PPAR-γ agonists and their role in type 2 diabetes mellitus management

American Journal of Therapeutics

Volumn 17, Issue 3, 2010, Pages 274-283

  Bermúdez, Valmore ^a   Finol, Freddy ^a   Parra, Nailyn ^a   Parra, Maria ^a   Pérez, Adriana ^a   Peñaranda, Lianny ^a   Vílchez, Daviel ^a   Rojas, Joselyn ^a   Arráiz, Nailet ^a   Velasco, Manuel ^b  

^a UNIVERSIDAD DEL ZULIA   (Venezuela)

^b UNIVERSIDAD CENTRAL DE VENEZUELA   (Venezuela)

Author keywords

Diabetes mellitus; Insulin resistance; PPARI; Thiazolidenediones

Indexed keywords

ANTIDIABETIC AGENT; GLITAZONE DERIVATIVE; GLUCOSE; INSULIN; METFORMIN; ORAL CONTRACEPTIVE AGENT; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; PIOGLITAZONE; PLACEBO; ROSIGLITAZONE; SULFONYLUREA; THIAZOLIDINEDIONE 18; TRANSCRIPTION FACTOR; TROGLITAZONE; UNCLASSIFIED DRUG;

ADIPOCYTE; ANEMIA; CARBOHYDRATE METABOLISM; CARDIOVASCULAR RISK; CELL DIFFERENTIATION; CLINICAL TRIAL; CONGESTIVE HEART FAILURE; DIET THERAPY; DRUG ANTAGONISM; DRUG CONTRAINDICATION; DRUG MECHANISM; DYSLIPIDEMIA; EDEMA; EXERCISE; GLUCOSE METABOLISM; GLYCEMIC CONTROL; HEART MUSCLE ISCHEMIA; HORMONE ACTION; HUMAN; INFLAMMATION; INSULIN RELEASE; INSULIN RESISTANCE; LIFESTYLE MODIFICATION; LIPID METABOLISM; LIVER TOXICITY; LUNG EDEMA; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN METABOLISM; PROTEIN PHOSPHORYLATION; PROTEIN STRUCTURE; PROTEIN SYNTHESIS; REVIEW; SIDE EFFECT; SIGNAL TRANSDUCTION; WEIGHT GAIN;

BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN; INSULIN RESISTANCE; LIPID METABOLISM; PPAR GAMMA; THIAZOLIDINEDIONES;

EID: 77952543578     PISSN: 10752765     EISSN: None     Source Type: Journal    
DOI: 10.1097/MJT.0b013e3181c08081     Document Type: Review

References (60)

1. Bosch X, Alfonso F, Bermejo J. Diabetes y enfermedad cardiovascular. Una mirada hacia la nueva epidemia del siglo XXI. Rev Esp Cardiol. 2002;55:525-527.
2. Bermúdez-Pirela VJ, Cano C, Medina MT, et al. Metformin plus low-dose glimeperide significantly improves Homeostasis Model Assessment for insulin resistance (HOMA (IR)) and beta-cell function (HOMA (beta-cell)) without hyperinsulinemia in patients with type 2 diabetes mellitus. Am J Ther. 2007;14:194-202.
3. Cases A. Morbimortalidad cardiovascular en la diabetes mellitus tipo 2. Hypertension. 2002;19:193-196.
4. Yki-Järvinen H. Insulin resistance in type 2 diabetes. In: Pickup JC, Williams G, eds. Textbook of Diabetes. 3rd ed. Oxford, UK: Blackwell; 2003:22:1-22.
5. Nathan DM, Buse JB, Davidson MB, et al. Management of hyperglycaemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy. A consensus statement from the American Diabetes Association and the European Association for the Study of Diabetes. Diabetología. 2006;49:1711-1721.
6. Nathan DM. Thiazolidinediones for initial treatment of type 2 diabetes? N Engl J Med. 2006;355:2477-2480.
7. Lebovitz HE, Kreider M, Freed MI. Evaluation of liver function in type 2 diabetic patients during clinical trials: evidence that rosiglitazone does not cause hepatic dysfunction. Diabetes Care. 2002;25:815-821.
8. Fox CS, Pencina MJ, Meigs JB, et al. Trends in the incidence of type 2 diabetes mellitus from the 1970s to the 1990s: the Framingham Heart Study. Circulation. 2006;113:2914-2918.
9. Son C, Hosoda K, Matsuda J, et al. Up-regulation of uncoupling protein 3 gene expression by fatty acids and agonists for PPARs in L6 myotubes. Endocrinology. 2001;142:4189-4194.
10. Ferré P. The biology of peroxisome proliferator-activated receptors: relationship with lipid metabolism and insulin sensitivity. Diabetes. 2004;53: S43-S50.
11. Lazennec G, Canaple L, Saugy D, et al. Activation of peroxisome proliferator-activated receptors (PPARs) by their ligands and protein kinase A activators. Mol. Endocrinol. 2000;14:1962-1975.
12. Desvergne B, Wahli W. Peroxisome proliferator-activated receptors: nuclear control of metabolism. Endocr Rev. 1999;20:649-688.
13. Wahli W, Martinez E. Superfamily of steroid nuclear receptors: positive and negative regulators of gene expression. FASEB J. 1991;5:2243-2249.
14. Van Raalte DH, Li M, Pritchard PH, et al. Peroxisome proliferator- activated receptor (PPAR) -alpha: a pharmacological target with a promising future. Pharm Res. 2004;21:1531-1538.
15. Brun RP, Tontonoz P, Forman BM, et al. Differential activation of adipogenesis by multiple PPAR isoforms. Genes Dev. 1996;10:974-984.
16. Shulman AI, Mangelsdorf DJ. Retinoid X receptor heterodimers in the metabolic syndrome. N Engl J Med. 2005;353:604-615.
17. Rosen ED, Spiegelman BM. PPARγ: a nuclear regulator of metabolism, differentiation, and cell growth. J Biol Chem. 2001;276:37731-37734.
18. Lehmann JM, Moore LB, Smith-Oliver TA, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator- activated receptor gamma (PPAR gamma). J Biol Chem. 1995;270:12953-12956.
19. Goldstein BJ. Current views on the mechanism of action of thiazolidinedione insulin sensitizers. Diabetes Technol Ther. 1999;1:267-275.
20. Kahn CR, Chen L, Cohen SE. Unraveling the mechanism of action of thiazolidinediones. J Clin Invest. 2000;106:1305-1307.
21. Saltiel AR, Olefsky JM. Thiazolidinediones in the treatment of insulin resistance and type II diabetes. Diabetes. 1996;45:1661-1669.
22. Kliewer SA, Lehmann JM, Milburn MV, et al. The PPARs and PXRs: nuclear xenobiotic receptors that define novel hormone signaling pathways. Recent Prog Horm Res. 1999;54:345-367.
23. Yki-Järvinen H. Thiazolidinediones. N Engl J Med. 2004;351:1106-1118.
24. Alemán G, Torres N, Tovar AR. Los receptores activados por proliferadores de Peroxisomas (PPARs) en el desarrollo de obesidad y resistencia a la insulina. Rev Invest Clín. 2004;56:351-367.
25. Greenfield JR, Chisholm DJ. Thiazolidinediones-Mechanism of Action. Austr Prescriber. 2004;27:67-70.
26. Lebovitz HE, Banerji MA. Insulin resistance and its treatment by thiazolidinediones. Recent Prog Horm Res. 2001;56:265-294.
27. Boyle PJ, King AB, Olansky L, et al. Effects of pioglitazone and rosiglitazone on blood lipid levels and glycemic control in patients with type 2 diabetes mellitus: a retrospective review of randomly selected medical records. Clin Ther. 2002;24:378-396.
28. Lehmann JM, Lenhard JM, Oliver BB, et al. Peroxisome proliferator- activated receptors alpha and gamma are activated by indomethacin and other non-steroidal antiinflammatory drugs. J Biol Chem. 1997;272:3406-3410.
29. LeBrasseur NK, Kelly M, Tsao TS, et al. Thiazolidinediones can rapidly activate AMP-activated protein kinase in mammalian tissues. Am J Physiol Endocrinol Metab. 2006;291: E175-E181.
30. Wiley SE, Murphy AN, Ross SA, et al. MitoNEET is an iron-containing outer mitochondrial membrane protein that regulates oxidative capacity. Proc Natl Acad Sci U S A. 2007;104:5318-5323.
31. Wiley SE, Paddock ML, Abresch EC, et al. The outer mitochondrial membrane protein mitoNEET contains a novel redox-active 2Fe-2S cluster. J Biol Chem. 2007;282:23745-23749.
32. Paddock ML, Wiley SE, Axelrod HL, et al. MitoNEET is a uniquely folded 2Fe-2S outer mitochondrial membrane protein stabilized by pioglitazone. Proc Natl Acad Sci U S A. 2007;104:14342-14347.
33. Kumar S, Boulton AJ, Beck-Nielsen H, et al. Troglitazone, an insulin action enhancer, improves metabolic control in NIDDM patients. Troglitazone Study Group. Diabetologia. 1996;39:701-709.
34. Buchanan TA, Xiang AH, Peters RK, et al. Preservation of pancreatic beta-cell function and prevention of type 2 diabetes by pharmacological treatment of insulin resistance in high-risk Hispanic women. Diabetes. 2002;51:2796-2803.
35. Mayerson AB, Hundal RS, Dufour S, et al. The effects of rosiglitazone on insulin sensitivity, lipolysis, and hepatic and skeletal muscle triglyceride content in patients with type 2 diabetes. Diabetes. 2002;51:797-802.
36. Willson TM, Lambert MH, Kliewer SA. Peroxisome proliferator-activated receptor gamma and metabolic disease. Annu Rev Biochem. 2001;70:341-367.
37. Tontonoz P, Hu E, Spiegelman BM. Stimulation of adipogenesis in fibroblasts by PPAR gamma 2, a lipidactivated transcription factor. Cell. 1994;79:1147-1156.
38. Rosen ED, Sarraf P, Troy AE, et al. PPAR gamma is required for the differentiation of adipose tissue in vivo and in vitro. Mol Cell. 1999;4:611-617.
39. Kramer D, Shapiro R, Adler A, et al. Insulin-sensitizing effect of rosiglitazone (BRL-49653) by regulation of glucose transporters in muscle and fat of Zucker rats. Metabolism. 2001;50:1294-1300.
40. Schoonjans K, Peinado-Onsurbe J, Lefebvre AM, et al. PPARalpha and PPARgamma activators direct a distinct tissue-specific transcriptional response via a PPRE in the lipoprotein lipase gene. EMBO J. 1996;15:5336-5348.
41. Tontonoz P, Hu E, Devine J, et al. PPAR gamma 2 regulates adipose expression of the phosphoenolpyruvate carboxykinase gene. Mol Cell Biol. 1995;15:351-357.
42. Schoonjans K, Watanabe M, Suzuki H, et al. Induction of the acyl-coenzyme A synthetase gene by fibrates and fatty acids is mediated by a peroxisome proliferator response element in the C promoter. J Biol Chem. 1995;270:19269-19276.
43. Qi C, Pekala PH. Tumor necrosis factor-alpha-induced insulin resistance in adipocytes. Proc Soc Exp Biol Med. 2000;223:128-135.
44. Walczak R, Tontonoz P. PPARadigms and PPARadoxes: expanding roles for PPARgamma in the control of lipid metabolism. J Lipid Res. 2002;43:177-186.
45. Steppan CM, Bailey ST, Bhat S, et al. The hormone resistin links obesity to diabetes. Nature. 2001;409:307-312.
46. Lee CH, Olson P, Evans RM. Minireview: lipid metabolism, metabolic diseases, and peroxisome proliferator activated receptors. Endocrinology. 2003;144:2201-2207.
47. Nissen SE, Wolski K. Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes. N Engl J Med. 2007;356:2457-2471.
48. Home PD, Pocock SJ, Beck-Nielsen H, et al. Rosiglitazone evaluated for cardiovascular outcomes-an interim analysis. N Engl J Med. 2007;357:28-38.
49. Rosen CJ. The rosiglitazone story-lessons from an FDA Advisory Committee meeting. N Engl J Med. 2007;357:844-846.
50. Dormandy JA, Charbonnel B, Eckland DJ, et al. Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive Study (PRO- spective pioglitAzone Clinical Trial In macroVascular Events): a randomised controlled trial. Lancet. 2005;366:1279-1289.
51. Lincoff AM, Wolski K, Nicholls SJ, et al. Pioglitazone and risk of cardiovascular events in patients with type 2 diabetes mellitus: a meta-analysis of randomized trials. JAMA. 2007;298:1180-1188.
52. Tang W H W. Do thiazolidinediones cause heart failure? A critical review. Cleve Clin J Med. 2006;73:390-397.
53. Erdmann E, Wilcox RG. Weighing up the cardiovascular benefits of thiazolidinedione therapy: the impact of increased risk of heart failure. Eur Heart J. 2008;29:12-20.
54. Cheng AY, Fantus IG. Oral antihyperglycemic therapy for type 2 diabetes mellitus. CMAJ. 2005;172:213-226.
55. Carey DG, Cowin GJ, Galloway GJ, et al. Effect of rosiglitazone on insulin sensitivity and body composition in type 2 diabetic patients. Obes Res. 2002;10:1008-1015.
56. Miyazaki Y, Mahankali A, Matsuda M, et al. Effect of pioglitazone on abdominal fat distribution and insulin sensitivity in type 2 diabetic patients. J Clin Endocrinol Metab. 2002;87:2784-2791.
57. Krentz AJ, Bailey CJ, Melander A. Thiazolidinediones for type 2 diabetes. New agents reduce insulin resistance but need long term clinical trials. BMJ. 2000;321:252-253.
58. Guo Q, Sahoo SP, Wang PR, et al. A novel peroxisome proliferator- activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis. Endocrinology. 2004;145:1640-1648.
59. Desai RC, Han W, Metzger EJ, et al. 5-aryl thiazolidine-2, 4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents. Bioorg Med Chem Lett. 2003;13:2795-2798.
60. Yki-Järvinen H. Pathogenesis of non-insulin-dependent diabetes mellitus. Lancet. 1994;343:91-95.