Browse GPER1

Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Basic function annotation.
> Subcellular Location, Domain and Function
> Gene Ontology
> KEGG and Reactome Pathway
> Subcellular Location, Domain and Function
 
Subcellular Location 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).
Domain PF00001 7 transmembrane receptor (rhodopsin family)
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.

> Gene Ontology
 
Biological Process GO:0001505 regulation of neurotransmitter levels
GO:0001508 action potential
GO:0001678 cellular glucose homeostasis
GO:0001836 release of cytochrome c from mitochondria
GO:0001933 negative regulation of protein phosphorylation
GO:0001956 positive regulation of neurotransmitter secretion
GO:0002683 negative regulation of immune system process
GO:0002694 regulation of leukocyte activation
GO:0002695 negative regulation of leukocyte activation
GO:0002790 peptide secretion
GO:0002791 regulation of peptide secretion
GO:0002793 positive regulation of peptide secretion
GO:0003012 muscle system process
GO:0003013 circulatory system process
GO:0003018 vascular process in circulatory system
GO:0006066 alcohol metabolic process
GO:0006109 regulation of carbohydrate metabolic process
GO:0006140 regulation of nucleotide metabolic process
GO:0006164 purine nucleotide biosynthetic process
GO:0006171 cAMP biosynthetic process
GO:0006323 DNA packaging
GO:0006816 calcium ion transport
GO:0006836 neurotransmitter transport
GO:0006874 cellular calcium ion homeostasis
GO:0006875 cellular metal ion homeostasis
GO:0006921 cellular component disassembly involved in execution phase of apoptosis
GO:0006936 muscle contraction
GO:0006937 regulation of muscle contraction
GO:0006939 smooth muscle contraction
GO:0006940 regulation of smooth muscle contraction
GO:0006997 nucleus organization
GO:0006998 nuclear envelope organization
GO:0007009 plasma membrane organization
GO:0007050 cell cycle arrest
GO:0007173 epidermal growth factor receptor signaling pathway
GO:0007187 G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
GO:0007188 adenylate cyclase-modulating G-protein coupled receptor signaling pathway
GO:0007189 adenylate cyclase-activating G-protein coupled receptor signaling pathway
GO:0007204 positive regulation of cytosolic calcium ion concentration
GO:0007269 neurotransmitter secretion
GO:0007507 heart development
GO:0008015 blood circulation
GO:0008277 regulation of G-protein coupled receptor protein signaling pathway
GO:0008637 apoptotic mitochondrial changes
GO:0009150 purine ribonucleotide metabolic process
GO:0009152 purine ribonucleotide biosynthetic process
GO:0009165 nucleotide biosynthetic process
GO:0009187 cyclic nucleotide metabolic process
GO:0009190 cyclic nucleotide biosynthetic process
GO:0009260 ribonucleotide biosynthetic process
GO:0009306 protein secretion
GO:0009743 response to carbohydrate
GO:0009746 response to hexose
GO:0009749 response to glucose
GO:0009755 hormone-mediated signaling pathway
GO:0009914 hormone transport
GO:0010522 regulation of calcium ion transport into cytosol
GO:0010524 positive regulation of calcium ion transport into cytosol
GO:0010578 regulation of adenylate cyclase activity involved in G-protein coupled receptor signaling pathway
GO:0010579 positive regulation of adenylate cyclase activity involved in G-protein coupled receptor signaling pathway
GO:0010675 regulation of cellular carbohydrate metabolic process
GO:0010676 positive regulation of cellular carbohydrate metabolic process
GO:0010720 positive regulation of cell development
GO:0010817 regulation of hormone levels
GO:0010821 regulation of mitochondrion organization
GO:0010822 positive regulation of mitochondrion organization
GO:0010919 regulation of inositol phosphate biosynthetic process
GO:0010948 negative regulation of cell cycle process
GO:0010950 positive regulation of endopeptidase activity
GO:0010952 positive regulation of peptidase activity
GO:0010959 regulation of metal ion transport
GO:0014065 phosphatidylinositol 3-kinase signaling
GO:0014066 regulation of phosphatidylinositol 3-kinase signaling
GO:0014068 positive regulation of phosphatidylinositol 3-kinase signaling
GO:0015833 peptide transport
GO:0016051 carbohydrate biosynthetic process
GO:0019216 regulation of lipid metabolic process
GO:0019226 transmission of nerve impulse
GO:0019228 neuronal action potential
GO:0019751 polyol metabolic process
GO:0023061 signal release
GO:0030072 peptide hormone secretion
GO:0030073 insulin secretion
GO:0030261 chromosome condensation
GO:0030262 apoptotic nuclear changes
GO:0030263 apoptotic chromosome condensation
GO:0030264 nuclear fragmentation involved in apoptotic nuclear change
GO:0030335 positive regulation of cell migration
GO:0030518 intracellular steroid hormone receptor signaling pathway
GO:0030522 intracellular receptor signaling pathway
GO:0030799 regulation of cyclic nucleotide metabolic process
GO:0030801 positive regulation of cyclic nucleotide metabolic process
GO:0030802 regulation of cyclic nucleotide biosynthetic process
GO:0030804 positive regulation of cyclic nucleotide biosynthetic process
GO:0030808 regulation of nucleotide biosynthetic process
GO:0030810 positive regulation of nucleotide biosynthetic process
GO:0030814 regulation of cAMP metabolic process
GO:0030816 positive regulation of cAMP metabolic process
GO:0030817 regulation of cAMP biosynthetic process
GO:0030819 positive regulation of cAMP biosynthetic process
GO:0031279 regulation of cyclase activity
GO:0031281 positive regulation of cyclase activity
GO:0031348 negative regulation of defense response
GO:0031958 corticosteroid receptor signaling pathway
GO:0031959 mineralocorticoid receptor signaling pathway
GO:0031960 response to corticosteroid
GO:0032024 positive regulation of insulin secretion
GO:0032102 negative regulation of response to external stimulus
GO:0032355 response to estradiol
GO:0032844 regulation of homeostatic process
GO:0032845 negative regulation of homeostatic process
GO:0032846 positive regulation of homeostatic process
GO:0032957 inositol trisphosphate metabolic process
GO:0032958 inositol phosphate biosynthetic process
GO:0032959 inositol trisphosphate biosynthetic process
GO:0032960 regulation of inositol trisphosphate biosynthetic process
GO:0032962 positive regulation of inositol trisphosphate biosynthetic process
GO:0033002 muscle cell proliferation
GO:0033500 carbohydrate homeostasis
GO:0034284 response to monosaccharide
GO:0034612 response to tumor necrosis factor
GO:0034762 regulation of transmembrane transport
GO:0034764 positive regulation of transmembrane transport
GO:0034765 regulation of ion transmembrane transport
GO:0034767 positive regulation of ion transmembrane transport
GO:0035051 cardiocyte differentiation
GO:0035150 regulation of tube size
GO:0035637 multicellular organismal signaling
GO:0035886 vascular smooth muscle cell differentiation
GO:0038127 ERBB signaling pathway
GO:0040017 positive regulation of locomotion
GO:0042058 regulation of epidermal growth factor receptor signaling pathway
GO:0042311 vasodilation
GO:0042312 regulation of vasodilation
GO:0042326 negative regulation of phosphorylation
GO:0042391 regulation of membrane potential
GO:0042593 glucose homeostasis
GO:0042692 muscle cell differentiation
GO:0042886 amide transport
GO:0043255 regulation of carbohydrate biosynthetic process
GO:0043270 positive regulation of ion transport
GO:0043280 positive regulation of cysteine-type endopeptidase activity involved in apoptotic process
GO:0043281 regulation of cysteine-type endopeptidase activity involved in apoptotic process
GO:0043401 steroid hormone mediated signaling pathway
GO:0043409 negative regulation of MAPK cascade
GO:0043410 positive regulation of MAPK cascade
GO:0043434 response to peptide hormone
GO:0043491 protein kinase B signaling
GO:0043647 inositol phosphate metabolic process
GO:0044057 regulation of system process
GO:0044262 cellular carbohydrate metabolic process
GO:0044283 small molecule biosynthetic process
GO:0044723 single-organism carbohydrate metabolic process
GO:0045444 fat cell differentiation
GO:0045598 regulation of fat cell differentiation
GO:0045599 negative regulation of fat cell differentiation
GO:0045742 positive regulation of epidermal growth factor receptor signaling pathway
GO:0045745 positive regulation of G-protein coupled receptor protein signaling pathway
GO:0045761 regulation of adenylate cyclase activity
GO:0045762 positive regulation of adenylate cyclase activity
GO:0045786 negative regulation of cell cycle
GO:0045787 positive regulation of cell cycle
GO:0045833 negative regulation of lipid metabolic process
GO:0045862 positive regulation of proteolysis
GO:0045909 positive regulation of vasodilation
GO:0045913 positive regulation of carbohydrate metabolic process
GO:0045933 positive regulation of muscle contraction
GO:0045981 positive regulation of nucleotide metabolic process
GO:0045987 positive regulation of smooth muscle contraction
GO:0046058 cAMP metabolic process
GO:0046165 alcohol biosynthetic process
GO:0046173 polyol biosynthetic process
GO:0046390 ribose phosphate biosynthetic process
GO:0046879 hormone secretion
GO:0046883 regulation of hormone secretion
GO:0046887 positive regulation of hormone secretion
GO:0046890 regulation of lipid biosynthetic process
GO:0046928 regulation of neurotransmitter secretion
GO:0048015 phosphatidylinositol-mediated signaling
GO:0048017 inositol lipid-mediated signaling
GO:0048545 response to steroid hormone
GO:0048659 smooth muscle cell proliferation
GO:0048660 regulation of smooth muscle cell proliferation
GO:0048662 negative regulation of smooth muscle cell proliferation
GO:0050708 regulation of protein secretion
GO:0050714 positive regulation of protein secretion
GO:0050727 regulation of inflammatory response
GO:0050728 negative regulation of inflammatory response
GO:0050769 positive regulation of neurogenesis
GO:0050796 regulation of insulin secretion
GO:0050804 modulation of synaptic transmission
GO:0050806 positive regulation of synaptic transmission
GO:0050865 regulation of cell activation
GO:0050866 negative regulation of cell activation
GO:0050880 regulation of blood vessel size
GO:0051047 positive regulation of secretion
GO:0051052 regulation of DNA metabolic process
GO:0051053 negative regulation of DNA metabolic process
GO:0051055 negative regulation of lipid biosynthetic process
GO:0051145 smooth muscle cell differentiation
GO:0051147 regulation of muscle cell differentiation
GO:0051149 positive regulation of muscle cell differentiation
GO:0051150 regulation of smooth muscle cell differentiation
GO:0051152 positive regulation of smooth muscle cell differentiation
GO:0051208 sequestering of calcium ion
GO:0051209 release of sequestered calcium ion into cytosol
GO:0051222 positive regulation of protein transport
GO:0051235 maintenance of location
GO:0051238 sequestering of metal ion
GO:0051272 positive regulation of cellular component movement
GO:0051279 regulation of release of sequestered calcium ion into cytosol
GO:0051281 positive regulation of release of sequestered calcium ion into cytosol
GO:0051282 regulation of sequestering of calcium ion
GO:0051283 negative regulation of sequestering of calcium ion
GO:0051339 regulation of lyase activity
GO:0051349 positive regulation of lyase activity
GO:0051385 response to mineralocorticoid
GO:0051480 regulation of cytosolic calcium ion concentration
GO:0051588 regulation of neurotransmitter transport
GO:0051590 positive regulation of neurotransmitter transport
GO:0051896 regulation of protein kinase B signaling
GO:0051898 negative regulation of protein kinase B signaling
GO:0051924 regulation of calcium ion transport
GO:0051928 positive regulation of calcium ion transport
GO:0051962 positive regulation of nervous system development
GO:0052547 regulation of peptidase activity
GO:0052548 regulation of endopeptidase activity
GO:0052652 cyclic purine nucleotide metabolic process
GO:0055074 calcium ion homeostasis
GO:0060401 cytosolic calcium ion transport
GO:0060402 calcium ion transport into cytosol
GO:0060732 positive regulation of inositol phosphate biosynthetic process
GO:0060947 cardiac vascular smooth muscle cell differentiation
GO:0060976 coronary vasculature development
GO:0070371 ERK1 and ERK2 cascade
GO:0070372 regulation of ERK1 and ERK2 cascade
GO:0070373 negative regulation of ERK1 and ERK2 cascade
GO:0070374 positive regulation of ERK1 and ERK2 cascade
GO:0070471 uterine smooth muscle contraction
GO:0070472 regulation of uterine smooth muscle contraction
GO:0070474 positive regulation of uterine smooth muscle contraction
GO:0070509 calcium ion import
GO:0070588 calcium ion transmembrane transport
GO:0070838 divalent metal ion transport
GO:0071103 DNA conformation change
GO:0071156 regulation of cell cycle arrest
GO:0071157 negative regulation of cell cycle arrest
GO:0071322 cellular response to carbohydrate stimulus
GO:0071326 cellular response to monosaccharide stimulus
GO:0071331 cellular response to hexose stimulus
GO:0071333 cellular response to glucose stimulus
GO:0071356 cellular response to tumor necrosis factor
GO:0071375 cellular response to peptide hormone stimulus
GO:0071383 cellular response to steroid hormone stimulus
GO:0071384 cellular response to corticosteroid stimulus
GO:0071389 cellular response to mineralocorticoid stimulus
GO:0071392 cellular response to estradiol stimulus
GO:0071396 cellular response to lipid
GO:0071407 cellular response to organic cyclic compound
GO:0071417 cellular response to organonitrogen compound
GO:0071763 nuclear membrane organization
GO:0072503 cellular divalent inorganic cation homeostasis
GO:0072507 divalent inorganic cation homeostasis
GO:0072511 divalent inorganic cation transport
GO:0072522 purine-containing compound biosynthetic process
GO:0072577 endothelial cell apoptotic process
GO:0072657 protein localization to membrane
GO:0072659 protein localization to plasma membrane
GO:0090002 establishment of protein localization to plasma membrane
GO:0090003 regulation of establishment of protein localization to plasma membrane
GO:0090004 positive regulation of establishment of protein localization to plasma membrane
GO:0090066 regulation of anatomical structure size
GO:0090087 regulation of peptide transport
GO:0090150 establishment of protein localization to membrane
GO:0090199 regulation of release of cytochrome c from mitochondria
GO:0090200 positive regulation of release of cytochrome c from mitochondria
GO:0090257 regulation of muscle system process
GO:0090276 regulation of peptide hormone secretion
GO:0090277 positive regulation of peptide hormone secretion
GO:0090279 regulation of calcium ion import
GO:0090280 positive regulation of calcium ion import
GO:0097191 extrinsic apoptotic signaling pathway
GO:0097194 execution phase of apoptosis
GO:0097553 calcium ion transmembrane import into cytosol
GO:0099531 presynaptic process involved in chemical synaptic transmission
GO:0099643 signal release from synapse
GO:1900371 regulation of purine nucleotide biosynthetic process
GO:1900373 positive regulation of purine nucleotide biosynthetic process
GO:1900542 regulation of purine nucleotide metabolic process
GO:1900544 positive regulation of purine nucleotide metabolic process
GO:1901184 regulation of ERBB signaling pathway
GO:1901186 positive regulation of ERBB signaling pathway
GO:1901293 nucleoside phosphate biosynthetic process
GO:1901342 regulation of vasculature development
GO:1901615 organic hydroxy compound metabolic process
GO:1901617 organic hydroxy compound biosynthetic process
GO:1901652 response to peptide
GO:1901653 cellular response to peptide
GO:1902532 negative regulation of intracellular signal transduction
GO:1902656 calcium ion import into cytosol
GO:1902930 regulation of alcohol biosynthetic process
GO:1902932 positive regulation of alcohol biosynthetic process
GO:1903076 regulation of protein localization to plasma membrane
GO:1903078 positive regulation of protein localization to plasma membrane
GO:1903169 regulation of calcium ion transmembrane transport
GO:1903522 regulation of blood circulation
GO:1903524 positive regulation of blood circulation
GO:1903532 positive regulation of secretion by cell
GO:1903729 regulation of plasma membrane organization
GO:1903829 positive regulation of cellular protein localization
GO:1904018 positive regulation of vasculature development
GO:1904019 epithelial cell apoptotic process
GO:1904035 regulation of epithelial cell apoptotic process
GO:1904037 positive regulation of epithelial cell apoptotic process
GO:1904062 regulation of cation transmembrane transport
GO:1904064 positive regulation of cation transmembrane transport
GO:1904375 regulation of protein localization to cell periphery
GO:1904377 positive regulation of protein localization to cell periphery
GO:1904427 positive regulation of calcium ion transmembrane transport
GO:1904705 regulation of vascular smooth muscle cell proliferation
GO:1904706 negative regulation of vascular smooth muscle cell proliferation
GO:1904951 positive regulation of establishment of protein localization
GO:1905063 regulation of vascular smooth muscle cell differentiation
GO:1905065 positive regulation of vascular smooth muscle cell differentiation
GO:1905207 regulation of cardiocyte differentiation
GO:1905209 positive regulation of cardiocyte differentiation
GO:1990778 protein localization to cell periphery
GO:1990874 vascular smooth muscle cell proliferation
GO:2000021 regulation of ion homeostasis
GO:2000116 regulation of cysteine-type endopeptidase activity
GO:2000147 positive regulation of cell motility
GO:2000351 regulation of endothelial cell apoptotic process
GO:2000353 positive regulation of endothelial cell apoptotic process
GO:2000722 regulation of cardiac vascular smooth muscle cell differentiation
GO:2000724 positive regulation of cardiac vascular smooth muscle cell differentiation
GO:2001056 positive regulation of cysteine-type endopeptidase activity
GO:2001233 regulation of apoptotic signaling pathway
GO:2001235 positive regulation of apoptotic signaling pathway
GO:2001236 regulation of extrinsic apoptotic signaling pathway
GO:2001238 positive regulation of extrinsic apoptotic signaling pathway
Molecular Function GO:0003682 chromatin binding
GO:0003707 steroid hormone receptor activity
GO:0004879 RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding
GO:0005496 steroid binding
GO:0017082 mineralocorticoid receptor activity
GO:0030284 estrogen receptor activity
GO:0042562 hormone binding
GO:0098531 transcription factor activity, direct ligand regulated sequence-specific DNA binding
GO:1990239 steroid hormone binding
Cellular Component GO:0005635 nuclear envelope
GO:0005769 early endosome
GO:0005802 trans-Golgi network
GO:0005882 intermediate filament
GO:0014069 postsynaptic density
GO:0030424 axon
GO:0030425 dendrite
GO:0030659 cytoplasmic vesicle membrane
GO:0031252 cell leading edge
GO:0031253 cell projection membrane
GO:0031256 leading edge membrane
GO:0031984 organelle subcompartment
GO:0032589 neuron projection membrane
GO:0032590 dendrite membrane
GO:0032591 dendritic spine membrane
GO:0033267 axon part
GO:0042734 presynaptic membrane
GO:0043197 dendritic spine
GO:0043198 dendritic shaft
GO:0043679 axon terminus
GO:0044306 neuron projection terminus
GO:0044309 neuron spine
GO:0044327 dendritic spine head
GO:0045095 keratin filament
GO:0045111 intermediate filament cytoskeleton
GO:0048786 presynaptic active zone
GO:0055037 recycling endosome
GO:0060076 excitatory synapse
GO:0097060 synaptic membrane
GO:0098791 Golgi subcompartment
GO:0098793 presynapse
GO:0098794 postsynapse
GO:0099572 postsynaptic specialization
> KEGG and Reactome Pathway
 
KEGG hsa04915 Estrogen signaling pathway
Reactome R-HSA-373076: Class A/1 (Rhodopsin-like receptors)
R-HSA-418594: G alpha (i) signalling events
R-HSA-388396: GPCR downstream signaling
R-HSA-500792: GPCR ligand binding
R-HSA-375276: Peptide ligand-binding receptors
R-HSA-162582: Signal Transduction
R-HSA-372790: Signaling by GPCR
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Literatures that report relations between GPER1 and anti-tumor immunity. The specific mechanism were also collected if the literature reports that a gene specifically promotes or inhibits the infiltration or function of T/NK cells.
> Text Mining
 
  Literatures describing the relation between GPER1 and anti-tumor immunity in human cancer.
PMID Cancer type Relation to immunity Evidence sentences
29336307MelanomaPromote immunity (T/NK cell function); increase the efficacy of immunotherapyActivation of G protein-coupled estrogen receptor signaling inhibits melanoma and improves response to immune checkpoint blockade. Selective GPER activation in primary melanocytes and melanoma cells induced long-term changes that maintained a more differentiated cell state as defined by increased expression of well-established melanocyte differentiation antigens, increased pigment production, decreased proliferative capacity, and decreased expression of the oncodriver and stem cell marker c-Myc. GPER signaling also rendered melanoma cells more vulnerable to immunotherapy.
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content High-throughput screening data (e.g. CRISPR-Cas9, shRNA and RNAi) for T cell-mediated killing. Genetic screen techniques can identify mechanisms of tumor cell resistance (e.g., PTPN2) and sensitivity (e.g., APLNR) to killing by cytotoxic T cells, the central effectors of anti-tumor immunity. After comprehensively searching, eight groups of screening data sets were collected in the current database. In this tab, users can check whether their selected genes cause resistance or increase sensitivity to T cell-mediated killing in various data sets.
> High-throughput Screening
  Statistical results of GPER1 in screening data sets for detecting immune reponses.
PMID Screening System Cancer Type Cell Line Data Set Statistical Results Relation to immunity
29301958CRISPR-Cas9 melanomaB16F10Pmel-1 T cell NA/NSNA/NS
29301958CRISPR-Cas9 melanomaB16F10OT-1 T cell NA/NSNA/NS
28783722CRISPR-Cas9 melanomaMel6242CT-CRISPR NA/NSNA/NS
28723893CRISPR-Cas9 melanomaB16GVAX+Anti-PD1 NA/NSNA/NS
28723893CRISPR-Cas9 melanomaB16GVAX NA/NSNA/NS
25691366RNAiBreast cancerMCF7Luc-CTL assay NA/NSNA/NS
24476824shRNAmelanomaB16Primary screen NA/NSNA/NS
24476824shRNAmelanomaB16Secondary screen NA/NSNA/NS
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Transcriptomic and genomic profiling of pre-treated tumor biopsies from responders and non-responders to immunotherapy. These data were used to identify signatures and mechanisms of response to checkpoint blockade (e.g., anti-PDL1 and anti-PD1). One example is that mutations in the gene PBRM1 benefit clinical survival of patients with clear cell renal cell carcinoma. After comprehensively searching, we collected 5 and 6 of transcriptomic and genomic data sets, respectively. In this tab, users can check whether their selected genes have significant difference of expression or mutation between responders and non-responders in various data sets.
> Expression difference between responders and non-responders
> Mutation difference between responders and non-responders
> Expression difference between responders and non-responders
 
Points in the above scatter plot represent the expression difference of GPER1 in various data sets.
No PMID Cancer type Group Drug # Res # NRes Log2 (Fold Change) P value Anno
126997480MelanomaallAnti-PD-1 (pembrolizumab and nivolumab)1412-0.4850.26
226997480MelanomaMAPKiAnti-PD-1 (pembrolizumab and nivolumab)65-0.9250.323
326997480Melanomanon-MAPKiAnti-PD-1 (pembrolizumab and nivolumab)87-0.1540.819
428552987Urothelial cancerallAnti-PD-L1 (atezolizumab) 9160.5110.387
528552987Urothelial cancersmokingAnti-PD-L1 (atezolizumab) 590.2980.843
628552987Urothelial cancernon-smokingAnti-PD-L1 (atezolizumab) 470.7870.696
729033130MelanomaallAnti-PD-1 (nivolumab) 2623-0.6010.245
829033130MelanomaNIV3-PROGAnti-PD-1 (nivolumab) 1511-0.5720.494
929033130MelanomaNIV3-NAIVEAnti-PD-1 (nivolumab) 1112-0.7760.432
1029301960Clear cell renal cell carcinoma (ccRCC)allAnti-PD-1 (nivolumab) 48-0.4020.713
1129301960Clear cell renal cell carcinoma (ccRCC)VEGFRiAnti-PD-1 (nivolumab) 2001
1229301960Clear cell renal cell carcinoma (ccRCC)non-VEGFRiAnti-PD-1 (nivolumab) 28-0.2270.877
1329443960Urothelial cancerallAnti-PD-L1 (atezolizumab) 68230-0.2920.0939
> Mutation difference between responders and non-responders
 
Points in the above scatter plot represent the mutation difference of GPER1 in various data sets.
No PMID Cancer type Group Drug # Res # NRes % Mut/Res % Mut/NRes % Diff (R vs NR) Pval Anno
125765070Non-small cell lung cancer (NSCLC)allAnti-PD-1 (pembrolizumab) 141705.9-5.91
225765070Non-small cell lung cancer (NSCLC)smokingAnti-PD-1 (pembrolizumab) 1030001
325765070Non-small cell lung cancer (NSCLC)non-smokingAnti-PD-1 (pembrolizumab) 41407.1-7.11
426359337MelanomaallAnti-CTLA-4 (ipilimumab) 27733.703.70.27
526359337MelanomaBRAFiAnti-CTLA-4 (ipilimumab) 0140001
626359337Melanomanon-BRAFiAnti-CTLA-4 (ipilimumab) 27593.703.70.314
726997480MelanomaallAnti-PD-1 (pembrolizumab and nivolumab)21170001
826997480MelanomaMAPKiAnti-PD-1 (pembrolizumab and nivolumab)860001
926997480Melanomanon-MAPKiAnti-PD-1 (pembrolizumab and nivolumab)13110001
1028552987Urothelial cancerallAnti-PD-L1 (atezolizumab) 9160001
1128552987Urothelial cancersmokingAnti-PD-L1 (atezolizumab) 590001
1228552987Urothelial cancernon-smokingAnti-PD-L1 (atezolizumab) 470001
1329033130MelanomaallAnti-PD-1 (nivolumab) 38270001
1429033130MelanomaNIV3-PROGAnti-PD-1 (nivolumab) 22130001
1529033130MelanomaNIV3-NAIVEAnti-PD-1 (nivolumab) 16140001
1629301960Clear cell renal cell carcinoma (ccRCC)allAnti-PD-1 (nivolumab) 11130001
1729301960Clear cell renal cell carcinoma (ccRCC)VEGFRiAnti-PD-1 (nivolumab) 610001
1829301960Clear cell renal cell carcinoma (ccRCC)non-VEGFRiAnti-PD-1 (nivolumab) 5120001
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Relations between abundance of tumor-infiltrating lymphocytes (TILs) and expression, copy number, methylation, or mutation of GPER1. The immune-related signatures of 28 TIL types from Charoentong's study, which can be viewed in the download page. For each cancer type, the relative abundance of TILs were inferred by using gene set variation analysis (GSVA) based on gene expression profile. In this tab, users can examine which kinds of TILs might be regulated by the current gene.
> Lymphocyte
 
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Relations between three kinds of immunomodulators and expression, copy number, methylation, or mutation of GPER1. These immunomo-dulators were collected from Charoentong's study. In this tab, users can examine which immunomodulators might be regulated by GPER1.
> Immunoinhibitor
> Immunostimulator
> MHC molecule
> Immunoinhibitor
 
> Immunostimulator
 
> MHC molecule
 
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Relations between chemokines (or receptors) and expression, copy number, methylation, or mutation of GPER1. In this tab, users can examine which chemokines (or receptors) might be regulated by the current gene.
> Chemokine
> Receptor
> Chemokine
 
> Receptor
 
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Distribution of GPER1 expression across immune and molecular subtypes.
> Immune subtype
> Molecular subtype
> Immune subtype
 
> Molecular subtype
 
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Associations between GPER1 and clinical features.
> Overall survival analysis
> Cancer stage
> Tumor grade
> Overall survival
 
> Stage
 
> Grade
 
Summary
SymbolGPER1
NameG protein-coupled estrogen receptor 1
Aliases FEG-1; GPCR-Br; LERGU; LERGU2; DRY12; LyGPR; CEPR; CMKRL2; GPR30; GPER; G protein-coupled receptor 30; IL8-r ......
Chromosomal Location7p22
External Links HGNC, NCBI, Ensembl, Uniprot, GeneCards
Content Drugs targeting GPER1 collected from DrugBank database.
> Drugs from DrugBank database
 

  Details on drugs targeting GPER1.
ID Name Drug Type Targets #Targets
DB00783EstradiolSmall MoleculeBECN1, CHRNA4, ESR1, ESR2, ESRRG, GPER1, HSD17B2, MT-ATP6, NCOA2, ......10
DB01645GenisteinSmall MoleculeAKT1, CYP1B1, ESR1, ESR2, ESRRA, ESRRB, GPER1, NCOA1, NCOA2, NR1I2 ......13
DB05939MK-0354Small MoleculeGPER11
DB13952Estradiol acetateSmall MoleculeBECN1, CHRNA4, ESR1, ESR2, ESRRG, GPER1, HSD17B2, MT-ATP6, NCOA2, ......10
DB13953Estradiol benzoateSmall MoleculeBECN1, CHRNA4, ESR1, ESR2, ESRRG, GPER1, HSD17B2, MT-ATP6, NCOA2, ......10
DB13954Estradiol cypionateSmall MoleculeBECN1, CHRNA4, ESR1, ESR2, ESRRG, GPER1, HSD17B2, MT-ATP6, NCOA2, ......10
DB13955Estradiol dienanthateSmall MoleculeBECN1, CHRNA4, ESR1, ESR2, ESRRG, GPER1, HSD17B2, MT-ATP6, NCOA2, ......10
DB13956Estradiol valerateSmall MoleculeBECN1, CHRNA4, ESR1, ESR2, ESRRG, GPER1, HSD17B2, MT-ATP6, NCOA2, ......10