G-protein coupled estrogen receptor 1; chemoattractant receptor-like 2; Flow-induced endothelial G-protein coupled receptor 1; FEG-1; G protein-coupled estrogen receptor 1; G-protein coupled receptor 30; GPCR-Br; IL8-related receptor DRY12; lymphocyte-derived G-protein coupled receptor; LYGPR; membrane estrogen receptor; mER (GPER1, CEPR, CMKRL2, DRY12, GPER, GPR30)

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Function

G-protein coupled estrogen receptor
binds to 17- beta-estradiol (E2) with high affinity, leading to rapid & transient activation of numerous intracellular signaling pathways
stimulates cAMP production, Ca+2 mobilization & c-Src inducing release of heparin-bound EGF & subsequent transactivation of EGFR, activating downstream signaling pathways such as PI3K/Akt & ERK/MAPK
mediates pleiotropic functions among others in the cardiovascular, endocrine, reproductive, immune & central nervous systems
role in cardioprotection by reducing cardiac hypertrophy & perivascular fibrosis in a RAMP3-dependent manner
regulates arterial blood pressure by stimulating vasodilation & reducing vascular smooth muscle & microvascular endothelial cell proliferation
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.
role in acute neuroprotection against NMDA-induced excitotoxic neuronal death
increases firing activity & intracellular Ca+2 oscillations in LHRH neurons
inhibits early osteoblast proliferation at growth plate during skeletal development
inhibits mature adipocyte differentiation & lipid accumulation
involved in the recruitment of beta-arrestin 2 ARRB2 at the plasma membrane in epithelial cells
functions s 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 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 & fibronectin matrix assembly in breast cancer cells
ubiquitinated
ubiquitination occurs at the plasma membrane & leads to proteasome-mediated degradation
glycosylated
homodimer (probable)
heterodimerizes with other G-protein-coupled receptor like CRHR1, HTR1A & PAQR8
interacts (via C-terminus tail motif) with DLG4 (via N-terminus tandem pair of PDZ domains)
- interaction induces the increase of GPER1 protein levels residing at the plasma membrane surface in an estradiol- independent manner
interacts with RAMP3
interacts with KRT7 & KRT8
interacts with EGFR
- interaction increases after agonist-induced stimulation in cancer-associated fibroblasts
interacts with ESR1