Free fatty acid receptor 1 as a novel therapeutic target for type 2 diabetes mellitus-current status.

The incidence of type 2 diabetes mellitus (T2DM) has been on the increase in recent times. Although several oral treatments for T2DM are available, some of them have been found to elicit undesirable side effects. This therefore underscores the need for new treatment options with lesser side effects than the existing ones for people with T2DM. Free fatty acid receptor 1 (FFAR1), also known as GPR40, belongs to a class of G-protein coupled receptors that are encoded by FFAR1 genes in humans. It is expressed in the pancreatic β-cells and it is activated by medium- and long-chain saturated and unsaturated fatty acids. Thus it responds to endogenous medium and long chain unsaturated fatty acids, resulting in enhancement of insulin secretion during increased glucose levels. The glucose dependency of insulin secretion has made this receptor a very good target for developing therapies that could be efficacious with fewer side effects than the existing therapies for the treatment of T2DM. Given that tremendous efforts have been made in recent times in developing novel FFAR1 agonists with antidiabetic potentials, this article provides a current status of knowledge on the efforts made so far in developing novel FFAR1 agonists that would be of relevance in the management of T2DM.