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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Chemical Compound Review: 

Clenicor     1-chloro-4- (dimethoxyphosphoryl...

Synonyms: Mifobate, Mifobato, Mifobatum, Clenicor (TN), CHEMBL284768, ...
 
 
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Disease relevance of SR 202

  • Because it yields both antiobesity and antidiabetic effects, SR-202 may be a lead for new compounds to be used in the treatment of obesity and type 2 diabetes [1].
  • In vivo, decreasing PPARgamma activity, either by treatment with SR-202 or by invalidation of one allele of the PPARgamma gene, leads to a reduction of both high fat diet-induced adipocyte hypertrophy and insulin resistance [1].
 

High impact information on SR 202

  • Treatment with SR-202 also dramatically improves insulin sensitivity in the diabetic ob/ob mice [1].
  • Here, we report on the identification of a new synthetic PPARgamma antagonist, the phosphonophosphate SR-202, which inhibits both TZD-stimulated recruitment of the coactivator steroid receptor coactivator-1 and TZD-induced transcriptional activity of the receptor [1].
  • In cell culture, SR-202 efficiently antagonizes hormone- and TZD-induced adipocyte differentiation [1].
  • Cell demise was attenuated by SR-202, a synthetic PPARgamma antagonist, and specificity was further verified by excluding a proapoptotic response to a PPARalpha agonist [2].
  • The specific peroxisome proliferator-activated receptor gamma (PPARgamma) inhibitor, SR-202, failed to modulate this effect [3].
 

Associations of SR 202 with other chemical compounds

  • The ob/ob mouse is diabetic at 8 weeks and plasma glucose and insulin levels continue to rise over the next 3 weeks, and treatment with SR-202 prevents these increases [4].
 

Gene context of SR 202

References

  1. A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesity and antidiabetic activity. Rieusset, J., Touri, F., Michalik, L., Escher, P., Desvergne, B., Niesor, E., Wahli, W. Mol. Endocrinol. (2002) [Pubmed]
  2. Peroxisome proliferator-activated receptor gamma contributes to T lymphocyte apoptosis during sepsis. Soller, M., Tautenhahn, A., Brüne, B., Zacharowski, K., John, S., Link, H., von Knethen, A. J. Leukoc. Biol. (2006) [Pubmed]
  3. Thiazolidinediones inhibit TNFalpha induction of PAI-1 independent of PPARgamma activation. Liu, H.B., Hu, Y.S., Medcalf, R.L., Simpson, R.W., Dear, A.E. Biochem. Biophys. Res. Commun. (2005) [Pubmed]
  4. Do peroxisome proliferation receptor-gamma antagonists have clinical potential as combined antiobesity and antidiabetic drugs? Doggrell, S. Expert opinion on investigational drugs. (2003) [Pubmed]
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