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NameG-protein coupled estrogen receptor 1
  • CEPR
  • Chemoattractant receptor-like 2
  • CMKRL2
  • DRY12
  • FEG-1
  • Flow-induced endothelial G-protein coupled receptor 1
  • G protein-coupled estrogen receptor 1
  • G-protein coupled receptor 30
  • GPCR-Br
  • GPER
  • GPR30
  • IL8-related receptor DRY12
  • Lymphocyte-derived G-protein coupled receptor
  • Membrane estrogen receptor
  • mER
Gene NameGPER1
Amino acid sequence
>lcl|BSEQ0020690|G-protein coupled estrogen receptor 1
Number of residues375
Molecular Weight42247.12
Theoretical pI8.36
GO Classification
  • estrogen receptor activity
  • drug binding
  • mineralocorticoid receptor activity
  • G-protein coupled receptor activity
  • steroid binding
  • chromatin binding
  • steroid hormone binding
  • positive regulation of phosphatidylinositol 3-kinase signaling
  • cellular response to peptide hormone stimulus
  • innate immune response
  • positive regulation of epidermal growth factor receptor signaling pathway
  • positive regulation of release of sequestered calcium ion into cytosol
  • negative regulation of cell cycle arrest
  • positive regulation of apoptotic process
  • positive regulation of release of cytochrome c from mitochondria
  • positive regulation of adenylate cyclase activity involved in G-protein coupled receptor signaling pathway
  • positive regulation of cytosolic calcium ion concentration
  • mineralocorticoid receptor signaling pathway
  • negative regulation of protein kinase B signaling
  • positive regulation of protein phosphorylation
  • positive regulation of inositol trisphosphate biosynthetic process
  • negative regulation of cell cycle process
  • negative regulation of inflammatory response
  • positive regulation of establishment of protein localization to plasma membrane
  • negative regulation of DNA metabolic process
  • positive regulation of cAMP biosynthetic process
  • positive regulation of extrinsic apoptotic signaling pathway
  • cellular response to tumor necrosis factor
  • positive regulation of insulin secretion
  • negative regulation of leukocyte activation
  • positive regulation of neurogenesis
  • positive regulation of cell migration
  • negative regulation of lipid biosynthetic process
  • positive regulation of G-protein coupled receptor protein signaling pathway
  • negative regulation of cell proliferation
  • positive regulation of vasodilation
  • negative regulation of vascular smooth muscle cell proliferation
  • neuronal action potential
  • intracellular steroid hormone receptor signaling pathway
  • positive regulation of transcription from RNA polymerase II promoter
  • cellular response to estradiol stimulus
  • nuclear fragmentation involved in apoptotic nuclear change
  • positive regulation of ERK1 and ERK2 cascade
  • cellular response to mineralocorticoid stimulus
  • positive regulation of cysteine-type endopeptidase activity involved in apoptotic process
  • positive regulation of cardiac vascular smooth muscle cell differentiation
  • inflammatory response
  • positive regulation of neurotransmitter secretion
  • cell cycle
  • positive regulation of gene expression
  • negative regulation of fat cell differentiation
  • negative regulation of gene expression
  • positive regulation of endothelial cell apoptotic process
  • G-protein coupled receptor signaling pathway
  • cellular response to glucose stimulus
  • steroid hormone mediated signaling pathway
  • cytosolic calcium ion homeostasis
  • positive regulation of uterine smooth muscle contraction
  • positive regulation of MAPK cascade
  • apoptotic chromosome condensation
  • positive regulation of cell proliferation
  • negative regulation of ERK1 and ERK2 cascade
  • perinuclear region of cytoplasm
  • cytoplasmic vesicle membrane
  • dendritic spine head
  • intracellular
  • cytoplasm
  • dendritic shaft
  • axon
  • postsynaptic density
  • nucleus
  • keratin filament
  • integral component of plasma membrane
  • early endosome
  • endoplasmic reticulum
  • recycling endosome
  • plasma membrane
  • neuronal postsynaptic density
  • nuclear envelope
  • endoplasmic reticulum membrane
  • Golgi membrane
  • presynaptic membrane
  • axon terminus
  • trans-Golgi network
  • mitochondrial membrane
  • dendrite
  • dendritic spine membrane
  • cell junction
  • Golgi apparatus
  • presynaptic active zone
  • cytosol
General FunctionSteroid hormone binding
Specific FunctionG-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.
Pfam Domain Function
Transmembrane Regions63-84 97-120 133-153 176-194 221-236 260-280 307-327
GenBank Protein IDNot Available
UniProtKB IDQ99527
UniProtKB Entry NameGPER1_HUMAN
Cellular LocationNucleus
Gene sequence
>lcl|BSEQ0020691|G-protein coupled estrogen receptor 1 (GPER1)
GenBank Gene IDBC011634
GeneCard IDNot Available
Chromosome Location7
LocusNot Available
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