MAATTPAQDVGVEIYLGPVWPAPSNSTPLALNLSLALREDAPGNLTGDLSEHQQYVIALF LSCLYTIFLFPIGFVGNILILVVNISFREKMTIPDLYFINLAAADLILVADSLIEVFNLD EQYYDIAVLCTFMSLFLQINMYSSVFFLTWMSFDRYLALAKAMRCGLFRTKHHARLSCGL IWMASVSATLVPFTAVHLRHTEEACFCFADVREVQWLEVTLGFIVPFAIIGLCYSLIVRA LIRAHRHRGLRPRRQKALRMIFAVVLVFFICWLPENVFISVHLLQWAQPGDTPCKQSFRH AYPLTGHIVNLAAFSNSCLSPLIYSFLGETFRDKLRLYVAQKTSLPALNRFCHATLKAVI PDSTEQSDVKFSSAV
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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
The results suggest that GPR30 activation inhibits myocardial fibrosis in diabetic ovariectomy female rats by suppressing cardiac iNOS activity and consequently nitric oxide levels.PMID:30227089
These present data have shown for the first time that total mRNA isolation and protein expression from both adipose tissues (abdominal and subcutaneous) of rat in obesity condition yield significative statistical difference among the control versus obese groups, showing that the diet high in carbohydrates modifies the total presence of mRNA and protein level expression of the receptors GPR41, 43 and 120PMID:29369009
This study aims to evaluate the potential role of GPER in coronary circulation in female and male rats.PMID:28733475
Results indicate that although administration of a GPR30 antagonist( G-15) reduced overall levels of sexual incentive motivation in male rats, sexual experience counteracted the effects of G-15 on sexual preference. Importantly, neither G-15 treatment nor sexual experience reduced overall sociosexual interest, initial exploratory behavior, or locomotor activity.PMID:28472669
GPR30 contributed to the development of BCP by both facilitating excitatory transmission and inhibiting inhibitory transmission in the spinal cord. Our findings provide the new spinal disinhibition and sensitivity mechanisms underlying the development of bone cancer pain.PMID:27608844
The cardiac electrogenic sodium/bicarbonate cotransporter (NBCe1) is activated by aldosterone through the G protein-coupled receptor 30PMID:27249584
Gper1 is up regulation regulates vascular remodeling in rats.PMID:27698063
ERalpha and GPER1 are localized exclusively to extranuclear sites in the striatum, and approximately 35% of the dendrites and axon terminals labeled for these receptors contain GABA immunoreactivity.PMID:27080432
We found that the GPER-1 agonist could significantly decrease immunoglobulin G (IgG) extravasation and increase the levels of tight junctions (occludin and claudin-5) in the CA1 at 24 h of reperfusion after GCI. Further, protein levels of vascular endothelial growth factor A (VEGF-A) was significantly decreased in the ischemic CA1 by G1. Our results suggest that GPER-1 activation reduce tight junctions disruption via inhiPMID:27311857
This study aimed to observe the possible protective effect of GPER on early-onset cognitive impairment after a single traumatic brain injury (TBI) and investigate the cellular mechanism underlying its actions. It was found that selective GPER agonist G-1 significantly reduced hippocampal CA1 neuronal loss and improved cognitive impairment in TBI rats.PMID:27908726
GPR30 activation reverses adverse effects of ovariectomy on exercise capacity in rats. GPR30 activation prevents Ovariectomy-related reductions in peak twitch in soleus muscle.PMID:27173878
Data suggest that expression of Gper1/Gpr30 can be up-regulated by dietary factors; dietary supplementation with flaxseed-derived lignan, secoisolariciresinol diglycoside, up-regulates expression of Gper1/Gpr30 in prostate and may prevent progression of benign prostatic hyperplasia.PMID:27849354
prunetin promotes osteoinduction in vivo and the mechanism is defined by signaling through GPR30 resulting in the up-regulation of the key osteogenic gene Runx2 that in turn up-regulates GPR30PMID:26345541
G-protein coupled estrogen receptor (GPER) agonist mimicked the effects of estradiol in enhancing mitochondrial function and biogenesis, whereas GPER inhibitor neutralized them.PMID:26628039
Osteoprotective effect of combination therapy of low-dose oestradiol with G15, a specific antagonist of GPR30/GPER in ovariectomy-induced osteoporotic rats.PMID:26181370
Activation of GPER results in inhibition of cardiomyocyte apoptosis and cardioprotection.PMID:25936661
GPER expression was increased in the aorta of pregnant versus virgin rats.PMID:26408543
GPR30 is expressed in rat cardiac fibroblasts.PMID:25893735
activation of GPR30 protected bones against osteoporosis in OVX rats and exerted no untoward effect on the uterusPMID:26187146
A novel form of synaptic plasticity in field CA3 of hippocampus requires GPER1 activation and BDNF release.PMID:26391661
GPR30 mediates the effects of nonylphenol on cardiac l-type calcium channels at lower but not higher concentrations.PMID:26070386
Data suggest that oestradiol improves ventricular remodelling by both G-protein coupled oestrogen receptor (GPER)- and membrane-bound oestrogen receptor-alpha-dependent mechanism.PMID:25256868
in rat aortic endothelial cells, E2-mediated endothelial effects are predominantly driven by ER and not by GPER.PMID:25150623
The results of this study conclude that local GPR30 agonists produce persistent mechanical hyperalgesia in naive female rats.PMID:25280432
By acting through GPR41 and 43, butyrate enhanced intracellular free cytosolic Ca2+. Gene-specific silencing of these receptors led to a partial inhibition of the butyrate-induced intracellular Ca2+ rise resulting in a decrease of hGH secretion.PMID:25310566
GPR30 decreases cardiac chymase/angiotensin II by inhibiting local mast cell number after estrogen loss.PMID:25712524
Our results indicate that activation of GPER-1 lowers testosterone levels in the rat and human testis.PMID:24736568
GPER is crucial in modulating glomerular mesangial cell function including extracellular matrix production and migration.PMID:24793639
GPR30 participates in mediating estrogen-2 rapid signaling and neuroprotection in the hippocampus following global cerebral ischemia.PMID:24594140
2-methoxyestradiol down-regulation of angiotensin AT1 receptor is dependent on endoplasmic reticulum membrane-associated GRP30.PMID:24262995
Activation of GPR30-AC-PKA is a key factor in the alteration of canalicular transporter function and localization induced by E17G.PMID:24115158
Activation of G protein-coupled estrogen receptor 1 confers protection after traumatic brain injury.PMID:23659385
GPER mediates cardiotropic effects in spontaneously hypertensive rat hearts.PMID:23950890
Rat R2C tumor cells express GPER and its activation is associated with decreased cell proliferation and initiation of apoptosis.PMID:23907461
GPR30 acts as a rapid transducer in the brain in response to estrogen level changes over the estrous cycle.PMID:22378360
Alterations in GPR30 expression and signaling may contribute to vascular dysfunction in aging females and a greater blood pressure in hypertensive males.PMID:23673155
Results suggest that estrogen regulates P2X3-mediated peripheral pain by acting on ERalpha and GPR30 receptors expressed in primary afferent neurons, which probably involves the intracellular cAMP-PKA-ERK1/2 pathway.PMID:23610132
data support an important role of GPER activation in aldosterone-mediated regulation of endothelial cell growth, as well as in aldosterone's endothelium-mediated regulation of vasoreactivity.PMID:23283935
GPR30 can play an important role in mediating the effects of estradiol on spatial learning, possibly by mediating estradiol effects on basal forebrain cholinergic function.PMID:22828404
Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3PMID:23066016
GPR30 is necessary for estradiol-induced changes in the 5-HT(1A) receptor signaling pathway and desensitization of 5-HT(1A) receptor signaling.PMID:22265196
Data show that the GPR30 agonist G-1 mitigates the adverse effects of oestrogen loss on LV remodelling and the development of diastolic dysfunction in oophorectomized mRen2 Lew rats.PMID:22328091
These results indicate that GPR30 is expressed and functional in rat myometrium. GPR30 activation produces depolarization, elevates [Ca2+]i and increases contractility in myometrial cells.PMID:21865584
The renoprotective actions of GPR30 may involve attenuation of tubular oxidative stress and activation of megalin-mediated protein reabsorption.PMID:21844484
Report expression of GPR30 in the serous and granular epithelial cells of submaxillary gland.PMID:21365775
GPR30 is expressed by cholinergic neurons in the basal forebrain, and activation of GPR30 enhances cholinergic function in the hippocampus similar to Estradiol.PMID:20696528
these findings would suggest that aldosterone is the predominant mediator of GPR30 activation in vascular cells.PMID:21242460
G protein-coupled estrogen receptor 1 may mediate actions important for Sertoli cell function and maintenance of normal testis development and homeostasisPMID:20445128
Investigated both mRNA and protein expression of GPER in the rat and human heart. The role of GPER in estrogen protection against ischaemic stress in the rat heart was also assessed.PMID:20596598
activation of GPR30 protects cardiac function and decreases myocardial inflammation after global ischemia/reperfusionPMID:20434187
Expressed in the brain. Expressed in neurons of the hippocampus, hypothalamic paraventricular nucleus (PVN), supraoptic nucleus (SON) and the median eminence. Expressed in magnocellular neurosecretory cells (MNCs) which secrete oxytocin but not in MNCs wh