0032962	Biological process	Positive regulation of inositol trisphosphate biosynthetic process	IDA	15705806
GO:0043401	Biological process	Steroid hormone mediated signaling pathway	IDA	19931550
GO:0045742	Biological process	Positive regulation of epidermal growth factor receptor signaling pathway	IDA	15705806
GO:0045745	Biological process	Positive regulation of G protein-coupled receptor signaling pathway	IDA	15539556
GO:0045944	Biological process	Positive regulation of transcription by RNA polymerase II	IDA	20551055
GO:0050728	Biological process	Negative regulation of inflammatory response	IDA	23285008
GO:0051281	Biological process	Positive regulation of release of sequestered calcium ion into cytosol	IDA	15705806
GO:0051898	Biological process	Negative regulation of protein kinase B signaling	IMP	23840305
GO:0070373	Biological process	Negative regulation of ERK1 and ERK2 cascade	IMP	23840305
GO:0070374	Biological process	Positive regulation of ERK1 and ERK2 cascade	IDA	20551055, 21427217
GO:0070474	Biological process	Positive regulation of uterine smooth muscle contraction	IDA	21427217
GO:0071356	Biological process	Cellular response to tumor necrosis factor	IDA	23285008
GO:0071375	Biological process	Cellular response to peptide hormone stimulus	IDA	21427217
GO:0071392	Biological process	Cellular response to estradiol stimulus	IBA	21873635
GO:0071392	Biological process	Cellular response to estradiol stimulus	IDA	15539556, 15705806, 19931550, 20551055, 21149639, 21427217, 21540189, 23285008
GO:1903078	Biological process	Positive regulation of protein localization to plasma membrane	IDA	23674134
GO:1904706	Biological process	Negative regulation of vascular smooth muscle cell proliferation	IMP	23840305
GO:2000724	Biological process	Positive regulation of cardiac vascular smooth muscle cell differentiation	IMP	23840305
GO:0005634	Cellular component	Nucleus	IDA	20551055, 23285008
GO:0005635	Cellular component	Nuclear envelope	IDA	15705806
GO:0005769	Cellular component	Early endosome	IDA	21540189
GO:0005783	Cellular component	Endoplasmic reticulum	IDA	15705806, 21540189
GO:0005794	Cellular component	Golgi apparatus	IBA	21873635
GO:0005794	Cellular component	Golgi apparatus	IDA	15705806
GO:0005802	Cellular component	Trans-Golgi network	IDA	21540189
GO:0005886	Cellular component	Plasma membrane	IDA	15539556, 19931550, 21149639, 21427217, 21540189, 23674134
GO:0005886	Cellular component	Plasma membrane	IDA	15705806
GO:0005887	Cellular component	Integral component of plasma membrane	TAS	8920907
GO:0030659	Cellular component	Cytoplasmic vesicle membrane	IDA	21540189
GO:0045095	Cellular component	Keratin filament	IDA	21149639
GO:0048471	Cellular component	Perinuclear region of cytoplasm	IDA	21540189
GO:0055037	Cellular component	Recycling endosome	IDA	21540189
GO:0003682	Molecular function	Chromatin binding	IDA	20551055
GO:0005496	Molecular function	Steroid binding	IDA	15539556, 15705806
GO:0005515	Molecular function	Protein binding	IPI	20551055, 21149639, 23674134
GO:0030284	Molecular function	Estrogen receptor activity	IBA	21873635
GO:0030284	Molecular function	Estrogen receptor activity	IDA	15539556, 15705806
GO:1990239	Molecular function	Steroid hormone binding	IDA	19931550

Protein Information

Protein Name

G-protein coupled estrogen receptor 1, G protein-coupled receptor 30, IL8-related receptor DRY12, chemoattractant receptor-like 2, chemokine receptor-like 2, constitutively expressed peptide-like receptor, flow-induced endothelial G-protein coupled receptor 1, heptahelix receptor, lymphocyte-derived G-protein coupled receptor, membrane estrogen receptor

Function

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.

UniProt

Q99527

GPER1

Expression of GPR30, ERalpha and ERbeta in endometrium during window of implantation in patients with polycystic ovary syndrome: a pilot study.