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Aliases for GPER1 Gene

Aliases for GPER1 Gene

  • G Protein-Coupled Estrogen Receptor 1 2 3 4
  • CMKRL2 3 4 6
  • GPR30 3 4 6
  • GPER 3 4 6
  • 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
  • LyGPR 3 4
  • DRY12 3 4
  • FEG-1 3 4
  • CEPR 3 4
  • MER 3 4
  • Constitutively Expressed Peptide-Like Receptor 3
  • G-Protein Coupled Estrogen Receptor 1 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 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 pain disorder. Among its related pathways are Signaling by GPCR and Signaling by GPCR. 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.

Tocris Summary for GPER1 Gene

  • The GPR30 receptor is an orphan G-protein-coupled receptor that has recently been shown to bind estrogen and cause estrogen-mediated adenylyl cyclase stimulation. GPR30 is widely distributed in neural, breast cancer, placental, heart, ovarian, prostate, hepatic, vascular epithelial and lymphoid tissue. The receptor acts independently of ERalpha and ERbeta and triggers ER-dependent EGFR action.

Gene Wiki entry for GPER1 Gene

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

Genomics for GPER1 Gene

Genomic Location for GPER1 Gene

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

UCSC Golden Path with GeneCards custom track
Cytogenetic band:
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

Other Protein References for GPER1 Gene

No data available for DME Specific Peptides for GPER1 Gene

Domains for GPER1 Gene

Protein Domains for GPER1 Gene

InterPro:
ProtoNet:

UniProtKB/Swiss-Prot:

GPER1_HUMAN
Family:
  • Belongs to the G-protein coupled receptor 1 family.:
    • Q99527
genes like me logo Genes that share domains with GPER1: view

No data available for Gene Families for GPER1 Gene

Function for GPER1 Gene

Molecular function for GPER1 Gene

UniProtKB/Swiss-Prot BiophysicochemicalProperties: Kinetic parameters: KM=3.3 mM for 17-beta-estradiol {ECO:0000269 PubMed:15539556, ECO:0000269 PubMed:15705806, ECO:0000269 PubMed:19931550}; KM=6.6 mM for 17-beta-estradiol {ECO:0000269 PubMed:15539556, ECO:0000269 PubMed:15705806, ECO:0000269 PubMed:19931550}; KM=3.3 mM for 17-beta-estradiol {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.

Gene Ontology (GO) - Molecular Function for GPER1 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0003682 chromatin binding IDA 20551055
GO:0004930 G-protein coupled receptor activity IEA --
GO:0005496 steroid binding IDA 15539556
GO:0005515 protein binding IPI 20551055
GO:0017082 mineralocorticoid receptor activity ISS --
genes like me logo Genes that share ontologies with GPER1: view
genes like me logo Genes that share phenotypes with GPER1: view

Animal Models for GPER1 Gene

MGI Knock Outs for GPER1:

miRNA for GPER1 Gene

miRTarBase miRNAs that target GPER1

No data available for Enzyme Numbers (IUBMB) , Transcription Factor Targeting 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:0000139 Golgi membrane IEA --
GO:0005622 intracellular ISS --
GO:0005634 nucleus IDA 20551055
GO:0005635 nuclear envelope IDA 15705806
GO:0005737 cytoplasm ISS --
genes like me logo Genes that share ontologies with GPER1: view

Pathways 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

Gene Ontology (GO) - Biological Process for GPER1 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0001934 positive regulation of protein phosphorylation ISS --
GO:0001956 positive regulation of neurotransmitter secretion ISS --
GO:0002695 negative regulation of leukocyte activation IDA 23285008
GO:0006954 inflammatory response IEA --
GO:0007049 cell cycle IEA --
genes like me logo Genes that share ontologies with GPER1: view

Compounds for GPER1 Gene

(3) Tocris Compounds for GPER1 Gene

Compound Action Cas Number
G-1 Potent and selective GPR30 agonist [881639-98-1]
G-15 High affinity and selective GPR30 antagonist [1161002-05-6]
G-36 Selective GPR30 antagonist [1392487-51-2]

(6) Novoseek inferred chemical compound relationships for GPER1 Gene

Compound -log(P) Hits PubMed IDs
estrogen 74.6 49
progestin 62.6 12
estradiol 48.4 1
steroid 44.2 5
progesterone 35 2
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 expression in embryonic tissues and stem cells from LifeMap Discovery

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

This gene is overexpressed in Stomach (4.1).

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 expressions with GPER1: view

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 36
  • 85.05 (n)
  • 84.57 (a)
GPER1 37
  • 83 (a)
OneToOne
dog
(Canis familiaris)
Mammalia GPER1 36
  • 86.49 (n)
  • 89.73 (a)
GPER1 37
  • 86 (a)
OneToOne
mouse
(Mus musculus)
Mammalia Gper1 36
  • 84.53 (n)
  • 86.93 (a)
Gper1 37
  • 87 (a)
OneToOne
Gpr30 16
oppossum
(Monodelphis domestica)
Mammalia GPER1 37
  • 80 (a)
OneToOne
platypus
(Ornithorhynchus anatinus)
Mammalia GPER1 37
  • 78 (a)
OneToOne
rat
(Rattus norvegicus)
Mammalia Gper1 36
  • 84 (n)
  • 86.13 (a)
chicken
(Gallus gallus)
Aves GPER 36
  • 71.06 (n)
  • 77.59 (a)
GPER 37
  • 76 (a)
OneToOne
lizard
(Anolis carolinensis)
Reptilia GPER1 37
  • 79 (a)
OneToOne
tropical clawed frog
(Silurana tropicalis)
Amphibia gper1 36
  • 67.5 (n)
  • 70.36 (a)
zebrafish
(Danio rerio)
Actinopterygii gper1 36
  • 71.2 (n)
  • 71.52 (a)
gper1 37
  • 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

Selected 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 MAF
VAR_033319 -

Relevant External Links for GPER1 Gene

HapMap Linkage Disequilibrium report
GPER1

No data available for Structural Variations from Database of Genomic Variants (DGV) for GPER1 Gene

Disorders for GPER1 Gene

(2) MalaCards Diseases for GPER1 Gene

Search for GPER1 Gene in MalaCards »

(4) Novoseek inferred disease relationships for GPER1 Gene

Disease -log(P) Hits PubMed IDs
breast cancer 48.8 19
ovarian cancer 22.1 4
tumors 15.2 6
cancer 0.465 4
genes like me logo Genes that share disorders with GPER1: view

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

Publications for GPER1 Gene

  1. Identification of a gene (GPR30) with homology to the G-protein- coupled receptor superfamily associated with estrogen receptor expression in breast cancer. (PMID: 9367686) Carmeci C. … Weigel R.J. (Genomics 1997) 3 4 23
  2. Estrogen-induced activation of Erk-1 and Erk-2 requires the G protein-coupled receptor homolog, GPR30, and occurs via trans- activation of the epidermal growth factor receptor through release of HB-EGF. (PMID: 11043579) Filardo E.J. … Frackelton A.R. Jr. (Mol. Endocrinol. 2000) 3 4 23
  3. Progestin upregulates G-protein-coupled receptor 30 in breast cancer cells. (PMID: 12027886) Ahola T.M. … Ylikomi T. (Eur. J. Biochem. 2002) 3 4 23
  4. Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. (PMID: 15539556) Thomas P. … Dong J. (Endocrinology 2005) 3 4 23
  5. G protein-coupled receptor 30 localizes to the endoplasmic reticulum and is not activated by estradiol. (PMID: 18566127) Otto C. … Fritzemeier K.H. (Endocrinology 2008) 3 4 23

Products for GPER1 Gene

  • DNA Methylation CpG Assay Predesigned for Pyrosequencing in human,mouse,rat
  • QIAGEN qRT-PCR Assays for microRNAs that regulate GPER1
    • QuantiTect SYBR Green Assays in human,mouse,rat
    • Pre-validated RT² qPCR Primer Assay in human,mouse,rat
    • QuantiFast Probe-based Assays in human,mouse,rat
    • Predesigned siRNA for gene silencing in human,mouse,rat for GPER1
    • Block miRNA regulation of GPER1 using miScript Target Protectors

    Sources for GPER1 Gene

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