Figure 1.

LCFAs augment insulin secretion by stimulating GPR40 in beta cells in the pancreas. GPR40 is also reportedly involved in the positive regulation of secretion of some intestinal hormones. Studies using GPR40 agonists and analyses of beta cell-specific GPR40 transgenic mice indicate that GPR40 is involved in the regulation of glucose metabolism, at least by the augmentation of insulin secretion. Because LCFA-mediated augmentation of insulin secretion is glucose-dependent, GPR40 is thought to be a potential target for novel anti-diabetic drugs with low risk of hypoglycemia.