Peroxisome Proliferator Activated Receptor Agonists

The peroxisome proliferator activated receptors (PPARs) represent a group of ligand-activated transcription factors that mediate the biological effects of various drugs, such as fibrates and thiazolidinediones. Three PPAR subtypes can be distinguished, alpha, beta and gamma, each of which has an unique pattern of expression among vertebrate tissues. The PPAR alpha receptor is activated by hypolipidemic drugs of the fibrate class, and regulates the expression of numerous genes involved in fatty acid catabolism. The PPAR gamma receptor is activated by hypoglycaemic drugs of the thiazolidinedione class, and is an important determinant of adipocyte differentiation. Little is currently known about PPAR beta. A heavy research effort is currently directed towards the identification of novel high-affinity, high-specificity agonists and antagonists that may be used in the treatment of hyperglycaemia, hyperlipidemia, and other diseases of metabolic origin.