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  4. Recombinant Human Free fatty acid receptor 1 (FFAR1)

Recombinant Human Free fatty acid receptor 1 (FFAR1)

  • 货号：
    CSB-CF008604HU
  • 规格：
  • 来源：
    in vitro E.coli expression system
  • 其他：

产品详情

  • 基因名：
  • Uniprot No.：
  • 别名：
    FFAR1; GPR40; Free fatty acid receptor 1; G-protein coupled receptor 40
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Full length protein
  • 表达区域：
    1-300
  • 氨基酸序列
    MDLPPQLSFGLYVAAFALGFPLNVLAIRGATAHARLRLTPSLVYALNLGCSDLLLTVSLP LKAVEALASGAWPLPASLCPVFAVAHFFPLYAGGGFLAALSAGRYLGAAFPLGYQAFRRP CYSWGVCAAIWALVLCHLGLVFGLEAPGGWLDHSNTSLGINTPVNGSPVCLEAWDPASAG PARFSLSLLLFFLPLAITAFCYVGCLRALARSGLTHRRKLRAAWVAGGALLTLLLCVGPY NASNVASFLYPNLGGSWRKLGLITGAWSVVLNPLVTGYLGRGPGLKTVCAARTQGGKSQK
    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 for medium and long chain saturated and unsaturated fatty acids that plays an important role in glucose homeostasis. Fatty acid binding increases glucose-stimulated insulin secretion, and may also enhance the secretion of glucagon-like peptide 1 (GLP-1). May also play a role in bone homeostasis; receptor signaling activates pathways that inhibit osteoclast differentiation. Ligand binding leads to a conformation change that triggers signaling via G-proteins that activate phospholipase C, leading to an increase of the intracellular calcium concentration. Seems to act through a G(q) and G(i)-mediated pathway. Mediates the anti-inflammatory effects of omega-3 polyunsaturated fatty acids (PUFAs) via inhibition of NLRP3 inflammasome activation.
  • 基因功能参考文献：
    1. Study reports the 2.76-A crystal structure of human GPR40 complexed with compound 1 bound in a second structurally distinct allosteric site, located at the receptor side facing the membrane lipophilic environment. Binding of compound 1 stabilizes the intracellular loop 2 (ICL2) of GPR40 in a helical conformation. Mutagenesis studies in ICL2 shows that this loop is important for Gs alpha subunit coupling. PMID: 29695780
    2. Data indicate that 20-HETE and FFAR1 function together in a positive feedback loop to enhance glucose-stimulated insulin secretion (GSIS). PMID: 29330456
    3. Comparison with an additional 2.2-A structure of the human GPR40-MK-8666 binary complex reveals an induced-fit conformational coupling between the partial agonist and AgoPAM binding sites, involving rearrangements of the transmembrane helices 4 and 5 (TM4 and TM5) and transition of the intracellular loop 2 (ICL2) into a short helix. PMID: 28581512
    4. Results show that GPR40 negatively regulated the cell motile and invasive activities of HT1080 cells suggesting that GPR40 negatively regulates the tumor progression of fibrosarcoma cells. PMID: 26331585
    5. Brain free long-chain fatty acids-GPR40/FFA1 signaling might have an important role in the modulation of endogenous pain control systems. (review) PMID: 28154332
    6. It regulates insulin secretion in pancreatic beta-cells. (review) PMID: 26028412
    7. Data from molecular docking simulations suggest that the binding pocket of GPR40 exhibits binding of free fatty acids (FFA) with chain lengths of C15 or fewer; for FFA with lengths longer than C15, part of alkyl chain extends out of binding pocket. PMID: 26974599
    8. GPR120 negatively and GPR40 positively regulate cellular functions during tumor progression in lung cancer cells. PMID: 26968637
    9. These data demonstrate that R104 in GPR40 is critically involved in the normal receptor functions. Interestingly, R104P is a registered single-nucleotide polymorphism of GPR40. PMID: 26505901
    10. Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4 PMID: 25131623
    11. results suggest that FFAR1 is the functionally dominant free fatty acid receptor in both human and guinea pig airway smooth muscle. PMID: 26342087
    12. upregulation of GPR40 expression enhances the mitogenic response to epoxyeicosatrienoic acids PMID: 25679385
    13. Palmitic acid boosted inflammatory response of microvascular endothelial cells to LPS via GPR40 and nSMase. PMID: 25795558
    14. knocking down the expression of the regulatory subunit PKAR1alpha, thereby reproducing the effects of IL-1beta and PGE on VSMCs, we demonstrated the contribution of PKA activity to the observed behavior of VSMCs PMID: 26408932
    15. These results suggest that distinct effects of GPR120 and GPR40 are involved in the acquisition of malignant property in pancreatic cancer cells. PMID: 26282200
    16. GPR40 functions via both G protein-mediated and beta-arrestin-mediated mechanisms; endogenous and synthetic ligands differentially engage these pathways to promote insulin secretion. PMID: 26157145
    17. GPR40 and PPARgamma can function as an integrated two-receptor signal transduction pathway, a finding with implications for rational antidiabetic drug development. PMID: 26105050
    18. the activation of GPR40 attenuates cisplatin-induced apoptosis. PMID: 25092426
    19. arrestin-3 and GRK2 play an essential role in the regulation of agonist-mediated GPR40 internalization, but are not involved in the regulation of constitutive GPR40 internalization. PMID: 25038452
    20. In a neuroblastoma cell line, GPR40 was activated by docosahexaenoic acid and selective agonists, yet not by palmitic acid. Its activation provoked the phosphorylation of CREB. PMID: 24550142
    21. the crystal structure of hGPR40 receptor bound to TAK-875 at 2.3 A resolution PMID: 25043059
    22. Potent free fatty acid 1 receptor agonist TUG-469 may be promising candidate for the treatment of type 2 diabetes mellitus. PMID: 23861168
    23. It was concluded that FFAR1 in the pancreatic beta-cell plays a substantial role not only in acute potentiation of insulin secretion by palmitate but also in the negative long-term effects of palmitate on insulin metabolism. PMID: 24035997
    24. FFAR1 agonists support beta-cell function, but variation in FFAR1 influences NEFA effects on insulin secretion and therefore could affect therapeutic efficacy of FFAR1 agonists. PMID: 23378609
    25. A review of the physiological role of GPR40 and potential antidiabetic drugs targeting GPR40. [Review] PMID: 23023155
    26. Propionate-stimulated GPR41 strongly coupled to ERK1/2 activation, while the coupling of linoleic acid-activated GPR40 and acetate-activated GPR43 was weaker. PMID: 22712802
    27. GPR41 gene expression is mediated by internal ribosome entry site (IRES)-dependent translation of bicistronic mRNA encoding GPR40 and GPR41 proteins PMID: 22493486
    28. Phytanic acid and pristanic acid activate the free fatty acid receptor GPR40, a G-protein-coupled receptor which is involved in the Ca2+ signaling of fatty acids. PMID: 21570468
    29. GPR40/FFA1 influences both insulin and glucagon secretion in rat islets, but only insulin secretion in human islets. PMID: 22106100
    30. differences in body composition and lipids associated with common SNPs in the FFAR1 gene PMID: 21552566
    31. Results describe agonist-receptor interactions of GPR40 using molecular dynamics simulations. PMID: 20227312
    32. results show expression of GPR40 in pancreatic islets which are regulated by FFA; finding that T2DM islets have lower GPR40 expression & correlation with insulin secretion raises possibility of involvement of GPR40 in diabetes beta-cell dysfunction PMID: 19758793
    33. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40 PMID: 12629551
    34. Results suggest that GPR40 is implicated in the control of breast cancer cell growth by fatty acids and that GPR40 may provide a link between fat and cancer. PMID: 15695516
    35. results suggest that the Arg211His polymorphism in the GPR40 protein gene may contribute to the variation of insulin secretory capacity in Japanese men PMID: 15736105
    36. study provides evidence for GPR40 gene expression in pancreatic beta cells and implicates GPR40 in insulin secretion in humans. PMID: 16525841
    37. GPR40 responded to fatty acids with different on-rates, and could be occupied by endogenous agonists before assay, masking the pharmacology of the receptor PMID: 17200419
    38. cell-specific expression of the GPR40 gene involves a characteristic chromatin organization of the locus and is controlled at the transcriptional level through HR2, a potent beta cell-specific enhancer PMID: 17525159
    39. analysis of residues important for agonist recognition and activation in GPR40 PMID: 17699519
    40. Variation in the FFAR1 gene may contribute to impaired beta cell function in type 2 diabetes PMID: 17987108
    41. This newly identified GPR40 variant results in a loss of function that prevents the beta-cell ability to adequately sense lipids as an insulin secretory stimulus because of impaired intracellular Ca2+ concentration increase. PMID: 18583466
    42. A flow cytometry-based binding assay for FFAR1 is reported. PMID: 18927207
    43. In this review, the mechanism of receptor activation, pharmacology, and the physiological functions of the fatty acid binding receptors GPR40, GPR41, GPR43, and GPR119 are discussed. PMID: 19009545
    44. Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation. PMID: 19068482
    45. Transfection of GPR40 into mice may provide a novel insulin secretagogue beneficial for the treatment of type 2 diabetes. PMID: 19401434
    46. This paper predicts the 5' structure of the human GP40 gene based on alignments between mouse and human genomic DNA. PMID: 17525159

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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：
    Detected in brain and pancreas. Detected in pancreatic beta cells.
  • 数据库链接：

    HGNC: 4498

    OMIM: 603820

    KEGG: hsa:2864

    STRING: 9606.ENSP00000246553

    UniGene: Hs.248127