Peroxisome proliferator-activated receptors (PPARs) are ligand-activated nuclear receptors that respond to several exogenous and\r\nendogenous ligands by modulating genes related to lipid, glucose, and insulin homeostasis. PPAR?, expressed in adipose tissue and\r\nliver, regulates lipid storage and glucose metabolism and is the target of type 2 diabetes drugs, thiazolidinediones (TZDs). Due to\r\nhigh levels of toxicity associated with the first generation TZDs, troglitazone (Rezulin), rosiglitazone (Avandia), and pioglitazone\r\n(Actos), there is a renewed search for newer PPAR drugs that exhibit better efficacy but lesser toxicity. In recent years, there has been\r\na definite increase in the consumption of dietary supplements among diabetics, due to the possible health benefits associated with\r\nthese nutraceutical components. With this impetus, investigations into alternative natural ligands of PPARs has also risen. This\r\nreview highlights some of the dietary compounds (dietary lipids, isoflavones, and other flavanoids) that bind and transactivate\r\nPPAR?. A better understanding of the physiological effects of this PPAR activation by nutraceuticals and the availability of highthroughput\r\ntechnologies should lead to the discovery of less toxic alternatives to the PPAR drugs currently on the market.
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