JTP-426467 acts as a selective antagonist for peroxisome proliferator-activated receptor γ in vitro and in vivo

Diabetes, Obesity and Metabolism

Volumn 8, Issue 5, 2006, Pages 508-516

  Nishiu, Jun ^a   Ito, M ^a   Ishida, Y ^a   Kakutani, M ^a   Shibata, T ^a   Matsushita, M ^a   Shindo, M ^a  

^a JAPAN TOBACCO INC   (Japan)

Author keywords

Antagonist; BRL49653 (rosiglitazone); JTP 426467; KK Ay; PPAR

Indexed keywords

2 CHLORO 5 NITROBENZANILIDE; CYCLOPHILIN; DNA; HORMONE SENSITIVE LIPASE; JTP 426467; LEPTIN; MESSENGER RNA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA ANTAGONIST; ROSIGLITAZONE; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ADIPOCYTE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRANCHED DNA SIGNAL AMPLIFICATION ASSAY; BROWN ADIPOSE TISSUE; CELL ASSAY; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG IDENTIFICATION; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; ENZYME INHIBITION; GLUCOSE BLOOD LEVEL; HORMONE BLOOD LEVEL; IN VITRO STUDY; IN VIVO STUDY; LIPID DIET; MALE; MONOTHERAPY; MOUSE; MOUSE STRAIN; NONHUMAN; NUCLEOTIDE SEQUENCE; PROTEIN DETERMINATION; PROTEIN EXPRESSION; STROMA CELL; STRUCTURE ANALYSIS; WEIGHT GAIN;

EID: 33746873672     PISSN: 14628902     EISSN: 14631326     Source Type: Journal    
DOI: 10.1111/j.1463-1326.2005.00536.x     Document Type: Article

References (30)

1. Nuclear Receptors Nomenclature Committee. A unified nomenclature system for the nuclear receptor superfamily. 1999; 97 (2): 161-163.
2. Issemann I, Green S. Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators. Nature 1990; 347 (6294): 645-650.
3. Tontonoz P, Hu E, Graves RA, Budavari AI, Spiegelman BM. mPPAR gamma 2: tissue-specific regulator of an adipocyte enhancer. Genes Dev 1994; 8 (10): 1224-1234.
4. Kliewer SA, Forman BM, Blumberg B et al. Differential expression and activation of a family of murine peroxisome proliferator-activated receptors. Proc Natl Acad Sci USA 1994; 91 (15): 7355-7359.
5. Braissant O, Foufelle F, Scotto C, Dauca M, Wahli W. Differential expression of peroxisome proliferator-activated receptors (PPARs): tissue distribution of PPAR-alpha-beta, and -gamma in the adult rat. Endocrinology 1996; 137 (1): 354-366.
6. Tontonoz P, Hu E, Spiegelman BM. Stimulation of adipogenesis in fibroblasts by PPAR gamma 2, a lipid-activated transcription factor. Cell 1994; 79 (7): 1147-1156.
7. Tontonoz P, Hu E, Spiegelman BM. Regulation of adipocyte gene expression and differentiation by peroxisome proliferator activated receptor gamma. Curr Opin Genet Dev 1995; 5 (5): 571-576.
8. Barak Y, Nelson MC, Ong ES et al. PPAR gamma is required for placental, cardiac, and adipose tissue development. Mol Cell 1999; 4 (4): 585-595.
9. 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 (4): 611-617.
10. Kubota N, Terauchi Y, Miki H et al. PPAR gamma mediates high-fat diet-induced adipocyte hypertrophy and insulin resistance. Mol Cell 1999; 4 (4): 597-609.
11. Lehmann JM, Moore LB, Smith-Oliver TA, Wilkison WO, Willson TM, Kliewer SA. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem 1995; 270 (22): 12953-12956.
12. Nolan JJ, Ludvik B, Beerdsen P, Joyce M, Olefsky J. Improvement in glucose tolerance and insulin resistance in obese subjects treated with troglitazone. N Engl J Med 1994; 331 (18): 1188-1193.
13. Miles PD, Barak Y, He W, Evans RM, Olefsky JM. Improved insulin-sensitivity in mice heterozygous for PPAR-gamma deficiency. J Clin Invest 2000; 105 (3): 287-292.
14. Yamauchi T, Kamon J, Waki H et al. The mechanisms by which both heterozygous peroxisome proliferator-activated receptor gamma (PPARgamma) deficiency and PPARgamma agonist improve insulin resistance. J Biol Chem 2001; 276 (44): 41245-41254.
15. Yamauchi T, Waki H, Kamon J et al. Inhibition of RXR and PPARgamma ameliorates diet-induced obesity and type 2 diabetes. J Clin Invest 2001; 108 (7): 1001-1013.
16. Leesnitzer LM, Parks DJ, Bledsoe RK et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry 2002; 41 (21): 6640-6650.
17. Lee G, Elwood F, McNally J et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem 2002; 277 (22): 19649-19657.
18. Camp HS, Chaudhry A, Leff T. A novel potent antagonist of peroxisome proliferator-activated receptor gamma blocks adipocyte differentiation but does not revert the phenotype of terminally differentiated adipocytes. Endocrinology 2001; 142 (7): 3207-3213.
19. Rieusset J, Touri F, Michalik L et al. A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesity and antidiabetic activity. Mol Endocrinol 2002; 16 (11): 2628-2644.
20. Wright HM, Clish CB, Mikami T et al. A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation. J Biol Chem 2000; 275 (3): 1873-1877.
21. Shibata T, Matsui K, Nagao K, Shinkai H, Yonemori F, Wakitani K. Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative. Eur J Pharmacol 1999; 364 (2-3): 211-219.
22. Hu E, Liang P, Spiegelman BM. AdipoQ is a novel adipose-specific gene dysregulated in obesity. J Biol Chem 1996; 271 (18): 10697-10703.
23. Burris TP, Pelton PD, Zhou L, Osborne MC, Cryan E, Demarest KT. A novel method for analysis of nuclear receptor function at natural promoters: peroxisome proliferator-activated receptor gamma agonist actions on aP2 gene expression detected using bDNA messenger RNA quantitation. Mol Endocrinol 1999; 13 (3): 410-417.
24. Shimaya A, Kurosaki E, Nakano R, Hirayama R, Shibasaki M, Shikama H. The novel hypoglycemic agent YM440 normalizes hyperglycemia without changing body fat weight in diabetic db/db mice. Metabolism 2000; 49 (3): 411-417.
25. Kishida K, Kuriyama H, Funahashi T et al. Aquaporin adipose, a putative glycerol channel in adipocytes. J Biol Chem 2000; 275 (27): 20896-20902.
26. Kopelman PG. Obesity as a medical problem. Nature 2000; 404: 635-643.
27. He W, Barak Y, Hevener A et al. Adipose-specific peroxisome proliferator-activated receptor gamma knockout causes insulin resistance in fat and liver but not in muscle. Proc Natl Acad Sci USA 2003; 100 (26): 15712-15717.
28. Zhang J, Fu M, Cui T et al. Selective disruption of PPARgamma 2 impairs the development of adipose tissue and insulin sensitivity. Proc Natl Acad Sci USA 2004; 101 (29): 10703-10708.
29. Akune T, Ohba S, Kamekura S et al. PPARgamma insufficiency enhances osteogenesis through osteoblast formation from bone marrow progenitors. J Clin Invest 2004; 113 (6): 846-855.
30. Rzonca SO, Suva LJ, Gaddy D, Montague DC, Lecka-Czernik B. Bone is a target for the antidiabetic compound rosiglitazone. Endocrinology 2004; 145 (1): 401-406.