Description
The Peroxisome Proliferator Activated Receptor (PPAR) family of ligand-activated transcription factors consists of three subtypes encoded by separate genes: PPARα, PPARδ and PPARγ. Of these, PPARγ plays an important role in the regulation of fatty acid storage and glucose metabolism. The genes activated by PPARγ stimulate lipid uptake and adipogenesis by fat cells. Many endogenous molecules such as, polyunsaturated fatty acids like arachidonic acid and its metabolites, are known to bind and activate PPARγ. The binding of activating ligands to the ligand binding domain (LBD) of PPARγ promotes its heterodimerization with retinoic acid-like receptor (RXR), which results in the regulated expression of target genes involved in lipid metabolism. Such ligand-based activation of PPARγ may be responsible for inhibiting the growth of cultured human breast, gastric, lung, prostate and other cancer cell lines. In addition, the thiazolidinedione-based anti-diabetic drugs activate PPARγ with greater specificity than PPARα