Ligands at Free Fatty Acid Receptor 1 (GPR40)

作者: Takafumi Hara

DOI: 10.1007/164_2016_59

关键词: AgonistBiochemistryIn vivoFree fatty acid receptorFatty acidInsulinG protein-coupled receptorReceptorChemistryFree fatty acid receptor 1

摘要: FFA1 is a G protein-coupled receptor activated by medium- to long-chain fatty acids. plays important roles in various physiological processes such as insulin secretion and energy metabolism. expressed on pancreatic β-cells intestine contributes incretin secretion, respectively. These functions of are interesting an attractive drug target for type II diabetes metabolic disorders. A number synthetic ligands have been developed they contributed our current understanding the pathophysiological both vitro vivo studies. In addition, these also provided information structure-activity relationships ligands. Further, protein crystallized with one high affinity agonist leads useful insights development more effective Among ligands, several compounds further investigated clinical trials. Thus, great potential candidates. this section, recent progress about possibility their use described.

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