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  4. Recombinant Human Free fatty acid receptor 2 (FFAR2)

Recombinant Human Free fatty acid receptor 2 (FFAR2)

  • 货号：
    CSB-CF008605HU
  • 规格：
  • 来源：
    in vitro E.coli expression system
  • 其他：

产品详情

  • 基因名：
  • Uniprot No.：
  • 别名：
    FFAR2; FFA2; GPCR43; GPR43; Free fatty acid receptor 2; G-protein coupled receptor 43
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Full length protein
  • 表达区域：
    1-330
  • 氨基酸序列
    MLPDWKSSLILMAYIIIFLTGLPANLLALRAFVGRIRQPQPAPVHILLLSLTLADLLLLL LLPFKIIEAASNFRWYLPKVVCALTSFGFYSSIYCSTWLLAGISIERYLGVAFPVQYKLS RRPLYGVIAALVAWVMSFGHCTIVIIVQYLNTTEQVRSGNEITCYENFTDNQLDVVLPVR LELCLVLFFIPMAVTIFCYWRFVWIMLSQPLVGAQRRRRAVGLAVVTLLNFLVCFGPYNV SHLVGYHQRKSPWWRSIAVVFSSLNASLDPLLFYFSSSVVRRAFGRGLQVLRNQGSSLLG RRGKDTAEGTNEDRGVGQGEGMPSSDFTTE
    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 receptor that is activated by a major product of dietary fiber digestion, the short chain fatty acids (SCFAs), and that plays a role in the regulation of whole-body energy homeostasis and in intestinal immunity. In omnivorous mammals, the short chain fatty acids acetate, propionate and butyrate are produced primarily by the gut microbiome that metabolizes dietary fibers. SCFAs serve as a source of energy but also act as signaling molecules. That G protein-coupled receptor is probably coupled to the pertussis toxin-sensitive, G(i/o)-alpha family of G proteins but also to the Gq family. Its activation results in the formation of inositol 1,4,5-trisphosphate, the mobilization of intracellular calcium, the phosphorylation of the MAPK3/ERK1 and MAPK1/ERK2 kinases and the inhibition of intracellular cAMP accumulation. May play a role in glucose homeostasis by regulating the secretion of GLP-1, in response to short-chain fatty acids accumulating in the intestine. May also regulate the production of LEP/Leptin, a hormone acting on the central nervous system to inhibit food intake. Finally, may also regulate whole-body energy homeostasis through adipogenesis regulating both differentiation and lipid storage of adipocytes. In parallel to its role in energy homeostasis, may also mediate the activation of the inflammatory and immune responses by SCFA in the intestine, regulating the rapid production of chemokines and cytokines. May also play a role in the resolution of the inflammatory response and control chemotaxis in neutrophils. In addition to SCFAs, may also be activated by the extracellular lectin FCN1 in a process leading to activation of monocytes and inducing the secretion of interleukin-8/IL-8 in response to the presence of microbes. Among SCFAs, the fatty acids containing less than 6 carbons, the most potent activators are probably acetate, propionate and butyrate. Exhibits a SCFA-independent constitutive G protein-coupled receptor activity.
  • 基因功能参考文献：
    1. Data suggest that the free fatty acid receptor 2 (FFA2/GPR43 receptor) plays an integral role in survival during and after sepsis. PMID: 29338778
    2. we show functional similarities but also some important differences between GPR84 and FFA2R in human phagocytes, thus providing some mechanistic insights into GPR84 regulation in blood neutrophils and cells recruited to an aseptic inflammatory site in vivo. PMID: 29477577
    3. Compared with the control group, the densitometric quantification and mean density of GPR43 and ChAT proteins, and expression of GPR43 and CHAT genes, were significantly decreased in the patients with mixed refractory constipation. PMID: 26921846
    4. FFA2 processes mediated by Gi signaling, whereas, in concert with blockade by the Gq/G11 inhibitor FR900359, the inability of AZ1729 to mimic or regulate propionate-mediated release of GLP-1 from mouse colonic preparations defined this physiological response as an end point transduced via activation of Gq/G11. PMID: 27385588
    5. the results of mutagenesis studies based on the crystal structure of hFFA1 bound to TAK-875 at 2.3 A resolution to identify important residues for orthosteric agonist 6e inducing FFA2 activation. PMID: 26808470
    6. Although both agonist and antagonist ligands contain negatively charged carboxylates that interact with two key positively charged arginine residues in transmembrane domains V and VII of FFA2, there are clear differences in how these interactions occur. PMID: 26518871
    7. FFAR2 signaling occurs by divergent G protein pathways. PMID: 26075576
    8. GPR3 agonism potentiates insulin secretion in isolated islets. PMID: 26023106
    9. GPR43 expression is reduced in monocytes upon siRNA-knockdown of XBP1, while A549 cells overexpressing XBP1 displayed elevated GPR43 levels. PMID: 25633224
    10. FFAR2 is a potential therapeutic target of T1 diabetes, representing a link between immune response and glucose homeostasis. PMID: 25298143
    11. FFAR2 is expressed in pancreatic beta cells and mediates an inhibition of insulin secretion by coupling to Gi-type G proteins. PMID: 25581519
    12. [review] In vivo and in vitro studies suggest that short-chain fatty acid receptors (SCFAs) stimulate gut hormone secretion; therefore, the SCFA-FFA signal is likely to be important for gut physiological functions. PMID: 24458110
    13. GPR43 modulates NF-kappaB activity via beta-arrestin 2. PMID: 23985900
    14. Data indicate that a single mutation in human FFA2 of C4.57G resulted in a human FFA2 receptor with ligand selectivity similar to the bovine receptor. PMID: 22919070
    15. They report the results of mutagenesis studies on the receptor, and the identification of previous unknown residues that may affect receptor activation as well as residues important for allosteric interactions on FFA2. PMID: 21216233
    16. Reduction of GPR43 expression is associated with colon cancers. PMID: 20979106
    17. Collaboration among C-reactive protein, M-ficolin, and GPR43 under acidosis curtails interleukin (IL)-8 production, thus preventing immune overactivation during bacterial infection. PMID: 21037097
    18. Mutational analysis revealed several important residues located in transmembrane domains 3, 4, 5, 6, and 7 for acetate binding. PMID: 20837008
    19. upregulation of FFAR2 expression may contribute to malignant transformation. PMID: 19780758
    20. might play pivotal role in differentiation and immune response of monocytes and granulocytes PMID: 12393494
    21. FFA2R is expressed on leukocytes and activated by short-chain fatty acids. PMID: 12684041
    22. the highly selective expression of GPR43 in leukocytes, particularly polymorphonuclear cells, suggests a role in the recruitment of these cell populations toward sites of bacterial infection PMID: 12711604
    23. Results indicate that the short chain fatty acid receptor, GPR43 is expressed by enteroendocrine L cells containing peptide YY in the human large intestine. PMID: 17899402

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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：
    Expressed at relatively high levels in peripheral blood leukocytes and, to lesser extent, in spleen.
  • 数据库链接：

    HGNC: 4501

    OMIM: 603823

    KEGG: hsa:2867

    STRING: 9606.ENSP00000246549

    UniGene: Hs.248056