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The mechanism by which medium to long chain fatty acids stimulate insulin release was discovered recently that these acids stimulate G-protein coupled receptor 40 (GPR 40) otherwise termed as FFAR1. Stimulation of FFAR1 by fatty acids will enhance glucose dependent secretion of insulin from pancreas by affecting several signaling pathways inclusive of protein kinase C [122-124].
New thiazolidinedione derivatives (46 and 47) presented in Figure 21 were found to produce dual PPAR[gamma] and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from pancreas.
The report provides comprehensive information on the Free Fatty Acid Receptor 1 (G-Protein Coupled Receptor 40 or FFAR1), targeted therapeutics, complete with analysis by indications, stage of development, mechanism of action (MoA), route of administration (RoA) and molecule type.
FFAR1 agonists are "'different and interesting" in that they may be capable of restricted initiation of insulin secretion, and "will mainly potentiate nutrient-induced insulin secretion, which will favor enhanced prandial insulin secretion and reduce the risk of interprandial hypoglycemia," Dr.
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