FFAR1 Antibody

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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HGNC: 4498

OMIM: 603820

KEGG: hsa:2864

STRING: 9606.ENSP00000246553

UniGene: Hs.248127