Free Fatty Acid Receptor Agonists for the Management of Type 2 Diabetes Mellitus

Signaling molecules such as fatty acids regulate a wide range of cellular activities and bodily functions. Free fatty acid receptors (FFARs) have recently been discovered in orphaned G-protein-coupled receptors (GPCRs). FFARs play a major role in insulin secretion and insulin resistance. These receptors have emerged as an attractive target for the management of type 2 diabetes mellitus (T2DM). FFAR4/GPCR120 are expressed in β-cells of the pancreas and can be regulated by medium- and long-chain fatty acids. Long-chain fatty acids have various biological functions beyond FFAR4 activation. FFAR4 plays an important role in regulating macrophage activation and can improve metabolic ailments associated with insulin resistance. FFAR4 activation may also be a promising therapeutic approach to addressing various metabolic and related disorders. The role of FFAR4 in T2DM has been briefly discussed in this review. Recent developments in FFAR4/GPCR120 agonists have also been reported, along with the mechanism by which GPCR120 agonists activate FFAR4.