GPR43: an emerging target for the potential treatment of type 2 diabetes, obesity and insulin resistance.

Abstract

A new role for fatty acids as endocrine regulators of lipid and carbohydrate metabolism through the activation of their cognate receptors, GPCRs, has been discovered during the past decade. GPR43 is a GPCR that has been implicated in the regulation of fatty-acid and glucose homeostasis in adipose tissue and the intestines, thus having potential therapeutic relevance in the treatment of type 2 diabetes, insulin resistance and obesity. Ongoing drug discovery efforts are focused toward the development of a novel, potent and selective orthosteric or allosteric modulator that acts as an agonist for GPR43. This review summarizes data supporting a role for GPR43 in the pharmacological management of metabolic disorders.