A nonthiazolidinedione peroxisome proliferator-activated receptor α/γ dual agonist CG301360 alleviates insulin resistance and lipid dysregulation in db/db mice

Molecular Pharmacology

Volumn 78, Issue 5, 2010, Pages 877-885

  Jeong, Hyun Woo ^a   Lee, Joo Won ^a   Kim, Woo Sik ^a   Choe, Sung Sik ^a   Shin, Hyun Jung ^a   Lee, Gha Young ^a   Shin, Dongkyu ^b   Lee, Jun Hee ^b   Choi, Eun Bok ^c   Lee, Hyun Kyu ^c   Yon, Gyu Hwan ^c   Cho, Bongjun ^d   Kim, Hye Ryung ^d   Choi, Sung Hee ^d   Chung, Young Sun ^e   Park, Seung Bum ^a   Chung, Heekyoung ^f   Ro, Seonggu ^b   Kim, Jae Bum ^a  

^a Seoul National University   (South Korea)

^b Crystal Genomics   (South Korea)

^c Korea Research Institute of Chemical Technology   (South Korea)

^d Seoul National University Bundang Hospital   (South Korea)

^e Korea Cyber University   (South Korea)

^f Hanyang University   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

CG 301360; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG INHIBITION; DRUG MECHANISM; FATTY ACID OXIDATION; GENE EXPRESSION; GLUCOSE TRANSPORT; INSULIN RESISTANCE; INSULIN SENSITIVITY; LIPID METABOLISM; MOUSE; NONHUMAN; PRIORITY JOURNAL; TRANSCRIPTION INITIATION; WEIGHT GAIN;

ADIPOCYTES; ANIMALS; CELLS, CULTURED; CYCLOOXYGENASE 2; CYTOKINES; FATTY ACIDS; GENE EXPRESSION REGULATION; GLUCOSE; INSULIN RESISTANCE; LIPID METABOLISM; MACROPHAGES; MATRIX METALLOPROTEINASE 9; MICE; MICE, OBESE; OXAZOLES; OXIDATION-REDUCTION; PIPECOLIC ACIDS; PPAR ALPHA; PPAR DELTA; STEREOISOMERISM; TRANSCRIPTION, GENETIC;

EID: 77958144044     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.110.065748     Document Type: Article

References (39)

1. Al-Salman J, Arjomand H, Kemp DG, and Mittal M (2000) Hepatocellular injury in a patient receiving rosiglitazone. A case report. Ann Intern Med 132:121-124. (Pubitemid 30044179)
2. Barak Y, Nelson MC, Ong ES, Jones YZ, Ruiz-Lozano P, Chien KR, Koder A, and Evans RM (1999) PPAR gamma is required for placental, cardiac, and adipose tissue development. Mol Cell 4:585-595. (Pubitemid 29531138)
3. Bourguet W, Germain P, and Gronemeyer H (2000) Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications. Trends Pharmacol Sci 21:381-388.
4. Carmona MC, Louche K, Nibbelink M, Prunet B, Bross A, Desbazeille M, Dacquet C, Renard P, Casteilla L, and Penicaud L (2005) Fenofibrate prevents rosiglitazone-induced body weight gain in ob/ob mice. Int J Obes (Lond) 29:864-871. (Pubitemid 40897026)
5. Chaput E, Saladin R, Silvestre M, and Edgar AD (2000) Fenofibrate and rosiglitazone lower serum triglycerides with opposing effects on body weight. Biochem Biophys Res Commun 271:445-450. (Pubitemid 30444746)
6. DeFronzo RA and Ferrannini E (1991) Insulin resistance. A multifaceted syndrome responsible for NIDDM, obesity, hypertension, dyslipidemia, and atherosclerotic cardiovascular disease. Diabetes Care 14:173-194.
7. Evans RM, Barish GD, and Wang YX (2004) PPARs and the complex journey to obesity. Nat Med 10:355-361.
8. Goldstein BJ, Rosenstock J, Anzalone D, Tou C, and Ohman KP (2006) Effect of tesaglitazar, a dual PPAR alpha/gamma agonist, on glucose and lipid abnormalities in patients with type 2 diabetes: a 12-week dose-ranging trial. Curr Med Res Opin 22:2575-2590. (Pubitemid 46048373)
9. Grether U, Bénardeau A, Benz J, Binggeli A, Blum D, Hilpert H, Kuhn B, Märki HP, Meyer M, Mohr P, et al. (2009) Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists. ChemMedChem 4:951-956.
10. Guérin M, Bruckert E, Dolphin PJ, Turpin G, and Chapman MJ (1996) Fenofibrate reduces plasma cholesteryl ester transfer from HDL to VLDL and normalizes the atherogenic, dense LDL profile in combined hyperlipidemia. Arterioscler Thromb Vasc Biol 16:763-772. (Pubitemid 26179365)
11. Guerre-Millo M, Gervois P, Raspé E, Madsen L, Poulain P, Derudas B, Herbert JM, Winegar DA, Willson TM, Fruchart JC, et al. (2000) Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem 275:16638-16642. (Pubitemid 30398891)
12. Harrity T, Farrelly D, Tieman A, Chu C, Kunselman L, Gu L, Ponticiello R, Cap M, Qu F, Shao C, et al. (2006) Muraglitazar, a novel dual (alpha/gamma) peroxisome proliferator-activated receptor activator, improves diabetes and other metabolic abnormalities and preserves beta-cell function in db/db mice. Diabetes 55:240-248. (Pubitemid 43343321)
13. He W, Barak Y, Hevener A, Olson P, Liao D, Le J, Nelson M, Ong E, Olefsky JM, and Evans RM (2003) Adipose-specific peroxisome proliferator-activated receptor gamma knockout causes insulin resistance in fat and liver but not in muscle. Proc Natl Acad Sci USA 100:15712-15717. (Pubitemid 38021055)
14. Hellmold H, Zhang H, Andersson U, Blomgren B, Holland T, Berg AL, Elebring M, Sjögren N, Bamberg K, Dahl B, et al. (2007) Tesaglitazar, a PPARalpha/gamma agonist, induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats. Toxicol Sci 98:63-74. (Pubitemid 47073822)
15. Hevener AL, He W, Barak Y, Le J, Bandyopadhyay G, Olson P, Wilkes J, Evans RM, and Olefsky J (2003) Muscle-specific Pparg deletion causes insulin resistance. Nat Med 9:1491-1497. (Pubitemid 38004776)
16. Hirsch IB, Kelly J, and Cooper S (1999) Pulmonary edema associated with troglitazone therapy. Arch Intern Med 159:1811. (Pubitemid 29379147)
17. Issemann I and Green S (1990) Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators. Nature 347:645-650.
18. Jeong HW, Hsu KC, Lee JW, Ham M, Huh JY, Shin HJ, Kim WS, and Kim JB (2009) Berberine suppresses proinflammatory responses through AMPK activation in macrophages. Am J Physiol Endocrinol Metab 296:E955-E964.
19. Kahn CR (1994) Banting Lecture. Insulin action, diabetogenes, and the cause of type II diabetes. Diabetes 43:1066-1084. (Pubitemid 24230714)
20. Kersten S, Seydoux J, Peters JM, Gonzalez FJ, Desvergne B, and Wahli W (1999) Peroxisome proliferator-activated receptor alpha mediates the adaptive response to fasting. J Clin Invest 103:1489-1498.
21. Kim WS, Lee YS, Cha SH, Jeong HW, Choe SS, Lee MR, Oh GT, Park HS, Lee KU, Lane MD, et al. (2009) Berberine improves lipid dysregulation in obesity by controlling central and peripheral AMPK activity. Am J Physiol Endocrinol Metab 296:E812-E819.
22. Lehmann JM, Moore LB, Smith-Oliver TA, Wilkison WO, Willson TM, and Kliewer SA (1995) An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem 270:12953-12956.
23. Lloyd S, Hayden MJ, Sakai Y, Fackett A, Silber PM, Hewitt NJ, and Li AP (2002) Differential in vitro hepatotoxicity of troglitazone and rosiglitazone among cryopreserved human hepatocytes from 37 donors. Chem Biol Interact 142:57-71. (Pubitemid 35232553)
24. Mittra S, Sangle G, Tandon R, Sharma S, Roy S, Khanna V, Gupta A, Sattigeri J, Sharma L, Priyadarsiny P, et al. (2007) Increase in weight induced by muraglitazar, a dual PPARalpha/gamma agonist, in db/db mice: adipogenesis/or oedema? Br J Pharmacol 150:480-487. (Pubitemid 46280645)
25. Muegge I and Martin YC (1999) A general and fast scoring function for proteinligand interactions: a simplified potential approach. J Med Chem 42:791-804. (Pubitemid 29136170)
26. Murakami K, Tobe K, Ide T, Mochizuki T, Ohashi M, Akanuma Y, Yazaki Y, and Kadowaki T (1998) A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats. Diabetes 47:1841-1847. (Pubitemid 28549189)
27. Nissen SE and Wolski K (2007) Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes. N Engl J Med 356:2457-2471. (Pubitemid 46919772)
28. Saltiel AR and Olefsky JM (1996) Thiazolidinediones in the treatment of insulin resistance and type II diabetes. Diabetes 45:1661-1669. (Pubitemid 26398943)
29. Seo JB, Moon HM, Kim WS, Lee YS, Jeong HW, Yoo EJ, Ham J, Kang H, Park MG, Steffensen KR, et al. (2004) Activated liver X receptors stimulate adipocyte differentiation through induction of peroxisome proliferator-activated receptor gamma expression. Mol Cell Biol 24:3430-3444. (Pubitemid 38455438)
30. Shim WS, Do MY, Kim SK, Kim HJ, Hur KY, Kang ES, Ahn CW, Lim SK, Lee HC, and Cha BS (2006) The long-term effects of rosiglitazone on serum lipid concentrations and body weight. Clin Endocrinol (Oxf) 65:453-459. (Pubitemid 44414268)
31. Shoelson SE, Lee J, and Goldfine AB (2006) Inflammation and insulin resistance. J Clin Invest 116:1793-1801.
32. Tamori Y, Masugi J, Nishino N, and Kasuga M (2002) Role of peroxisome proliferator-activated receptor-gamma in maintenance of the characteristics of mature 3T3-L1 adipocytes. Diabetes 51:2045-2055. (Pubitemid 34729007)
33. Tang WH, Francis GS, Hoogwerf BJ, and Young JB (2003) Fluid retention after initiation of thiazolidinedione therapy in diabetic patients with established chronic heart failure. J Am Coll Cardiol 41:1394-1398.
34. Tannehill-Gregg SH, Sanderson TP, Minnema D, Voelker R, Ulland B, Cohen SM, Arnold LL, Schilling BE, Waites CR, and Dominick MA (2007) Rodent carcinogenicity profile of the antidiabetic dual PPAR alpha and gamma agonist muraglitazar. Toxicol Sci 98:258-270. (Pubitemid 47073837)
35. Wang YX, Lee CH, Tiep S, Yu RT, Ham J, Kang H, and Evans RM (2003) Peroxisome- proliferator-activated receptor delta activates fat metabolism to prevent obesity. Cell 113:159-170. (Pubitemid 36514968)
36. Watkins PB and Whitcomb RW (1998) Hepatic dysfunction associated with troglitazone. N Engl J Med 338:916-917.
37. Xu J, Lloyd DJ, Hale C, Stanislaus S, Chen M, Sivits G, Vonderfecht S, Hecht R, Li YS, Lindberg RA, et al. (2009) Fibroblast growth factor 21 reverses hepatic steatosis, increases energy expenditure, and improves insulin sensitivity in diet-induced obese mice. Diabetes 58:250-259.
38. Yamauchi T, Kamon J, Minokoshi Y, Ito Y, Waki H, Uchida S, Yamashita S, Noda M, Kita S, Ueki K, et al. (2002) Adiponectin stimulates glucose utilization and fatty-acid oxidation by activating AMP-activated protein kinase. Nat Med 8:1288-1295. (Pubitemid 35373562)
39. Yoon MJ, Lee GY, Chung JJ, Ahn YH, Hong SH, and Kim JB (2006) Adiponectin increases fatty acid oxidation in skeletal muscle cells by sequential activation of AMP-activated protein kinase, p38 mitogen-activated protein kinase, and peroxisome proliferator-activated receptor alpha. Diabetes 55:2562-2570.