Identification
HMDB Protein ID CDBP05654
Secondary Accession Numbers Not Available
Name G-protein coupled estrogen receptor 1
Description Not Available
Synonyms Not Available
Gene Name GPER1
Protein Type Receptor
Biological Properties
General Function steroid hormone receptor activity
Specific 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.
GO Classification
Biological Process
positive regulation of epidermal growth factor receptor signaling pathway
cellular response to estradiol stimulus
negative regulation of lipid biosynthetic process
cell cycle
positive regulation of G-protein coupled receptor protein signaling pathway
positive regulation of protein phosphorylation
negative regulation of vascular smooth muscle cell proliferation
elevation of cytosolic calcium ion concentration
positive regulation of cysteine-type endopeptidase activity involved in apoptotic process
neuronal action potential
positive regulation of apoptotic process
positive regulation of cell migration
positive regulation of release of sequestered calcium ion into cytosol
positive regulation of ERK1 and ERK2 cascade
nuclear fragmentation involved in apoptotic nuclear change
positive regulation of cell proliferation
innate immune response
positive regulation of blood vessel diameter
positive regulation of cardiac vascular smooth muscle cell differentiation
positive regulation of neurogenesis
cytosolic calcium ion homeostasis
positive regulation of extrinsic apoptotic signaling pathway
cellular response to peptide hormone stimulus
positive regulation of transcription from RNA polymerase II promoter
positive regulation of inositol trisphosphate biosynthetic process
negative regulation of inflammatory response
positive regulation of endothelial cell apoptotic process
positive regulation of MAPK cascade
negative regulation of fat cell differentiation
intracellular steroid hormone receptor signaling pathway
positive regulation of neurotransmitter secretion
negative regulation of protein kinase B signaling cascade
negative regulation of cell proliferation
positive regulation of protein localization to plasma membrane
positive regulation of release of cytochrome c from mitochondria
negative regulation of ERK1 and ERK2 cascade
positive regulation of uterine smooth muscle contraction
G-protein coupled receptor signaling pathway
apoptotic chromosome condensation
positive regulation of gene expression
steroid hormone mediated signaling pathway
inflammatory response
cellular response to mineralocorticoid stimulus
positive regulation of phosphatidylinositol 3-kinase cascade
cellular response to tumor necrosis factor
negative regulation of cell cycle process
negative regulation of cell cycle arrest
cellular response to glucose stimulus
negative regulation of DNA metabolic process
negative regulation of gene expression
adenylate cyclase-activating G-protein coupled receptor signaling pathway
positive regulation of insulin secretion
negative regulation of leukocyte activation
Cellular Component
cell
trans-Golgi network
presynaptic active zone
endoplasmic reticulum membrane
axon
mitochondrial membrane
postsynaptic density
cytoplasm
recycling endosome
dendritic shaft
endoplasmic reticulum
dendritic spine head
Golgi membrane
plasma membrane
dendritic spine membrane
integral to plasma membrane
dendrite
hippocampal mossy fiber to CA3 synapse
Golgi apparatus
keratin filament
perinuclear region of cytoplasm
presynaptic membrane
nucleus
cytoplasmic vesicle membrane
early endosome
axon terminus
nuclear envelope
Molecular Function
G protein-coupled receptor activity
steroid hormone receptor activity
estrogen receptor activity
steroid hormone binding
chromatin binding
steroid binding
Cellular Location
  1. Cell membrane
  2. Nucleus
  3. Cytoplasm
  4. perinuclear region
  5. Golgi apparatus membrane
  6. Endoplasmic reticulum membrane
  7. Mitochondrion membrane
  8. Golgi apparatus
  9. Basolateral cell membrane
  10. cytoskeleton
  11. Cell junction
  12. synapse
  13. Cell projection
  14. Early endosome
  15. Cytoplasmic vesicle membrane
  16. postsynaptic density
  17. dendrite
  18. axon
  19. trans-Golgi network
  20. Recycling endosome
  21. Dendritic spine membrane
Pathways
Gene Properties
Chromosome Location 7
Locus 7p22.3
SNPs Not Available
Gene Sequence Not Available
Protein Properties
Number of Residues 375
Molecular Weight 42247.12
Theoretical pI Not Available
Pfam Domain Function
Signals Not Available
Transmembrane Regions
  • ["63-84", "97-120", "133-153", "176-194", "221-236", "260-280", "307-327"]
Protein Sequence
>G-protein coupled estrogen receptor 1
MDVTSQARGVGLEMYPGTAQPAAPNTTSPELNLSHPLLGTALANGTGELSEHQQYVIGLF
LSCLYTIFLFPIGFVGNILILVVNISFREKMTIPDLYFINLAVADLILVADSLIEVFNLH
ERYYDIAVLCTFMSLFLQVNMYSSVFFLTWMSFDRYIALARAMRCSLFRTKHHARLSCGL
IWMASVSATLVPFTAVHLQHTDEACFCFADVREVQWLEVTLGFIVPFAIIGLCYSLIVRV
LVRAHRHRGLRPRRQKALRMILAVVLVFFVCWLPENVFISVHLLQRTQPGAAPCKQSFRH
AHPLTGHIVNLAAFSNSCLNPLIYSFLGETFRDKLRLYIEQKTNLPALNRFCHAALKAVI
PDSTEQSDVRFSSAV
GenBank ID Protein Not Available
UniProtKB/Swiss-Prot ID Q99527
UniProtKB/Swiss-Prot Entry Name GPER1_HUMAN
PDB IDs Not Available
GenBank Gene ID Not Available
GeneCard ID Not Available
GenAtlas ID Not Available
HGNC ID HGNC:4485
References
General References Not Available