ET1702-57·Anti-PPAR gamma Anti

Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear hormone receptor subfamily of transcription factors. PPARs form heterodimers with retinoid X receptors (RXRs). These heterodimers regulate transcription of genes involved in insulin action, adipocyte differentiation, lipid metabolism and inflammation. PPARγ is implicated in numerous diseases including obesity, diabetes, atherosclerosis and cancer. PPARγ activators include prostanoids, fatty acids, thiazolidinediones and N-(2-benzoylphenyl) tyrosine analogues. A key component in adipocyte differentiation and fat-specific gene expression, PPARγ may modulate macrophage functions such as proinflammatory activities, and stimulate oxidized low-density lipoprotein (x-LDL) uptake. A Pro12Ala polymorphism of the PPARγ2 gene has been reported to reduce transactivation activity in vitro. This substitution may affect the immune response to ox-LDL and be associated with type 2 diabetes. In addition, the Pro12Ala variant of the PPARγ2 gene maybe correlated with abdominal obesity in type 2 diabetes.