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  4. FFAR1 Antibody

FFAR1 Antibody

  • 货号：
    CSB-PA008938
  • 规格：
    ￥880
  • 图片：
    • Western Blot analysis of COS7 cells using GPR40 Polyclonal Antibody
    • Western Blot analysis of COS-7 cells using GPR40 Polyclonal Antibody
    • Western blot analysis of Mouse-kidney lysis using GPR40 antibody.
  • 其他：

产品详情

  • Uniprot No.：
    O14842
  • 基因名：
  • 别名：
    FFAR1; GPR40; Free fatty acid receptor 1; G-protein coupled receptor 40
  • 宿主：
    Rabbit
  • 反应种属：
    Human,Monkey
  • 免疫原：
    Synthesized peptide derived from the Internal region of Human GPR40.
  • 免疫原种属：
    Homo sapiens (Human)
  • 标记方式：
    Non-conjugated
  • 抗体亚型：
    IgG
  • 纯化方式：
    The antibody was affinity-purified from rabbit antiserum by affinity-chromatography using epitope-specific immunogen.
  • 浓度：
    It differs from different batches. Please contact us to confirm it.
  • 保存缓冲液：
    Liquid in PBS containing 50% glycerol, 0.5% BSA and 0.02% sodium azide.
  • 产品提供形式：
    Liquid
  • 应用范围：
    WB, IF, ELISA
  • 推荐稀释比：
    Application Recommended Dilution
    WB 1:500-1:2000
    IF 1:200-1:1000
    ELISA 1:10000
  • Protocols：
  • 储存条件：
    Upon receipt, store at -20°C or -80°C. Avoid repeated freeze.
  • 货期：
    Basically, we can dispatch the products out in 1-3 working days after receiving your orders. Delivery time maybe differs from different purchasing way or location, please kindly consult your local distributors for specific delivery time.

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