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Aliases for GPER1 Gene

Aliases for GPER1 Gene

  • G Protein-Coupled Estrogen Receptor 1 2 3 4 5
  • 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
  • CMKRL2 3 4
  • LyGPR 3 4
  • GPR30 3 4
  • DRY12 3 4
  • FEG-1 3 4
  • GPER 3 4
  • CEPR 3 4
  • MER 3 4
  • Constitutively Expressed Peptide-Like Receptor 3
  • Leucine Rich Protein In GPR30 3UTR 3
  • G-Protein Coupled Receptor 30 4
  • Chemokine Receptor-Like 2 3
  • Heptahelix Receptor 3
  • LERGU2 3
  • LERGU 3

External Ids for GPER1 Gene

Previous HGNC Symbols for GPER1 Gene

  • CMKRL2
  • GPR30
  • GPER

Summaries for GPER1 Gene

Entrez Gene Summary 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 urethral intrinsic sphincter deficiency. Among its related pathways are Signaling by GPCR and Peptide ligand-binding receptors. 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.

Gene Wiki entry for GPER1 Gene

No data available for Tocris Summary , PharmGKB "VIP" Summary , fRNAdb sequence ontologies and piRNA Summary for GPER1 Gene

Genomics for GPER1 Gene

Genomic Location for GPER1 Gene

Chromosome:
7
Start:
1,082,208 bp from pter
End:
1,093,815 bp from pter
Size:
11,608 bases
Orientation:
Plus strand

Genomic View for GPER1 Gene

Genes around GPER1 on UCSC Golden Path with GeneCards custom track

Cytogenetic band:
GPER1 Gene in genomic location: bands according to Ensembl, locations according to GeneLoc (and/or Entrez Gene and/or Ensembl if different)
Genomic Location for GPER1 Gene
GeneLoc Logo Genomic Neighborhood Exon StructureGene Density

RefSeq DNA sequence for GPER1 Gene

No data available for Regulatory Elements for GPER1 Gene

Proteins for GPER1 Gene

  • Protein details for GPER1 Gene (UniProtKB/Swiss-Prot)

    Protein Symbol:
    Q99527-GPER1_HUMAN
    Recommended name:
    G-protein coupled estrogen receptor 1
    Protein Accession:
    Q99527
    Secondary Accessions:
    • A8K6C5
    • B5BUJ1
    • O00143
    • O43494
    • Q13631
    • Q6FHL1
    • Q96F42
    • Q99981

    Protein attributes for GPER1 Gene

    Size:
    375 amino acids
    Molecular mass:
    42248 Da
    Quaternary structure:
    • Homodimer (Probable). Heterodimer; heterodimerizes with other G-protein-coupled receptor (GPCRs) like CRHR1, HTR1A and PAQR8. Interacts (via C-terminus tail motif) with DLG4 (via N-terminus tandem pair of PDZ domains); the interaction is direct and induces the increase of GPER1 protein levels residing at the plasma membrane surface in a estradiol-independent manner (By similarity). Interacts with RAMP3. Interacts with KRT7 and KRT8. Interacts with EGFR; the interaction increases after agonist-induced stimulation in cancer-associated fibroblasts (CAF). Interacts with EGFR and ESR1.
    Miscellaneous:
    • Does not bind estradiol according to PubMed:18566127 and PubMed:16645038.

neXtProt entry for GPER1 Gene

Proteomics data for GPER1 Gene at MOPED

Post-translational modifications for GPER1 Gene

Antibody Products

No data available for DME Specific Peptides for GPER1 Gene

Domains & Families for GPER1 Gene

Gene Families for GPER1 Gene

Protein Domains for GPER1 Gene

InterPro:
ProtoNet:

Suggested Antigen Peptide Sequences for GPER1 Gene

Graphical View of Domain Structure for InterPro Entry

Q99527

UniProtKB/Swiss-Prot:

GPER1_HUMAN :
  • Belongs to the G-protein coupled receptor 1 family.
Family:
  • Belongs to the G-protein coupled receptor 1 family.
genes like me logo Genes that share domains with GPER1: view

Function for GPER1 Gene

Molecular function for GPER1 Gene

UniProtKB/Swiss-Prot BiophysicochemicalProperties:
Kinetic parameters: Note=Binds 17-beta-estradiol (E2) in plasma membranes with high affinity (Kd is 3.3 nM) and displays rapid kinetics of association and dissociation. {ECO:0000269 PubMed:15539556, ECO:0000269 PubMed:15705806, ECO:0000269 PubMed:19931550};
UniProtKB/Swiss-Prot 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.
UniProtKB/Swiss-Prot Induction:
Up-regulated by EGF and TGF-alpha in endometrial, ovarian and breast tumor cells. Up-regulated by progestin and by phorbol 12-myristate 13-acetate (PMA) in breast cancer cell lines.
genes like me logo Genes that share phenotypes with GPER1: view

Animal Models for GPER1 Gene

MGI Knock Outs for GPER1:

Animal Model Products

  • Taconic Biosciences Mouse Models for GPER1

miRNA for GPER1 Gene

miRTarBase miRNAs that target GPER1

No data available for Enzyme Numbers (IUBMB) , Gene Ontology (GO) - Molecular Function , Human Phenotype Ontology , Transcription Factor Targets and HOMER Transcription for GPER1 Gene

Localization for GPER1 Gene

Subcellular locations from UniProtKB/Swiss-Prot for GPER1 Gene

Nucleus. Cytoplasm. Cytoplasm, perinuclear region. Cytoplasm, cytoskeleton. Cell membrane; Multi-pass membrane protein. Basolateral cell membrane; Multi-pass membrane protein. Cytoplasmic vesicle membrane; Multi-pass membrane protein. Early endosome. Recycling endosome. Golgi apparatus membrane; Multi-pass membrane protein. Golgi apparatus, trans-Golgi network. Endoplasmic reticulum membrane; Multi-pass membrane protein. Cell projection, dendrite. Cell projection, dendritic spine membrane; Multi-pass membrane protein. Cell projection, axon. Cell junction, synapse, postsynaptic cell membrane, postsynaptic density. Mitochondrion membrane; Multi-pass membrane protein. Note=Colocalized with BSN to the active zone of presynaptic density. Colocalized with DLG4/PSD95 and neurabin-2 PPP1R9B in neuronal synaptosomes (By similarity). Endocytosed in a agonist- and arrestin-independent manner. Colocalized with RAMP3 and clathrin-coated pits at the plasma membrane. Colocalized with transferrin receptor at the plasma membrane and perinuclear region. Accumulated and colocalized with RAB11 proteins in recycling endosomes and trans-Golgi network (TGN), but does neither recycle back to the cell surface nor traffics to late endosome or lysosome. Colocalized with calnexin in the endoplasmic reticulum. Traffics to intracellular sites via cytokeratin intermediate filaments like KRT7 and KRT8 after constitutive endocytosis in epithelial cells. Colocalized with EGFR in the nucleus of agonist-induced cancer-associated fibroblasts (CAF). {ECO:0000250}.

Gene Ontology (GO) - Cellular Components for GPER1 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0005829 cytosol IEA --
GO:0030424 axon ISS --
GO:0030425 dendrite ISS --
GO:0030659 cytoplasmic vesicle membrane IDA 21540189
GO:0031966 mitochondrial membrane ISS --
genes like me logo Genes that share ontologies with GPER1: view

No data available for Subcellular locations from COMPARTMENTS for GPER1 Gene

Pathways & Interactions for GPER1 Gene

genes like me logo Genes that share pathways with GPER1: view

Pathways by source for GPER1 Gene

Interacting Proteins for GPER1 Gene

SIGNOR curated interactions for GPER1 Gene

Activates:

Gene Ontology (GO) - Biological Process for GPER1 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0001956 positive regulation of neurotransmitter secretion ISS --
GO:0006954 inflammatory response IEA --
GO:0007186 G-protein coupled receptor signaling pathway IEA,IMP 23840305
GO:0007204 positive regulation of cytosolic calcium ion concentration IEA,ISS --
GO:0010579 positive regulation of adenylate cyclase activity involved in G-protein coupled receptor signaling pathway IDA 15539556
genes like me logo Genes that share ontologies with GPER1: view

Drugs & Compounds for GPER1 Gene

(31) Drugs for GPER1 Gene - From: Tocris, ApexBio, Novoseek, and DGIdb

Name Status Disease Links Group Role Mechanism of Action Clinical Trials
Fulvestrant Approved, Investigational Pharma Antagonist, inhibitor, antagonist Estrogen receptor antagonist,high affinity, Hormone therapy 173
Estradiol Approved, Investigational Pharma Sex hormone 1094
Estriol Approved Pharma Agonist 0
Estrone Approved Pharma Agonist Estrogenic hormone 19
Ethinyl Estradiol Approved Pharma Oral contraceptive 659

(3) Additional Compounds for GPER1 Gene - From: Tocris and Novoseek

Name Synonyms Role CAS Number PubChem IDs PubMed IDs
beta-Estradiol
50-28-2
ICI 182,780
129453-61-8

(5) Tocris Compounds for GPER1 Gene

Compound Action Cas Number
beta-Estradiol Endogenous ER agonist 50-28-2
Genistein EGFR kinase inhibitor. Also estrogen and PPARgamma ligand 446-72-0
ICI 182,780 Estrogen receptor antagonist 129453-61-8
Quercetin Non-selective PI 3-kinase inhibitor 117-39-5
Tamoxifen citrate Estrogen receptor partial agonist/antagonist 54965-24-1

(19) ApexBio Compounds for GPER1 Gene

Compound Action Cas Number
Altrenogest 850-52-2
Bazedoxifene HCl 198480-56-7
Clomiphene citrate 50-41-9
Equol 531-95-3
Estradiol Sex hormone 50-28-2
Estradiol Cypionate 313-06-4
Estriol 50-27-1
Estrone Estrogenic hormone 53-16-7
Ethinyl Estradiol Oral contraceptive 57-63-6
Ethisterone Progestogen hormone 434-03-7
Ethynodiol diacetate 297-76-7
Fulvestrant Estrogen receptor antagonist,high affinity 129453-61-8
Gestodene 60282-87-3
Hexestrol 84-16-2
Medroxyprogesterone acetate Steroidal progestin 71-58-9
Ospemifene 128607-22-7
Raloxifene HCl Estrogen receptor (ER) 82640-04-8
Tamoxifen Citrate Antiestrogen drug 54965-24-1
Toremifene Citrate 89778-27-8
genes like me logo Genes that share compounds with GPER1: view

Transcripts for GPER1 Gene

Alternative Splicing Database (ASD) splice patterns (SP) for GPER1 Gene

No ASD Table

Relevant External Links for GPER1 Gene

GeneLoc Exon Structure for
GPER1
ECgene alternative splicing isoforms for
GPER1

Expression for GPER1 Gene

mRNA expression in normal human tissues for GPER1 Gene

mRNA differential expression in normal tissues according to GTEx for GPER1 Gene

This gene is overexpressed in Stomach (x4.1).

mRNA Expression by UniProt/SwissProt for GPER1 Gene

Q99527-GPER1_HUMAN
Tissue specificity: Expressed in placenta, endothelial and epithelial cells, non laboring and laboring term myometrium, fibroblasts and cancer-associated fibroblasts (CAF), prostate cancer cells and invasive adenocarcinoma (at protein level). Ubiquitously expressed, but is most abundant in placenta. In brain regions, expressed as a 2.8 kb transcript in basal forebrain, frontal cortex, thalamus, hippocampus, caudate and putamen.
genes like me logo Genes that share expression patterns with GPER1: view

Primer Products

In Situ Assay Products

No data available for mRNA expression in embryonic tissues and stem cells from LifeMap Discovery , Protein differential expression in normal tissues , Protein expression and Protein tissue co-expression partners for GPER1 Gene

Orthologs for GPER1 Gene

This gene was present in the common ancestor of chordates.

Orthologs for GPER1 Gene

Organism Taxonomy Gene Similarity Type Details
cow
(Bos Taurus)
Mammalia GPER 35
  • 85.05 (n)
  • 84.57 (a)
GPER1 36
  • 83 (a)
OneToOne
dog
(Canis familiaris)
Mammalia GPER1 35
  • 86.49 (n)
  • 89.73 (a)
GPER1 36
  • 86 (a)
OneToOne
mouse
(Mus musculus)
Mammalia Gper1 35
  • 84.53 (n)
  • 86.93 (a)
Gper1 16
Gper1 36
  • 87 (a)
OneToOne
rat
(Rattus norvegicus)
Mammalia Gper1 35
  • 84 (n)
  • 86.13 (a)
oppossum
(Monodelphis domestica)
Mammalia GPER1 36
  • 80 (a)
OneToOne
platypus
(Ornithorhynchus anatinus)
Mammalia GPER1 36
  • 78 (a)
OneToOne
chicken
(Gallus gallus)
Aves GPER 35
  • 71.06 (n)
  • 77.59 (a)
GPER 36
  • 76 (a)
OneToOne
lizard
(Anolis carolinensis)
Reptilia GPER1 36
  • 79 (a)
OneToOne
tropical clawed frog
(Silurana tropicalis)
Amphibia gper1 35
  • 67.5 (n)
  • 70.36 (a)
zebrafish
(Danio rerio)
Actinopterygii gper1 35
  • 71.2 (n)
  • 71.52 (a)
gper1 36
  • 65 (a)
OneToOne
Species with no ortholog for GPER1:
  • A. gosspyii yeast (Ashbya gossypii)
  • Actinobacteria (Mycobacterium tuberculosis)
  • African clawed frog (Xenopus laevis)
  • African malaria mosquito (Anopheles gambiae)
  • Alicante grape (Vitis vinifera)
  • alpha proteobacteria (Wolbachia pipientis)
  • amoeba (Dictyostelium discoideum)
  • Archea (Pyrococcus horikoshii)
  • baker's yeast (Saccharomyces cerevisiae)
  • barley (Hordeum vulgare)
  • beta proteobacteria (Neisseria meningitidis)
  • bread mold (Neurospora crassa)
  • chimpanzee (Pan troglodytes)
  • Chromalveolata (Phytophthora infestans)
  • common water flea (Daphnia pulex)
  • corn (Zea mays)
  • E. coli (Escherichia coli)
  • filamentous fungi (Aspergillus nidulans)
  • Firmicute bacteria (Streptococcus pneumoniae)
  • fission yeast (Schizosaccharomyces pombe)
  • fruit fly (Drosophila melanogaster)
  • green algae (Chlamydomonas reinhardtii)
  • honey bee (Apis mellifera)
  • K. lactis yeast (Kluyveromyces lactis)
  • loblloly pine (Pinus taeda)
  • malaria parasite (Plasmodium falciparum)
  • medicago trunc (Medicago Truncatula)
  • moss (Physcomitrella patens)
  • orangutan (Pongo pygmaeus)
  • pig (Sus scrofa)
  • rainbow trout (Oncorhynchus mykiss)
  • rice (Oryza sativa)
  • rice blast fungus (Magnaporthe grisea)
  • schistosome parasite (Schistosoma mansoni)
  • sea anemone (Nematostella vectensis)
  • sea squirt (Ciona intestinalis)
  • sea squirt (Ciona savignyi)
  • sea urchin (Strongylocentrotus purpuratus)
  • sorghum (Sorghum bicolor)
  • soybean (Glycine max)
  • stem rust fungus (Puccinia graminis)
  • sugarcane (Saccharum officinarum)
  • thale cress (Arabidopsis thaliana)
  • tomato (Lycopersicon esculentum)
  • toxoplasmosis (Toxoplasma gondii)
  • Trichoplax (Trichoplax adhaerens)
  • wheat (Triticum aestivum)
  • worm (Caenorhabditis elegans)

Evolution for GPER1 Gene

ENSEMBL:
Gene Tree for GPER1 (if available)
TreeFam:
Gene Tree for GPER1 (if available)

Paralogs for GPER1 Gene

Paralogs for GPER1 Gene

(5) SIMAP similar genes for GPER1 Gene using alignment to 2 proteins:

genes like me logo Genes that share paralogs with GPER1: view

Variants for GPER1 Gene

Sequence variations from dbSNP and Humsavar for GPER1 Gene

SNP ID Clin Chr 07 pos Sequence Context AA Info Type
VAR_033319 -

Variation tolerance for GPER1 Gene

Residual Variation Intolerance Score: 11.8% of all genes are more intolerant (likely to be disease-causing)
Gene Damage Index Score: 4.28; 62.64% of all genes are more intolerant (likely to be disease-causing)

Relevant External Links for GPER1 Gene

HapMap Linkage Disequilibrium report
GPER1

No data available for Polymorphic Variants from UniProtKB/Swiss-Prot and Structural Variations from Database of Genomic Variants (DGV) for GPER1 Gene

Disorders for GPER1 Gene

MalaCards: The human disease database

(2) MalaCards diseases for GPER1 Gene - From: DISEASES, Novoseek, and GeneCards

Disorder Aliases PubMed IDs
breast cancer
  • breast cancer, invasive ductal
urethral intrinsic sphincter deficiency
  • intrinsic sphincter deficiency [isd]
- elite association - COSMIC cancer census association via MalaCards
Search GPER1 in MalaCards View complete list of genes associated with diseases

Relevant External Links for GPER1

Atlas of Genetics and Cytogenetics in Oncology and Haematology:
GPER1
genes like me logo Genes that share disorders with GPER1: view

No data available for UniProtKB/Swiss-Prot and Genatlas for GPER1 Gene

Publications for GPER1 Gene

  1. Discovery of three novel G-protein-coupled receptor genes. (PMID: 9479505) O'Dowd B.F. … George S.R. (Genomics 1998) 2 3 4 67
  2. Involvement of estrogen receptor variant ER-alpha36, not GPR30, in nongenomic estrogen signaling. (PMID: 20197310) Kang L. … Wang Z.Y. (Mol. Endocrinol. 2010) 3 23
  3. Coordinate regulation of estrogen-mediated fibronectin matrix assembly and epidermal growth factor receptor transactivation by the G protein-coupled receptor, GPR30. (PMID: 19342448) Quinn J.A. … Filardo E.J. (Mol. Endocrinol. 2009) 3 23
  4. Estrogenic G protein-coupled receptor 30 signaling is involved in regulation of endometrial carcinoma by promoting proliferation, invasion potential, and interleukin-6 secretion via the MEK/ERK mitogen-activated protein kinase pathway. (PMID: 19432902) He Y.Y. … Wan X.P. (Cancer Sci. 2009) 3 23
  5. G protein-coupled receptor 30 expression is up-regulated by EGF and TGF alpha in estrogen receptor alpha-positive cancer cells. (PMID: 19749156) Vivacqua A. … Maggiolini M. (Mol. Endocrinol. 2009) 3 23

Products for GPER1 Gene

Sources for GPER1 Gene

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