[Recent trends in PPARgamma agonist development of thiazolidinediones and non-thiazolidinediones]

Abstract

Peroxisome proliferator-activated receptor-gamma (PPARgamma) is a ligand-activated transcription factor regulating gene expression involved in the fatty acids, lipoprotein and carbohydrate metabolism and inflammation. Its wide range of potential therapeutic actions make it attractive targets for the development of drugs treating metabolic disorders such as metabolic syndrome, type 2 diabetes and dyslipidemia. The thiazolidinediones (TZDs) insulin-sensitizer of PPARgamma agonist have been clinically used for insulin resistant and diabetes patients in a decade. Despite the proven benefits of TZDs, safety concerns have led to drop out of the various newly developed PPARgamma targeting drugs. Here, I summarize the therapeutic potential and adverse events of TZDs and non-TZDs class of PPARgamma modulators, and will discuss the future strategy of the PPARgamma modulator development.