G-protein coupled estrogen receptor 1

Details

Name
G-protein coupled estrogen receptor 1
Synonyms
  • 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
  • LYGPR
  • Lymphocyte-derived G-protein coupled receptor
  • Membrane estrogen receptor
  • mER
Gene Name
GPER1
Organism
Humans
Amino acid sequence
>lcl|BSEQ0020690|G-protein coupled estrogen receptor 1
MDVTSQARGVGLEMYPGTAQPAAPNTTSPELNLSHPLLGTALANGTGELSEHQQYVIGLF
LSCLYTIFLFPIGFVGNILILVVNISFREKMTIPDLYFINLAVADLILVADSLIEVFNLH
ERYYDIAVLCTFMSLFLQVNMYSSVFFLTWMSFDRYIALARAMRCSLFRTKHHARLSCGL
IWMASVSATLVPFTAVHLQHTDEACFCFADVREVQWLEVTLGFIVPFAIIGLCYSLIVRV
LVRAHRHRGLRPRRQKALRMILAVVLVFFVCWLPENVFISVHLLQRTQPGAAPCKQSFRH
AHPLTGHIVNLAAFSNSCLNPLIYSFLGETFRDKLRLYIEQKTNLPALNRFCHAALKAVI
PDSTEQSDVRFSSAV
Number of residues
375
Molecular Weight
42247.12
Theoretical pI
8.36
GO Classification
Functions
chromatin binding / drug binding / estrogen receptor activity / G-protein coupled receptor activity / mineralocorticoid receptor activity / steroid binding / steroid hormone binding
Processes
apoptotic chromosome condensation / cell cycle / cellular response to estradiol stimulus / cellular response to glucose stimulus / cellular response to mineralocorticoid stimulus / cellular response to peptide hormone stimulus / cellular response to tumor necrosis factor / cytosolic calcium ion homeostasis / G-protein coupled receptor signaling pathway / inflammatory response / innate immune response / intracellular steroid hormone receptor signaling pathway / mineralocorticoid receptor signaling pathway / negative regulation of cell cycle arrest / negative regulation of cell cycle process / negative regulation of cell proliferation / negative regulation of DNA metabolic process / negative regulation of ERK1 and ERK2 cascade / negative regulation of fat cell differentiation / negative regulation of gene expression / negative regulation of inflammatory response / negative regulation of leukocyte activation / negative regulation of lipid biosynthetic process / negative regulation of protein kinase B signaling / negative regulation of vascular smooth muscle cell proliferation / neuronal action potential / nuclear fragmentation involved in apoptotic nuclear change / positive regulation of adenylate cyclase activity involved in G-protein coupled receptor signaling pathway / positive regulation of apoptotic process / positive regulation of cAMP biosynthetic process / positive regulation of cardiac vascular smooth muscle cell differentiation / positive regulation of cell migration / positive regulation of cell proliferation / positive regulation of cysteine-type endopeptidase activity involved in apoptotic process / positive regulation of cytosolic calcium ion concentration / positive regulation of endothelial cell apoptotic process / positive regulation of epidermal growth factor receptor signaling pathway / positive regulation of ERK1 and ERK2 cascade / positive regulation of establishment of protein localization to plasma membrane / positive regulation of extrinsic apoptotic signaling pathway / positive regulation of G-protein coupled receptor protein signaling pathway / positive regulation of gene expression / positive regulation of inositol trisphosphate biosynthetic process / positive regulation of insulin secretion / positive regulation of MAPK cascade / positive regulation of neurogenesis / positive regulation of neurotransmitter secretion / positive regulation of phosphatidylinositol 3-kinase signaling / positive regulation of protein phosphorylation / positive regulation of release of cytochrome c from mitochondria / positive regulation of release of sequestered calcium ion into cytosol / positive regulation of transcription from RNA polymerase II promoter / positive regulation of uterine smooth muscle contraction / positive regulation of vasodilation / steroid hormone mediated signaling pathway
Components
axon / axon terminus / cell junction / cytoplasm / cytoplasmic vesicle membrane / cytosol / dendrite / dendritic shaft / dendritic spine head / dendritic spine membrane / early endosome / endoplasmic reticulum / endoplasmic reticulum membrane / Golgi apparatus / Golgi membrane / integral component of plasma membrane / intracellular / keratin filament / mitochondrial membrane / neuronal postsynaptic density / nuclear envelope / nucleus / perinuclear region of cytoplasm / plasma membrane / postsynaptic density / presynaptic active zone / presynaptic membrane / recycling endosome / trans-Golgi network
General Function
Steroid hormone binding
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.
Pfam Domain Function
Transmembrane Regions
63-84 97-120 133-153 176-194 221-236 260-280 307-327
Cellular Location
Nucleus
Gene sequence
>lcl|BSEQ0020691|G-protein coupled estrogen receptor 1 (GPER1)
ATGGATGTGACTTCCCAAGCCCGGGGCGTGGGCCTGGAGATGTACCCAGGCACCGCGCAG
CCTGCGGCCCCCAACACCACCTCCCCCGAGCTCAACCTGTCCCACCCGCTCCTGGGCACC
GCCCTGGCCAATGGGACAGGTGAGCTCTCGGAGCACCAGCAGTACGTGATCGGCCTGTTC
CTCTCGTGCCTCTACACCATCTTCCTCTTCCCCATCGGCTTTGTGGGCAACATCCTGATC
CTGGTGGTGAACATCAGCTTCCGCGAGAAGATGACCATCCCCGACCTGTACTTCATCAAC
CTGGCGGTGGCGGACCTCATCCTGGTGGCCGACTCCCTCATTGAGGTGTTCAACCTGCAC
GAGCGGTACTACGACATCGCCGTCCTGTGCACCTTCATGTCGCTCTTCCTGCAGGTCAAC
ATGTACAGCAGCGTCTTCTTCCTCACCTGGATGAGCTTCGACCGCTACATCGCCCTGGCC
AGGGCCATGCGCTGCAGCCTGTTCCGCACCAAGCACCACGCCCGGCTGAGCTGTGGCCTC
ATCTGGATGGCATCCGTGTCAGCCACGCTGGTGCCCTTCACCGCCGTGCACCTGCAGCAC
ACCGACGAGGCCTGCTTCTGTTTCGCGGATGTCCGGGAGGTGCAGTGGCTCGAGGTCACG
CTGGGCTTCATCGTGCCCTTCGCCATCATCGGCCTGTGCTACTCCCTCATTGTCCGGGTG
CTGGTCAGGGCGCACCGGCACCGTGGGCTGCGGCCCCGGCGGCAGAAGGCGCTCCGCATG
ATCCTCGCGGTGGTGCTGGTCTTCTTCGTCTGCTGGCTGCCGGAGAACGTCTTCATCAGC
GTGCACCTCCTGCAGCGGACGCAGCCTGGGGCCGCTCCCTGCAAGCAGTCTTTCCGCCAT
GCCCACCCCCTCACGGGCCACATTGTCAACCTCGCCGCCTTCTCCAACAGCTGCCTAAAC
CCCCTCATCTACAGCTTTCTCGGGGAGACCTTCAGGGACAAGCTGAGGCTGTACATTGAG
CAGAAAACAAATTTGCCGGCCCTGAACCGCTTCTGTCACGCTGCCCTGAAGGCCGTCATT
CCAGACAGCACCGAGCAGTCGGATGTGAGGTTCAGCAGTGCCGTGTAG
Chromosome Location
7
Locus
Not Available
External Identifiers
ResourceLink
UniProtKB IDQ99527
UniProtKB Entry NameGPER1_HUMAN
GenBank Gene IDBC011634
GenAtlas IDGPER
HGNC IDHGNC:4485
General References
  1. Owman C, Blay P, Nilsson C, Lolait SJ: Cloning of human cDNA encoding a novel heptahelix receptor expressed in Burkitt's lymphoma and widely distributed in brain and peripheral tissues. Biochem Biophys Res Commun. 1996 Nov 12;228(2):285-92. [PubMed:8920907]
  2. Feng Y, Gregor P: Cloning of a novel member of the G protein-coupled receptor family related to peptide receptors. Biochem Biophys Res Commun. 1997 Feb 24;231(3):651-4. [PubMed:9070864]
  3. Takada Y, Kato C, Kondo S, Korenaga R, Ando J: Cloning of cDNAs encoding G protein-coupled receptor expressed in human endothelial cells exposed to fluid shear stress. Biochem Biophys Res Commun. 1997 Nov 26;240(3):737-41. [PubMed:9398636]
  4. Kvingedal AM, Smeland EB: A novel putative G-protein-coupled receptor expressed in lung, heart and lymphoid tissue. FEBS Lett. 1997 Apr 21;407(1):59-62. [PubMed:9141481]
  5. Carmeci C, Thompson DA, Ring HZ, Francke U, Weigel RJ: Identification of a gene (GPR30) with homology to the G-protein-coupled receptor superfamily associated with estrogen receptor expression in breast cancer. Genomics. 1997 Nov 1;45(3):607-17. [PubMed:9367686]
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  30. Chakrabarti S, Davidge ST: G-protein coupled receptor 30 (GPR30): a novel regulator of endothelial inflammation. PLoS One. 2012;7(12):e52357. doi: 10.1371/journal.pone.0052357. Epub 2012 Dec 20. [PubMed:23285008]
  31. Van Damme P, Lasa M, Polevoda B, Gazquez C, Elosegui-Artola A, Kim DS, De Juan-Pardo E, Demeyer K, Hole K, Larrea E, Timmerman E, Prieto J, Arnesen T, Sherman F, Gevaert K, Aldabe R: N-terminal acetylome analyses and functional insights of the N-terminal acetyltransferase NatB. Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12449-54. doi: 10.1073/pnas.1210303109. Epub 2012 Jul 18. [PubMed:22814378]
  32. Gros R, Ding Q, Liu B, Chorazyczewski J, Feldman RD: Aldosterone mediates its rapid effects in vascular endothelial cells through GPER activation. Am J Physiol Cell Physiol. 2013 Mar;304(6):C532-40. doi: 10.1152/ajpcell.00203.2012. Epub 2013 Jan 2. [PubMed:23283935]
  33. Lenhart PM, Broselid S, Barrick CJ, Leeb-Lundberg LM, Caron KM: G-protein-coupled receptor 30 interacts with receptor activity-modifying protein 3 and confers sex-dependent cardioprotection. J Mol Endocrinol. 2013 Jul 3;51(1):191-202. doi: 10.1530/JME-13-0021. Print 2013. [PubMed:23674134]
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Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB05939MK-0354investigationalunknownDetails
DB00783Estradiolapproved, investigational, vet_approvedunknownDetails
DB01645GenisteininvestigationalunknownDetails
DB13952Estradiol acetateapproved, investigational, vet_approvedunknownDetails
DB13953Estradiol benzoateapproved, investigational, vet_approvedunknownDetails
DB13954Estradiol cypionateapproved, investigational, vet_approvedunknownDetails
DB13955Estradiol dienanthateapproved, investigational, vet_approvedunknownDetails
DB13956Estradiol valerateapproved, investigational, vet_approvedunknownDetails