Because FFAs have been long recognized as important regulators of glucose homeostasis via their ability to stimulate insulin secretion in the presence of glucose, GPR40 became a promising therapeutic target for type 2 diabetes treatment since its deorphanization, and a number of small-molecule GPR40 agonists are under development as drugs for type 2 diabetes [4,6]. The gene discussed is FFAR1; the disease is type 2 diabetes mellitus.