PPAR Ligands

Effects of thiazolidinediones beyond glycaemic control

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Kalaitzidis RG, Sarafidis PA, Bakris GL. Effects of thiazolidinediones beyond glycaemic control. Curr Pharm Des. 2009;15(5):529-536. The incidence of type 2 diabetes continues to increase in the western world over the past decade. Consequently, complications of this disease have reached crisis proportions.

Peroxisome proliferator-activated receptor-gamma coactivator-1 and insulin resistance: acute effect of fatty acids

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Hoeks J, Hesselink MK, Russell AP, et al. Peroxisome proliferator-activated receptor-gamma coactivator-1 and insulin resistance: acute effect of fatty acids. Diabetologia. 2006;49:2419-2426. Peroxisome proliferator-activated receptor (PPAR)-gamma coactivator-1 (PPARGC1), a coactivator regulating the transcription of genes involved in oxidative metabolism, is downregulated in patients with type 2 diabetes and in their first-degree relatives.

Peroxisome proliferator-activated receptor gamma agonists: their role as vasoprotective agents in diabetes

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Blaschke F, Caglayan E, Hsueh WA. Peroxisome proliferator-activated receptor gamma agonists: their role as vasoprotective agents in diabetes. Endocrinol Metabl Clin North Am. 2006;35:561-574. Thiazolidinediones (TZDs) a class of insulin sensitizing agents commonly used in the treatment of patients who have type 2 diabetes, improve endothelial dysfunction and exert beneficial effects on lipid profiles by activating the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-gamma).

PPAR-gamma Agonists and Diabetic Nephropathy

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Zhang Y, Guan Y. PPAR-gamma Agonists and Diabetic Nephropathy. Curr Diab Rep. 2005;5:470-475. Diabetic nephropathy is a clinical syndrome of albuminuria, declining glomerular filtration rate, and increased risk of cardiovascular disease.

Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive Study

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Dormandy JA, Charbonnel B, Eckland DJ, et al. Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive Study (PROspective pioglitAzone Clinical Trial In macroVascular Events): a randomised controlled trial. Lancet. 2005;366:1279-1289. Patients with type 2 diabetes are at high risk of fatal and non-fatal myocardial infarction and stroke. There is indirect evidence that agonists of peroxisome proliferator-activated receptor gamma (PPAR gamma) could reduce macrovascular complications. Our aim, therefore, was to ascertain whether pioglitazone reduces macrovascular morbidity and mortality in high-risk patients with type 2 diabetes.

PPAR Ligands: Potential Therapies for Metabolic Syndrome

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Akiyama TE, Meinke PT, Berger JP. PPAR Ligands: Potential Therapies for Metabolic Syndrome. Curr Diab Rep. 2005;5:45-52. Metabolic syndrome (MS), a condition characterized by multiple related clinical disorders including insulin resistance, central obesity, hyperlipidemia, hypertension, and heart disease, is an increasingly prevalent disease in industrialized societies.

Evidence for a potent antiinflammatory effect of rosiglitazone

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Mohanty P, Aljada A, Ghanim H, Hofmeyer D, Tripathy D, Syed T, Al-Haddad W, Dhindsa S, Dandona P. Evidence for a potent antiinflammatory effect of rosiglitazone. J Clin Endocrinol Metab. 2004;89:2728-2735. We have recently demonstrated a potent antiinflammatory effect of troglitazone, an agonist of peroxisome proliferator-activated receptor gamma (PPAR-gamma) and a partial agonist of PPAR-alpha in both the nondiabetic obese and diabetic obese subjects.

Peroxisome Proliferator-Activated Receptor-Gamma: Therapeutic Target for Diseases Beyond Diabetes: Quo Vadis?

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Pershadsingh, H. A.. Peroxisome Proliferator-Activated Receptor-Gamma: Therapeutic Target for Diseases Beyond Diabetes: Quo Vadis?. Expert Opin Investig Drugs. 2004;13:215-228. The discovery that the insulin-sensitising thiazolidinediones (TZDs), specific peroxisome proliferator-activated receptor-gamma (PPARgamma) agonists, have antiproliferative, anti-inflammatory and immunomodulatory effects has led to the evaluation of their potential use in the treatment of diabetic complications and inflammatory, proliferative diseases in non-insulin-resistant, euglycaemic individuals.

Long-term glycaemic control with pioglitazone in patients with type 2 diabetes

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Campbell IW. Long-term glycaemic control with pioglitazone in patients with type 2 diabetes. Int J Clin Pract. 2004;58:192-200. Patients with type 2 diabetes have dual defects: insulin resistance and beta-cell dysfunction. Thiazolidinediones (TZDs), a new class of oral drugs used for the treatment of type 2 diabetes, reduce insulin resistance via an action on peroxisome proliferator-activated receptors.

Peroxisome Proliferator-Activated Receptor-g Ligands Inhibit TGF-ß1-Induced Fibronectin Expression in Glomerular Mesangial Cells

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Guo B, Koya D, Isona M, Sugimoto T, Kashiwagi A, Haneda M. Peroxisome Proliferator-Activated Receptor-g Ligands Inhibit TGF-ß1-Induced Fibronectin Expression in Glomerular Mesangial Cells. Diabetes. 2004;53:200-208. are ligands for peroxisome proliferator-activated receptor (PPAR)-g, has been shown to possess potent anti-inflammatory and antineoplastic actions.

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