Aliases for GPER1 Gene
- G Protein-Coupled Estrogen Receptor 1 2 3 4
- CMKRL2 3 4 6
- GPR30 3 4 6
- GPER 3 4 6
- Flow-Induced Endothelial G-Protein Coupled Receptor 1 3 4
- Lymphocyte-Derived G-Protein Coupled Receptor 3 4
- Chemoattractant Receptor-Like 2 3 4
- G Protein-Coupled Receptor 30 2 3
- Membrane Estrogen Receptor 3 4
- IL8-Related Receptor DRY12 3 4
- GPCR-Br 3 4
- LyGPR 3 4
- DRY12 3 4
External Ids for GPER1 Gene
Previous Symbols for GPER1 Gene
This gene is a member of the G-protein coupled receptor 1 family and encodes a multi-pass membrane protein that localizes to the endoplasmic reticulum. The protein binds estrogen, resulting in 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. Alternate transcriptional splice variants which encode the same protein have been characterized. [provided by RefSeq, Jul 2008]
GeneCards Summary for GPER1 Gene
GPER1 (G Protein-Coupled Estrogen Receptor 1) is a Protein Coding gene. Diseases associated with GPER1 include breast cancer and pain disorder. Among its related pathways are Signaling by GPCR and Signaling by GPCR. GO annotations related to this gene include G-protein coupled receptor activity and steroid binding. An important paralog of this gene is GPR146.
UniProtKB/Swiss-Prot for GPER1 Gene
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.
The GPR30 receptor is an orphan G-protein-coupled receptor that has recently been shown to bind estrogen and cause estrogen-mediated adenylyl cyclase stimulation. GPR30 is widely distributed in neural, breast cancer, placental, heart, ovarian, prostate, hepatic, vascular epithelial and lymphoid tissue. The receptor acts independently of ERalpha and ERbeta and triggers ER-dependent EGFR action.