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Symbol GPER1 contributors: mct/npt/pgu - updated : 10-06-2015
HGNC name G protein-coupled estrogen receptor 1
HGNC id 4485
Location 7p22.3      Physical location : -
Synonym name
  • chemokine receptor-like 2
  • flow-induced endothelial G-protein coupled receptor
  • leucine rich protein in GPR30 3'UTR
  • G protein-coupled receptor 30
  • lymphocyte-derived G-protein coupled receptor
  • IL8-related receptor DRY12
  • sex comb on midleg-like protein 2
  • Synonym symbol(s) CMKRL2, DRY12, FEG-1, GPCR-Br, LERGU, LERGU2, LyGPR, MGC99678, GPR30, CEPR, GPER, LERGU, LERGU2, LyGPR, mER
    TYPE fragile site
    STRUCTURE 7.01 kb     3 Exon(s)
    regulatory sequence Promoter
    text structure
  • IGF1 transactivates the GPER1 promoter sequence and upregulates GPER1 mRNA and protein levels
  • MAPPING cloned Y linked   status provisional
    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
    Type widely
       expressed in (based on citations)
    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   
    SystemTissueTissue level 1Tissue level 2LevelPubmedSpeciesStageRna symbol
    Epithelialbarrier lininguroepithelium highly Homo sapiens
    Epithelialbarrier liningendometrium highly Homo sapiens
    SystemCellPubmedSpeciesStageRna symbol
    Cardiovascularendothelial cell Homo sapiens
    Nervouscholinergic neuron Homo sapiens
    not specificchondrocyte
    cell lineage
    cell lines
    at STAGE
    physiological period puberty, pregnancy
  • most abundant in placenta
  • in normal cyclic endometrium and early pregnancy decidua
  • seven transmembrane segments (7TM) receptor
  • G protein coupled receptor family
  • CATEGORY receptor G
    SUBCELLULAR LOCALIZATION     plasma membrane
    intracellular,cytoplasm,organelle,endoplasmic reticulum
    intracellular,nuclear envelope
  • 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
    a component
    small molecule
  • 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
    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)
    Variant & Polymorphism
    Candidate gene
    Therapy target
    may represent a new target to combat estrogen receptor-positive breast cancer
    under cardiac stress exerts direct protection in the heart and may serve as a potential therapeutic target for cardiac drug therapy
  • Gper deficiency in male mice results in insulin resistance, dyslipidemia, and a proinflammatory state