MDATTPAQTVGVEIYLGPVWPAPSNSTPLALNLSLALREDAPGNLTGDLSEHQQYVIALF LSCLYTIFLFPIGFVGNILILVVNISFREKMTIPDLYFINLAAADLILVADSLIEVFNLD EQYYDIAVLCTFMSLFLQINMYSSVFFLTWMSFDRYLALAKAMRCGLFRTKHHARLSCGL IWMASVSATLVPFTAVHLRHTEEACFCFADVREVQWLEVTLGFIMPFAIIGLCYSLIVRA LIRAHRHRGLRPRRQKALRMIFAVVLVFFICWLPENVFISVHLLQWTQPGDTPCKQSFRH AYPLTGHIVNLAAFSNSCLNPLIYSFLGETFRDKLRLYVEQKTSLPALNRFCHATLKAVI PDSTEQSEVRFSSAV
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sequence may include tag sequence, target protein sequence, linker sequence and extra sequence that is
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Protein Length
full length protein
Tag Info
N-terminal 10xHis-tagged
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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 References into Functions
Gene Set Enrichment Analysis (GSEA) revealed that mitochondrial genes are enriched in GPER KO females, whereas inflammatory response genes are enriched in GPER KO males, compared to their wild type counterparts of the same sex. The cardiomyocyte-specific GPER KO mouse model provides us with a powerful tool to study the functions of GPER in cardiomyocytes.PMID:27725247
For the first time, we report here the importance of GPER-PPARalpha and -PPARgamma 'neopartnership' in maintenance of Leydig cell morpho-functional status.PMID:30149370
In murine osteoblasts cultured in vitro, treatment with 17beta-estradiol resulted in the expression of GPR30 and enhanced mitophagy through the GPR30 and ERK1/2 signaling pathway.PMID:29438359
findings provide evidence for the first time that GPR30 promotes adipogenesis and therefore the development of obesity in female mice exposed to excess fat energyPMID:27698362
Study demonstrates that selective activation of G protein-coupled estrogen receptor can control microglial activation induced by an inflammatory stimulus in vitro, and promote neuronal and functional protection of DA neurons against a unilateral intranigral injection of LPS in male mice.neuroinflammatory diseases.PMID:28450223
it suppresses lipopolysaccharide-induced interleukin 6 via inhibition of nuclear factor-kappa B pathway in murine macrophage cellsPMID:28722236
this study revealed a role for GPER activity in regulating Nox1 abundance and associated O2(-)-mediated structural and functional damage that contributes to disease pathologyPMID:27803283
These findings provide strong evidence for aldosterone serving a causal role in renal cell cancer regulation via its GPER receptor; thus, antagonism of GPER represents a potential new target for treatment to reduce metastatic spread.PMID:26911792
GPER protects against hepatic tumorigenesis by regulating inflammatory responses.PMID:27594673
Data suggest that prenatal exposure to p,p'-DDT (an endocrine disrupting pesticide) causes sex- and age-independent attenuation of Gper1 in brain which appears to play key role in propagation of DDT-induced depressive-like neurotoxicity.PMID:28263910
Study suggested that the neuroprotective effect of estrogen requires intact GPER1-associated signaling in an in vitro model of ischemia. The membrane-associated signaling mediates the estrogen actions, and depends on PI3K/Akt signaling for Ask1 inhibition that prevents the cell death triggered by ischemia. These mechanisms may help for a therapeutic strategy to target on GPER1 for the treatment of neurological disorders.PMID:27113328
Phosphorylation of myosin regulatory light chain triggered by E2 was found to be mediated by estrogen receptor-beta and the G protein-coupled estrogen receptor.PMID:26956186
Our study demonstrated the ameliorative role of GPR30 in NOR memory impaired by AD pathology in female micePMID:27423484
identified a novel regulatory mechanism through which the endogenous Gper facilitates the age-dependent increase in myocardial expression of ECE-2 and the ETB receptor, which is compatible with an activating role of GPER for the local endothelin system with agingPMID:26880534
We suggest that activation of GPER exerts an inhibitory effect on colonic motility by promoting nitric oxide release from myenteric nitrergic nervesPMID:26661936
GPR30 is expressed in diverse intracellular compartments in undifferentiated and differentiated C2C12 cells and mediates estradiol actions.PMID:26359786
Results demonstrate that ERalpha, ERbeta, and GPER1 all participate in the rapid effects of 17beta-estradiol-3-benzoate on hippocampal synaptic functionPMID:25980457
GPR30 can mediate the fast effect of estrogen on blastocysts and play an important role in embryo implantation.PMID:25820689
the pharmacology and signalling properties of GPER1 in an immortalized embryonic hippocampal cell line, are reported.PMID:26998610
E2 activates GPR30 and ERa to produce liquid crystalline versus anhydrous crystalline metastable intermediates evolving to cholesterol monohydrate crystals . GPR30 produces a synergistic lithogenic action with ERa to enhance E2-induced gallstone formationPMID:26152119
These data indicate that estrogen-Gper1 acute coupling plays a key role in cardioprotection against ischemia/reperfusion injury.PMID:26356837
Suggest that the effects of diethylstilbestrol on mouse gubernaculum testis cells are mediated at least partially by the regulation of GPER expression.PMID:26261617
The stimulating effect of estradiol on progesterone synthesis relies on the estrogen no-classical protein-coupled receptor 30, and MAP3K8.PMID:25763610
Results suggest that ERalpha requires GPER1 in protection of dopamine neurons and modulation of signaling pathways, and that the effect of GPER1 occurs independently of ERalpha/beta, whereas GPER1 require ERalpha/beta to increase BDNF levelsPMID:25892506
Treatment with 17beta-estradiol is renoprotective after whole-body ischemia-reperfusion in ovariectomized female mice irrespective of GPR30 gene deletion.PMID:24923556
Data (including data from studies in knockout mice) suggest that, under proinflammatory conditions, estrogen inhibits vasoconstrictor prostanoid production in vascular endothelium and inhibits activity of prostanoids in intact arteries through Gper1.PMID:26303299
GPR30 activation induced anxiolytic effects but did not affect the nociceptive threshold of mice under chronic pain. The anxiolytic effects of GPR30 were partially due to Glur1 upregulation and GABA-A receptor downregulation in the basolateral amygdala.PMID:25614360
GPER1 is involved in anxiety and stress control.PMID:25236887
this study reveals an atheroprotective function of GPER and introduces selective GPER activation as a novel therapeutic approach to inhibit postmenopausal atherosclerosis and inflammation in the absence of uterotrophic activity.PMID:25532911
Study demonstrates that activation of GPR30 stimulates social behavior in a rodent model in a manner similar to 17beta-estradiol benzoatePMID:25012534
This is the first description of a role for the novel estrogen receptor GPER in breast tumorigenesis and metastasis.PMID:25030371
role in breast cancer cell adhesion and growthPMID:25096985
GPER1 is regulated by insulin in cancer cells and cancer-associated fibroblastsPMID:25012984
estrogen's actions via GPER1 may converge on the same synaptic elements, different pathways are used to achieve these actionsPMID:25673833
This study demonstrates that stimulation of AhR-signaling and impairment of GPR30-signaling play important roles in the propagation of dichlorodiphenyltrichloroethane-induced apoptosis during the early stages of neural development.PMID:24859647
GPER-1 expression is modulated during the estrus cycle which may suggest a physiological role for GPER-1 in the kidney during reproduction.PMID:24239983
A potential role of Gpr30 in preserving lipid metabolism and cardiac function in a sex- and age-dependent fashion.PMID:24582972
Activation of ERK1/2 through GPR30 and ERalpha/beta is involved in low dose bisphenol A promotion of Sertoli cell proliferation.PMID:24495410
G-protein-coupled receptor 30 interacts with receptor activity-modifying protein 3 and confers sex-dependent cardioprotection.PMID:23674134
This study demonstrates for the first time that in male mice, GPER regulates metabolic parameters associated with obesity and diabetes.PMID:23970785
GPER expression is elevated in the ischemic hemisphere of male, but not female, mice who have undergone experimental stroke. Moreover, GPER mRNA expression in males was elevated at 4 h but had returned to baseline by 24 h.PMID:22869326
GPER participates in the control of hippocampal neuritogenesis by a mechanism involving the activation of PI3K signaling.PMID:23545157
The changes of expression of GPER (GPR30) on mouse oocytes plasma membrane confirm oocyte membrane maturation, suggesting that those changes of GPER may be related to the functional role of oocyte maturationPMID:23420106
Results showed an important role of GPER1 in neuroprotection in a mouse model of Parkinson disease. Activation of GPER1 led to an increase in striatal dopamine metabolite concentrations as well as the turnover of dopamine.PMID:22749492
endogenous GPER inhibits ET-1-induced vasoconstriction, an effect that may be associated with reduced vascular smooth muscle cell calcium sensitivityPMID:22326502
Our data suggest that GPR30 induces acute anxiogenic effects of oestrogen in rodentsPMID:22143579
Fast neuroprotection by estradiol is partially mediated by GPR30 and the subsequent downregulation of N-methyl D-aspartate receptor NR2B-containing NMDARs.PMID:22492045
GPER is the first estrogen receptor with inhibitory activity on endothelium-dependent contractility.PMID:22203741
The GPR30 agonist, G1, and E2 attenuated apoptosis induced by H(2)O(2) exposure.PMID:21645039
Activation of the G-protein coupled estrogen receptor (GPER) in Th17 cells induces the production and secretion of IL-10 by these cells.PMID:21722102
Expressed in brain, heart, spleen, preadipocytes, mature adipocytes and primary hippocampal neurons. Expressed in neurons of the hippocampus, hypothalamic paraventricular nucleus (PVH), supraoptic nucleus (SON) and the median eminence. Expressed in the nu