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Peroxisome Proliferator-Activated Receptors (PPARs) -A Review


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1 Ezhuthachan College of Pharmaceutical Sciences, Marayamuttom, Neyyattinkara, Thiruvananthapuram, Kerala, India
     

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PPARs are ligand-activated transcription factors involved in the transcriptional regulation of key metabolic pathways such as lipid metabolism, adipogenesis, and insulin sensitivity. More recent work implicates all 3 PPAR isotypes (α, γ, and δ) in inflammatory and atherosclerotic pathways. Because these nuclear receptors are activated by extracellular signals and control multiple gene targets, PPARs can be seen as nodes that control multiple inputs and outputs involved in energy balance, providing insight into how metabolism and the vasculature may be integrated. The ongoing clinical use of synthetic PPAR agonists, eg, insulin-sensitizing thiazolidinediones (TZDs) and lipid-lowering fibrates, and the evidence that PPAR activation also may limit inflammation and atherosclerosis have only heightened this interest and the pursuit of novel PPAR agonists. Together, these various observations have stimulated intense interest in PPARs as therapeutic targets and led to large-scale cardiovascular end-point trials with PPAR agonists.
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  • Larsen TM, Toubro S, Astrup A. Efficacy and safety of dietary supplements containing CLA for the treatment of obesity: evidence from animal and human studies. J Lipid Res. 2003 Dec;44(12):2234-41.
  • Gaullier JM, Halse J, Hoye K, Kristiansen K, Fagertun H, Vik H, Gudmundsen O. Conjugated linoleic acid supplementation for 1 y reduces body fat mass in healthy overweight humans. Am J Clin Nutr. 2004 Jun;79(6):1118-25.
  • Lefebvre AM, Chen I, Desreumaux P, Najib J, Fruchart JC, Geboes K, Briggs M, Heyman R, Auwerx J 1998 Activation of the peroxisome proliferator-activated receptor g promotes the development of colon tumors in C57BL/6J-APCMin/1 mice. Nat Med 4:1053-1057
  • Saez E, Tontonoz P, Nelson MC, Alvarez JGA, Ming UT, Baird S, Thomazy VA, EvansRM1998 Activators of the nuclear receptor PPARg enhance colon polyp formation. Nat Med 4: 1058-1061
  • Ito Y, Azrolan N, O’Connell A, Walsh A, Breslow JL 1990 Hypertriglyceridemia as a result of human apo CIII gene expression in transgenic mice. Science 249:790-793
  • Lock EA, Mitchell AM, Elcombe CR 1989 Biochemical mechanisms of induction of hepatic peroxisome proliferation. Annu Rev Pharmacol Toxicol 29:145-163
  • Gulick T, Cresci S, Caira T, Moore DD, Kelly DP 1994 The peroxisome proliferator-activated receptor regulates mitochondrial fatty acid oxidative enzyme gene expression. Proc Natl Acad Sci USA 91:11012-11016

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  • Peroxisome Proliferator-Activated Receptors (PPARs) -A Review

Abstract Views: 91  |  PDF Views: 2

Authors

N. J. Merlin
Ezhuthachan College of Pharmaceutical Sciences, Marayamuttom, Neyyattinkara, Thiruvananthapuram, Kerala, India
Sufiyan
Ezhuthachan College of Pharmaceutical Sciences, Marayamuttom, Neyyattinkara, Thiruvananthapuram, Kerala, India
Chitra C. Nair
Ezhuthachan College of Pharmaceutical Sciences, Marayamuttom, Neyyattinkara, Thiruvananthapuram, Kerala, India
Shaiju S. Dharan
Ezhuthachan College of Pharmaceutical Sciences, Marayamuttom, Neyyattinkara, Thiruvananthapuram, Kerala, India

Abstract


PPARs are ligand-activated transcription factors involved in the transcriptional regulation of key metabolic pathways such as lipid metabolism, adipogenesis, and insulin sensitivity. More recent work implicates all 3 PPAR isotypes (α, γ, and δ) in inflammatory and atherosclerotic pathways. Because these nuclear receptors are activated by extracellular signals and control multiple gene targets, PPARs can be seen as nodes that control multiple inputs and outputs involved in energy balance, providing insight into how metabolism and the vasculature may be integrated. The ongoing clinical use of synthetic PPAR agonists, eg, insulin-sensitizing thiazolidinediones (TZDs) and lipid-lowering fibrates, and the evidence that PPAR activation also may limit inflammation and atherosclerosis have only heightened this interest and the pursuit of novel PPAR agonists. Together, these various observations have stimulated intense interest in PPARs as therapeutic targets and led to large-scale cardiovascular end-point trials with PPAR agonists.

References