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  4. Recombinant Human G-protein coupled bile acid receptor 1 (GPBAR1), partial

Recombinant Human G-protein coupled bile acid receptor 1 (GPBAR1), partial

  • 货号：
    CSB-YP819471HU1
  • 规格：
  • 来源：
    Yeast
  • 其他：
  • 货号：
    CSB-EP819471HU1-B
  • 规格：
  • 来源：
    E.coli
  • 共轭：
    Avi-tag Biotinylated

    E. coli biotin ligase (BirA) is highly specific in covalently attaching biotin to the 15 amino acid AviTag peptide. This recombinant protein was biotinylated in vivo by AviTag-BirA technology, which method is BriA catalyzes amide linkage between the biotin and the specific lysine of the AviTag.

  • 其他：
  • 货号：
    CSB-BP819471HU1
  • 规格：
  • 来源：
    Baculovirus
  • 其他：
  • 货号：
    CSB-MP819471HU1
  • 规格：
  • 来源：
    Mammalian cell
  • 其他：

产品详情

  • 纯度：
    >85% (SDS-PAGE)
  • 基因名：
  • Uniprot No.：
  • 别名：
    GPBAR1; TGR5; G-protein coupled bile acid receptor 1; G-protein coupled receptor GPCR19; hGPCR19; Membrane-type receptor for bile acids; M-BAR; hBG37; BG37
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Partial
  • 蛋白标签：
    Tag type will be determined during the manufacturing process.
    The tag type will be determined during production process. If you have specified tag type, please tell us and we will develop the specified tag preferentially.
  • 产品提供形式：
    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.
  • 复溶：
    We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20℃/-80℃. Our default final concentration of glycerol is 50%. Customers could use it as reference.
  • 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：
    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 ：
    Please contact us to get it.

产品评价

靶点详情

  • 功能：
    Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids.
  • 基因功能参考文献：
    1. Activation of FXR inhibits, whereas TGR5 activation may promote, cholangiocarcinoma progression by regulating proliferation, migration and mitochondrial energy metabolism. PMID: 28916388
    2. RYGB increased circulating bile acids, ileal Takeda G protein-coupled receptor 5 (TGR5) and mTORC1 signaling activity, as well as GLP-1 production in both mice and human subjects. Inhibition of ileal mTORC1 signaling by rapamycin significantly attenuated the stimulation of bile acid secretion, TGR5 expression and GLP-1 synthesis induced by RYGB in lean and diet-induced obese mice. PMID: 29859856
    3. TGR5 is strongly expressed in collecting ducts, distal convoluted tubules and thin loop of Henle. TGR5 protein and mRNA expression were notably decreased in clear cell renal cell carcinomas and may be helpful in differentiating these tumors from other renal cell carcinomas. PMID: 29606134
    4. The findings suggest that activation of TGR5 promoted mitochondrial biogenesis in endothelial cells, which is mediated by the CREB/PGC-1a signaling pathway. PMID: 29709472
    5. Higher-order oligomers, likely with a tetramer organization, are formed from dimers, the smallest unit suggested for TGR5 Y111A variants. PMID: 27833095
    6. Data suggest that TGR5 and FXR in intestinal mucosa are important for glucose homeostasis, in particular in metabolic disorders such as type 2 diabetes and obesity. (TGR5 = membrane-type receptor for bile acids TGR5; FXR = farnesoid X receptor) [REVIEW; Congress as Topic] PMID: 27846919
    7. GPBAR1 is expressed in advanced gastric cancers and its expression correlates with markers of epithelial-mesenchymal transition PMID: 27409173
    8. TGR5 activation induces mitochondrial biogenesis and prevents renal oxidative stress and lipid accumulation, establishing a role for TGR5 in inhibiting Kidney Disease in Obesity and Diabetes Mellitus. PMID: 27045028
    9. TGR5 exhibits significantly higher expression in NSCLC tumor samples and facilitates the growth and metastasis of NSCLC by activating the JAK2/STAT3 signaling pathway. PMID: 29074425
    10. TGR5 may have a role in the progression from Barrett's Esophagus to high-grade dysplasia and esophageal adenocarcinoma PMID: 28293080
    11. contributes to hepatic cystogenesis by increasing cAMP and enhancing cholangiocyte proliferation PMID: 28543567
    12. anti-inflammation therapy targeting Gpbar1/NF-kappaB pathway could be effective in suppressing bile acid-induced inflammation and alleviating Intrahepatic cholestasis of pregnancy-associated fetal disorders. PMID: 27402811
    13. human TGR5 (hTGR5) shows higher nomilin responsiveness than does mouse TGR5. PMID: 28594916
    14. bile acids promote intestinal epithelial cell proliferation and decrease mucosal injury by upregulating TGR5 expression in obstructive jaundice. PMID: 28034761
    15. The generated contour maps revealed the important structural insights for the activity of the compounds. The results obtained from this study could be helpful in the development of novel and more potent agonists of TGR5. PMID: 27267434
    16. TGR5 functions as a tumor-suppressor in patients with ampullary adenocarcinoma and preoperative hyperbilirubinemia PMID: 27510297
    17. We conclude that Claudin-2 expression is significantly associated with bile acid receptors VDR and TGR5 expression. Our studies identify a novel role of a tight junction protein in the development and progression of esophageal mucosal metaplasia, dysplasia and carcinoma. PMID: 28212604
    18. this is the first report of bile acid derivatives able to antagonize GPBAR1 and and farnesoid X receptor (FXR) modulatory activity. PMID: 26607331
    19. These findings identify TGR5 as a suppressor of gastric cancer cell proliferation and migration PMID: 26417930
    20. Because elevated levels of circulatory LPS may contribute to the development of insulin resistance, the results from this study suggest that bile acids through the activation of TGR5 may have a role in the development of insulin resistance as well. PMID: 25418122
    21. TGR5 is a mediator of bile acid-induced cholangiocyte proliferation and protects cholangiocytes from apoptosis but may trigger proliferation and apoptosis resistance in malignantly transformed cholangiocytes, promoting cholangiocarcinoma. PMID: 26420419
    22. Collectively, these data suggest the involvement of TGR5 in PLD and that TGR5 targeting in cystic cholangiocytes may have therapeutic potential. PMID: 26045278
    23. GPBAR1 plays a role in secondary bile acid induced vasodilation via reglation of cystathionine gamma-lyase. The GPBAR1/CSE pathway might contribute to endothelial dysfunction and hyperdynamic circulation in liver cirrhosis. PMID: 25934094
    24. Study demonstrates that highly lipophilic 3-epi-betulinic acid derivatives can be potent and selective TGR5 agonists with improved cellular efficacy. PMID: 25283506
    25. GPBAR1 SNP is associated with symptoms and pathobiology in IBS-D and IBS-C. PMID: 25012842
    26. Our findings strongly suggested the combination of serum TGR5 promoter methylation and AFP enhanced the diagnostic value of AFP alone in discriminating HCC from CHB patients. PMID: 24465162
    27. the secondary structure of the TGR5 membrane-proximal C terminus is the determining factor for plasma membrane localization and responsiveness towards extracellular ligands. PMID: 24338481
    28. Data suggest that TGR5 is expressed in 2 cell types of term placenta, macrophage/trophoblast; TGR5 expression is low in maternal cholestasis; TGR5 appears to trigger different responses to bile acid/progesterone metabolites depending on cell type. PMID: 23849932
    29. DCA, taurolithocholic acid, and oleanolic acid did not stimulate TGR5 association with beta-arrestin 1/2 or G protein-coupled receptor kinase (GRK) 2/5/6, as determined by bioluminescence resonance energy transfer PMID: 23818521
    30. TGR5 agonism induces NO production via Akt activation and intracellular Ca(2+) increase in vascular endothelial cells, and this function inhibits monocyte adhesion in response to inflammatory stimuli. PMID: 23619297
    31. Human adipose tissue TGR5 expression is positively correlated to obesity and reduced during diet-induced weight loss. PMID: 23523790
    32. TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease. PMID: 23566200
    33. TGR5 is overexpressed in most gastric intestinal-type adenocarcinomas, and moderate to strong TGR5 staining is associated with decreased patient survival in all gastric adenocarcinomas. PMID: 23238937
    34. this study demonstrates that the TGR5 expressed in the pancreatic beta cells regulates insulin secretion and highlights the importance of ongoing therapeutic strategies targeting TGR5 in the control of glucose homeostasis. PMID: 23022524
    35. the mechanisms of metabolic regulation by FXR and TGR5 PMID: 22550135
    36. These results indicate that bile acids induce the differentiation of IL-12 hypo-producing dendritic cells from monocytes via the TGR5-cAMP pathway. PMID: 22236403
    37. Data suggest that variation in bile acid receptor TGR5 may contribute to altered small bowel transit and colonic transit in lower functional gastrointestinal disorders. PMID: 21883702
    38. TGR5 is a key factor in energy expenditure by regulating metabolism. PMID: 21754919
    39. The current knowledge on BA receptors is reviewed, with a strong focus on the cell membrane receptor TGR5, which has emerged as a promising target for intervention in metabolic diseases. PMID: 21691102
    40. The aim of the present study was to determine the localization and function of the receptor in biliary epithelial cells. PMID: 21691103
    41. The TGR5 gene is localized at chromosome 2q35, close to a genetic variant associated with both primary sclerosing cholangitis and ulcerative colitis in recent genome-wide association studies. PMID: 21691110
    42. The ability of the bile acid analogues obtained by chemical modification of ursodeoxycholic acid (UDCA) for TGR5 activation in HEK 293 cells is reported. PMID: 21212509
    43. The TGR5 is localized in the primary cilium of human cholangiocytes and the receptor could play an important role in coupling biliary bile acid concentration and composition to ductular bile formation. PMID: 20623999
    44. resequencing of TGR5 along with functional investigations of novel variants PMID: 20811628
    45. Expression of BG37 was detected in various specific tissues, suggesting its physiological role. PMID: 12419312
    46. TGR5 is implicated in the suppression of macrophage functions by bile acids PMID: 12524422
    47. Combined blockade of both epidermal growth factor receptors and GPCRs may be a rational strategy to treat cancers, including head and neck squamous cell carcinoma that shows cross-talk between GPCR and EGFR signaling pathways. PMID: 17178880
    48. These results suggest that in AGS cells, DC transactivates EGFR through M-BAR- and ADAM/HB-EGF-dependent mechanisms. PMID: 17214962
    49. This is the first report on the expression of TGR5 in sinusoidal endothelial cells. Regulation of eNOS by TGR5 connects bile salts with hepatic hemodynamics. PMID: 17326144
    50. TGR5 mediates chloride secretion via activation of CFTR. The presence of the receptor in both the plasma membrane and the recycling endosome indicate that TGR5 can be regulated by translocation. PMID: 19582812

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  • 亚细胞定位：
    Cell membrane; Multi-pass membrane protein.
  • 蛋白家族：
    G-protein coupled receptor 1 family
  • 组织特异性：
    Ubiquitously expressed. Expressed at higher level in spleen and placenta. Expressed at lower level in other tissues. In digestive tissues, it is expressed in stomach, duodenum, ileocecum, ileum, jejunum, ascending colon, transverse colon, descending colon
  • 数据库链接：

    HGNC: 19680

    OMIM: 610147

    KEGG: hsa:151306

    STRING: 9606.ENSP00000428824

    UniGene: Hs.160954