[Pharmacology of PPARalpha, PPARgamma and dual PPARalpha/gamma agonists in clinical development].
Cardiovascular diseases (CVD) remain the leading cause of mortality in the western societies. Several risk factors predispose to CVD including diabetes, obesity, insulin resistance, dyslipidemia and hypertension. Various pharmacological therapies have been developed to control the risk factors associated to CVD. Fibrates are able to correct dyslipidemia, therefore decreasing CVD risk. Thiazolidinediones (TZD) or glitazones by increasing insulin sensitivity decrease plasma glucose levels in diabetic patients. Both fibrates and TZD activate the peroxisome proliferator-activated receptors (PPARs), a family of nuclear receptors that play a central role in the control of lipid and glucose metabolism. In this review, we will discuss the mode of action of fibrates and TZD and we will present an overview on PPAR ligands under development.
Inserm U.545, Département d'athérosclérose, Institut Pasteur de Lille, 1, rue du Professeur Calmette, 59019 Lille, France.
Daniel
D
Duran-Sandoval
Anne-Claire
AC
Thomas
Bernard
B
Bailleul
Jean-Charles
JC
Fruchart
Bart
B
Staels
D002318:Cardiovascular Diseases / Q000209:etiology / Q000517:prevention & control; D003924:Diabetes Mellitus, Type 2 / Q000150:complications; D006801:Humans; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents / Q000627:therapeutic use; D007333:Insulin Resistance; D024821:Metabolic Syndrome / Q000150:complications; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000037:antagonists & inhibitors; D014157:Transcription Factors / Q000819:agonists* / Q000037:antagonists & inhibitors
D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors