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FLASH GENE
Symbol GPER1 contributors: mct/npt/pgu - updated : 10-06-2015
HGNC name G protein-coupled estrogen receptor 1
HGNC id 4485
RNA
TRANSCRIPTS type messenger
text Variants 2, 3 and 4 encode the same protein
identificationnb exonstypebpproduct
ProteinkDaAAspecific expressionYearPubmed
2 - 2857 54 375 - 1997 9367686
3 - 2981 54 375 - 1997 9367686
2 - 2654 54 375 - 1997 9367686
EXPRESSION
Type widely
   expressed in (based on citations)
organ(s)
SystemOrgan level 1Organ level 2Organ level 3Organ level 4LevelPubmedSpeciesStageRna symbol
Cardiovascularvessel     Homo sapiens
Endocrinethyroid   highly Homo sapiens
Nervousbrainforebrain  highly Homo sapiens
Reproductivefemale systemuterus  highly Homo sapiens
 male systemtestis  highly Homo sapiens
Skeletonappendicular skeletonlower limbs   
tissue
SystemTissueTissue level 1Tissue level 2LevelPubmedSpeciesStageRna symbol
Epithelialbarrier lininguroepithelium highly Homo sapiens
Epithelialbarrier liningendometrium highly Homo sapiens
cells
SystemCellPubmedSpeciesStageRna symbol
Cardiovascularendothelial cell Homo sapiens
Nervouscholinergic neuron Homo sapiens
not specificchondrocyte
cell lineage
cell lines
fluid/secretion
at STAGE
physiological period puberty, pregnancy
Text
  • most abundant in placenta
  • in normal cyclic endometrium and early pregnancy decidua
  • PROTEIN
    PHYSICAL PROPERTIES
    STRUCTURE
    motifs/domains
  • seven transmembrane segments (7TM) receptor
  • HOMOLOGY
    Homologene
    FAMILY
  • G protein coupled receptor family
  • CATEGORY receptor G
    SUBCELLULAR LOCALIZATION     plasma membrane
        intracellular
    intracellular,cytoplasm,organelle,mitochondria
    intracellular,cytoplasm,organelle,membrane
    intracellular,cytoplasm,organelle,endoplasmic reticulum
    intracellular,cytoplasm,organelle,Golgi
    intracellular,cytoplasm,organelle,endosome
    intracellular,cytoplasm,cytosolic
    intracellular,nucleus
    intracellular,nuclear envelope
    text
  • expressed in the growth plate in infancy and the level of expression declines during pubertal progression (localized to the resting and hypertrophic zones, being absent from the proliferative zone)
  • localized both intracellularly and in the plasma membrane and subject to limited basal endocytosis
  • basic FUNCTION
  • intracellular transmembrane estrogen receptor that may contribute to normal estrogen physiology as well as pathophysiology
  • mediates the nongenomic signaling of 17beta-estradiol (E2) in a variety of estrogen-sensitive cancer cells through activation of the epidermal growth factor receptor (EGFR) pathway
  • playing a potential role as a modulator of pubertal growth, and could be involved in the modulation of longitudinal bone growth during puberty
  • playing an important role for the inhibitory effect of progestin on cellular growth
  • G protein-coupled receptor for estrogen that responds to estrogen with rapid cellular signaling
  • indispensable for thymocyte apoptosis that preferentially occurs in T cell receptor beta chain(-/low) double-positive thymocytes
  • responds to estrogen and tamoxifen stimulation with rapid cellular signaling including ERK activation, PI3K activation, calcium mobilization and cAMP production
  • GPR30-mediated inhibition of urothelial cell proliferation is the result of decreased CCND1 by down-regulation of activation protein-1 signaling
  • mediate some of the rapid signal transduction events following cell stimulation, such as calcium mobilization and kinase activation, and it also appears to regulate rapid transcriptional activation of genes such as c-fos
  • antagonizes growth of ESR1-positive breast cancer
  • implicated in rapid non-genomic effects of estrogens
  • may have potential functions during sperm migration at midcycle as well as decidualization and blastocyst implantation in the mid-secretory phase
  • role in estrogen protection against ischaemic stress
  • activation of GPER1 enhances cholinergic function in the hippocampus similar to E2
  • ESR1, ESR2 and GPER1 are involved in preventing beta-cell apoptosis, impeding the loss of critical beta-cell mass
  • endogenous GPER1 inhibits EDN1-induced vasoconstriction, an effect that may be associated with reduced VSMC Ca(2+) sensitivity)
  • regulates endothelin-dependent vascular tone and intracellular calcium
  • normal endometrial GPER1 expression is cyclic and regulated by nuclear estrogen and progesterone receptors, while expression is dysregulated in endometriosis
  • IGF1 system regulates GPER1 expression and function, triggering the activation of a signaling network that leads to the migration and proliferation of cancer cells
  • endothelial GPER1 is a novel regulator of the inflammatory response which could be a potential therapeutic target against atherosclerosis and other inflammatory diseases
  • important role in mediating the rapid signaling and neuroprotective actions of E2 in the hippocampus
  • is crucial in modulating glomerular mesangial cell function including extracellular matrix production and migration
  • GPER1 forms a plasma membrane complex with a membrane-associated guanylate kinase and AKAP5
  • may be included among the complex network of transduction signaling triggered by insulin that drives cells toward cancer progression
  • is the estrogen receptor that mediates the anorectic effect of estrogen through the STAT3 pathway in the hypothalamus
  • plays an important role in mediating the effects of estradiol
  • CELLULAR PROCESS
    PHYSIOLOGICAL PROCESS
    PATHWAY
    metabolism
    signaling
    a component
    INTERACTION
    DNA
    RNA
    small molecule
    protein
  • progestin target gene whose expression correlates with progestin-induced growth inhibition in breast cancer cells
  • BSG release in microvesicles can be mediated by stimulation of GPER1 in uterine epithelial cells, suggesting that inappropriate stimulation or expression of this receptor may be significant in uterine pathology
  • GPER1-RAMP3 interaction has functional consequences on the localization of G-protein-coupled receptors (GPCRs) and RAMP3 is required for GPER1-mediated cardioprotection
  • interacted with membrane-associated guanylate kinases, including DLG1 and DLG4, and protein kinase A-anchoring protein (AKAP5) in the plasma membrane in a PDZ-dependent manner
  • SLC9A3R1 is a new binding partner for GPER1 and its overexpression promotes protein stability and activation of GPER1 in ER-positive invasive breast cancer (IBC)
  • MDH2 stimulated by estrogen, was involved in the development of PTEN-regulated endometrial carcinoma through GPER1-related pathway
  • cell & other
    REGULATION
    ASSOCIATED DISORDERS
    corresponding disease(s)
    Other morbid association(s)
    TypeGene ModificationChromosome rearrangementProtein expressionProtein Function
    tumoral   deletion    
    in gastric cancer
    constitutional     --low  
    in Goiter
    tumoral     --over  
    implicated to associate with the malignant progress of invasive breast cancer (IBC)
    Susceptibility
    Variant & Polymorphism
    Candidate gene
    Marker
    Therapy target
    SystemTypeDisorderPubmed
    cancerreproductivebreast
    may represent a new target to combat estrogen receptor-positive breast cancer
    cardiovascularaquired 
    under cardiac stress exerts direct protection in the heart and may serve as a potential therapeutic target for cardiac drug therapy
    ANIMAL & CELL MODELS
  • Gper deficiency in male mice results in insulin resistance, dyslipidemia, and a proinflammatory state