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Chemical Compound Review

Darglitazone     5-[[4-[3-(5-methyl-2-phenyl- 1,3-oxazol-4...

Synonyms: CHEMBL55624, AC1L1U33, AC1Q6GK7, Tox21_113876, 141200-24-0, ...
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Disease relevance of Darglitazone


High impact information on Darglitazone


Biological context of Darglitazone

  • CONCLUSION AND CLINICAL RELEVANCE: The response of obese cats to darglitazone was similar to the response to thiazolidinediones in obese humans and rodents Darglitazone was effective in improving insulin sensitivity and glucose and lipid metabolism in obese cats [6].

Anatomical context of Darglitazone


Associations of Darglitazone with other chemical compounds


Gene context of Darglitazone

  • Furthermore, the PPARgamma agonists 9-hydroxy-(S)-10,12-octadecadienoic acid (9-HODE) and darglitazone also decreased VEGFR-1 mRNA expression [9].
  • RESULTS: Darglitazone increased CD36 mRNA and protein expression in human macrophage cells [7].
  • Within 4 h of exposing these cells to 30 microM darglitazone, there was an increase in UCP2 mRNA which reached a plateau of 5-10 times the basal in about 8 h [8].
  • Treatment of mature adipocytes with t10,c12 CLA alone or in combination with Darglitazone down-regulates the mRNA expression of PPARgamma as well as its target genes, fatty acid binding protein (aP2) and liver X receptor alpha (LXRalpha) [10].
  • A TZD, darglitazone (darg), can rapidly induce differentiation of HIB-1B cells, as judged by the expression of the adipocyte lipid binding protein (aP2), lipoprotein lipase (LPL), uncoupling protein (UCP) and beta3-adrenergic receptors [11].


  1. Mechanism and implications of brown adipose tissue proliferation in rats and monkeys treated with the thiazolidinedione darglitazone, a potent peroxisome proliferator-activated receptor-gamma agonist. Aleo, M.D., Lundeen, G.R., Blackwell, D.K., Smith, W.M., Coleman, G.L., Stadnicki, S.W., Kluwe, W.M. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  2. Thiazolidinediones increase plasma-adipose tissue FFA exchange capacity and enhance insulin-mediated control of systemic FFA availability. Oakes, N.D., Thalén, P.G., Jacinto, S.M., Ljung, B. Diabetes (2001) [Pubmed]
  3. Thiazolidinediones inhibit the expression of beta3-adrenergic receptors at a transcriptional level. Bakopanos, E., Silva, J.E. Diabetes (2000) [Pubmed]
  4. Fatty acids modulate the composition of extracellular matrix in cultured human arterial smooth muscle cells by altering the expression of genes for proteoglycan core proteins. Olsson, U., Bondjers, G., Camejo, G. Diabetes (1999) [Pubmed]
  5. Metabolic effects of darglitazone, an insulin sensitizer, in NIDDM subjects. Chaiken, R.L., Eckert-Norton, M., Pasmantier, R., Boden, G., Ryan, I., Gelfand, R.A., Lebovitz, H.E. Diabetologia (1995) [Pubmed]
  6. Effect of darglitazone on glucose clearance and lipid metabolism in obese cats. Hoenig, M., Ferguson, D.C. Am. J. Vet. Res. (2003) [Pubmed]
  7. Fatty acids modulate the effect of darglitazone on macrophage CD36 expression. Svensson, L., Camejo, G., Cabré, A., Vallvé, J.C., Pedreño, J., Norén, K., Wiklund, O., Hultén, L.M. Eur. J. Clin. Invest. (2003) [Pubmed]
  8. Thiazolidinediones stimulate uncoupling protein-2 expression in cell lines representing white and brown adipose tissues and skeletal muscle. Camirand, A., Marie, V., Rabelo, R., Silva, J.E. Endocrinology (1998) [Pubmed]
  9. Oxidised LDL decreases VEGFR-1 expression in human monocyte-derived macrophages. Salomonsson, L., Svensson, L., Pettersson, S., Wiklund, O., Ohlsson, B.G. Atherosclerosis (2003) [Pubmed]
  10. Trans10, cis12-conjugated linoleic acid prevents triacylglycerol accumulation in adipocytes by acting as a PPARgamma modulator. Granlund, L., Juvet, L.K., Pedersen, J.I., Nebb, H.I. J. Lipid Res. (2003) [Pubmed]
  11. 3',5'-cyclic adenosine monophosphate-response sequences of the uncoupling protein gene are sequentially recruited during darglitazone-induced brown adipocyte differentiation. Rabelo, R., Camirand, A., Silva, J.E. Endocrinology (1997) [Pubmed]
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