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  4. Recombinant Rat G-protein coupled estrogen receptor 1 (Gper)

Recombinant Rat G-protein coupled estrogen receptor 1 (Gper)

  • 货号：
    CSB-CF009713RA
  • 规格：
  • 来源：
    in vitro E.coli expression system
  • 其他：

产品详情

  • 基因名：
  • Uniprot No.：
  • 别名：
    Gper1; Cmkrl2; Gper; Gpr30; Gpr41; G-protein coupled estrogen receptor 1; Chemoattractant receptor-like 2; G protein-coupled estrogen receptor 1; G-protein coupled receptor 30; G-protein coupled receptor 41; Membrane estrogen receptor; mER
  • 种属：
    Rattus norvegicus (Rat)
  • 蛋白长度：
    Full length protein
  • 表达区域：
    1-375
  • 氨基酸序列
    MAATTPAQDVGVEIYLGPVWPAPSNSTPLALNLSLALREDAPGNLTGDLSEHQQYVIALF LSCLYTIFLFPIGFVGNILILVVNISFREKMTIPDLYFINLAAADLILVADSLIEVFNLD EQYYDIAVLCTFMSLFLQINMYSSVFFLTWMSFDRYLALAKAMRCGLFRTKHHARLSCGL IWMASVSATLVPFTAVHLRHTEEACFCFADVREVQWLEVTLGFIVPFAIIGLCYSLIVRA LIRAHRHRGLRPRRQKALRMIFAVVLVFFICWLPENVFISVHLLQWAQPGDTPCKQSFRH AYPLTGHIVNLAAFSNSCLSPLIYSFLGETFRDKLRLYVAQKTSLPALNRFCHATLKAVI PDSTEQSDVKFSSAV
    Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
  • 蛋白标签：
    N-terminal 10xHis-tagged
  • 产品提供形式：
    Liquid or Lyophilized powder
    Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.
  • 缓冲液：
    Lyophilized from Tris/PBS-based buffer, 6% Trehalose, pH 8.0
  • 储存条件：
    Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
  • 保质期：
    The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
    Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
  • 货期：
    Basically, we can dispatch the products out in 1-3 working days after receiving your orders. Delivery time may differ from different purchasing way or location, please kindly consult your local distributors for specific delivery time.
    Note: All of our proteins are default shipped with normal blue ice packs, if you request to ship with dry ice, please communicate with us in advance and extra fees will be charged.
  • 注意事项：
    Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.
  • Datasheet & COA：
    Please contact us to get it.

产品评价

靶点详情

  • 功能：
    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.
  • 基因功能参考文献：
    1. 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
    2. 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 120 PMID: 29369009
    3. This study aims to evaluate the potential role of GPER in coronary circulation in female and male rats. PMID: 28733475
    4. 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
    5. 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
    6. The cardiac electrogenic sodium/bicarbonate cotransporter (NBCe1) is activated by aldosterone through the G protein-coupled receptor 30 PMID: 27249584
    7. Gper1 is up regulation regulates vascular remodeling in rats. PMID: 27698063
    8. 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
    9. 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 inhi PMID: 27311857
    10. 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
    11. 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
    12. 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
    13. 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 GPR30 PMID: 26345541
    14. 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
    15. Osteoprotective effect of combination therapy of low-dose oestradiol with G15, a specific antagonist of GPR30/GPER in ovariectomy-induced osteoporotic rats. PMID: 26181370
    16. Activation of GPER results in inhibition of cardiomyocyte apoptosis and cardioprotection. PMID: 25936661
    17. GPER expression was increased in the aorta of pregnant versus virgin rats. PMID: 26408543
    18. GPR30 is expressed in rat cardiac fibroblasts. PMID: 25893735
    19. activation of GPR30 protected bones against osteoporosis in OVX rats and exerted no untoward effect on the uterus PMID: 26187146
    20. A novel form of synaptic plasticity in field CA3 of hippocampus requires GPER1 activation and BDNF release. PMID: 26391661
    21. GPR30 mediates the effects of nonylphenol on cardiac l-type calcium channels at lower but not higher concentrations. PMID: 26070386
    22. 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
    23. in rat aortic endothelial cells, E2-mediated endothelial effects are predominantly driven by ER and not by GPER. PMID: 25150623
    24. The results of this study conclude that local GPR30 agonists produce persistent mechanical hyperalgesia in naive female rats. PMID: 25280432
    25. 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
    26. GPR30 decreases cardiac chymase/angiotensin II by inhibiting local mast cell number after estrogen loss. PMID: 25712524
    27. Our results indicate that activation of GPER-1 lowers testosterone levels in the rat and human testis. PMID: 24736568
    28. GPER is crucial in modulating glomerular mesangial cell function including extracellular matrix production and migration. PMID: 24793639
    29. GPR30 participates in mediating estrogen-2 rapid signaling and neuroprotection in the hippocampus following global cerebral ischemia. PMID: 24594140
    30. 2-methoxyestradiol down-regulation of angiotensin AT1 receptor is dependent on endoplasmic reticulum membrane-associated GRP30. PMID: 24262995
    31. Activation of GPR30-AC-PKA is a key factor in the alteration of canalicular transporter function and localization induced by E17G. PMID: 24115158
    32. Activation of G protein-coupled estrogen receptor 1 confers protection after traumatic brain injury. PMID: 23659385
    33. GPER mediates cardiotropic effects in spontaneously hypertensive rat hearts. PMID: 23950890
    34. Rat R2C tumor cells express GPER and its activation is associated with decreased cell proliferation and initiation of apoptosis. PMID: 23907461
    35. GPR30 acts as a rapid transducer in the brain in response to estrogen level changes over the estrous cycle. PMID: 22378360
    36. Alterations in GPR30 expression and signaling may contribute to vascular dysfunction in aging females and a greater blood pressure in hypertensive males. PMID: 23673155
    37. 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
    38. 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
    39. 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
    40. Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3 PMID: 23066016
    41. 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
    42. 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
    43. 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
    44. The renoprotective actions of GPR30 may involve attenuation of tubular oxidative stress and activation of megalin-mediated protein reabsorption. PMID: 21844484
    45. Report expression of GPR30 in the serous and granular epithelial cells of submaxillary gland. PMID: 21365775
    46. 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
    47. these findings would suggest that aldosterone is the predominant mediator of GPR30 activation in vascular cells. PMID: 21242460
    48. G protein-coupled estrogen receptor 1 may mediate actions important for Sertoli cell function and maintenance of normal testis development and homeostasis PMID: 20445128
    49. 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
    50. activation of GPR30 protects cardiac function and decreases myocardial inflammation after global ischemia/reperfusion PMID: 20434187

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  • 亚细胞定位：
    Nucleus. Cytoplasm, perinuclear region. Cytoplasm. Cytoplasm, cytoskeleton. Cytoplasmic vesicle membrane; Multi-pass membrane protein. Cell membrane; Multi-pass membrane protein. Basolateral cell membrane; Multi-pass membrane protein. Endoplasmic reticulum membrane; Multi-pass membrane protein. Early endosome. Recycling endosome. Golgi apparatus, trans-Golgi network. Golgi apparatus membrane; Multi-pass membrane protein. Cell projection, dendrite. Cell projection, dendritic spine membrane; Multi-pass membrane protein. Cell projection, axon. Cell junction, synapse, postsynaptic density. Mitochondrion membrane; Multi-pass membrane protein.
  • 蛋白家族：
    G-protein coupled receptor 1 family
  • 组织特异性：
    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
  • 数据库链接：

    KEGG: rno:171104

    STRING: 10116.ENSRNOP00000001732

    UniGene: Rn.9806