activated under control of PPAR-γ|
Drugs that bind to and either mimic (agonist) PPAR -αorγ effects are useful therapeutically in conditions characterized by lipid abnormalities (diabetes, cardiovascular disease). Drugs that bind to and activate PPAR-g (Rezulin, Avandia) can lower blood glucose levels and are used to treat type II diabetes. Drugs that activate PPAR-a (fibrates like gemfibrozil) can lower serum triglycerides (by stimulating liver fatty acid oxidation). Both drugs ultimately lower serum lipids.
PPARs also have an effect on plasma lipoprotein (LDL, HDL) levels. Both also might have a role in inflammation, which can promote cardiovascular disease. Fibrates, which interact with PPAR-a , appear to inhibit the inflammatory response mediated by the immune system by decreasing the release of protein "hormones" or cytokines, from stimulated immune cells.
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