Role of peroxisome proliferator-activated receptor gamma (Ppar?) in different disease states: Recent updates

Abstract

Peroxisome proliferator-activated receptor (PPAR), a ligand dependant transcription factor, is a member of the nuclear receptor superfamily. PPAR exists in three isoforms i.e. PPAR alpha (PPAR?), PPAR beta (PPAR?), and PPAR gamma (PPAR?). These are multi-functional transcription factors and help in regulating inflammation, type 2 diabetes, lipid concentration in the body, metastasis, and tumor growth or angiogenesis. Activation of PPAR? causes inhibition of growth of cultured human breast, gastric, lung, prostate, and other cancer cells. PPAR? is mainly involved in fatty acid storage, glucose metabolism, and homeo-stasis and adipogenesis regulation. A large number of natural and synthetic ligands bind to PPAR? and modulate its activity. Ligands such as thiazolidinedione troglitazone, rosiglita-zone, pioglitazone effectively bind to PPAR?; however, most of these were found to display severe side effects such as hepatotoxicity, weight gain, cardiovascular complications and bladder tumor. Now the focus is shifted towards the development of dual-acting or pan PPAR ligands. The current review article describes the functions and role of PPAR? in various disease states. In addition, recently reported PPAR? ligands and pan PPAR ligands were dis-cussed in detail. It is envisaged that the present review article may help in the development of potent PPAR ligands with no or minimal side effects. � 2021 Bentham Science Publishers.