Novel Peroxisome Proliferating Activated Receptor (PPAR) modulator drug discovery : consensus virtual screening and characterisation of biochemcial and pharmacological activities

Abstract

Peroxisome proliferator-activated receptors (PPARs) are ligand activated transcription factors that form a subfamily of the nuclear receptor superfamily. PPARs form heterodimers with the 9-cis-retinoic acid receptor (RXR) and activate transcription events by binding to a specific DNA element called the PPAR response element (PPRE). Their transcription factor activity accounts for a wide range of effects on metabolism, cellular proliferation, cellular differentiation, and immune responses. From a pathological perspective, PPARs are implicated in a diverse range of disease states including type II diabetes, obesity, dyslipidemia, atherosclerosis, inflammation, and neurodegeneration.