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Chemical Compound Review

CHEMBL514958     (2R,3S)-3-(hydroxy-methanoyl- amino)-4...

Synonyms: GW-3333, CHEBI:556718, AC1Q5NWC, CID216470, DNC000079, ...
 
 
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High impact information on GW3333

  • Inhibition of tumor necrosis factor-alpha (TNF-alpha) production and arthritis in the rat by GW3333, a dual inhibitor of TNF-alpha-converting enzyme and matrix metalloproteinases [1].
  • In a model wherein intrapleural zymosan injection causes an increase in TNF in the pleural cavity, GW3333 completely inhibited the increase in TNF in the pleural cavity for 12 h [1].
  • The CYP3A induction level achieved with GW3333 at a concentration of approximately 10 microM in human hepatocytes was comparable to that achieved with rifampicin at a concentration of 10 microM [2].
  • The extent of rodent CYP3A induction caused by GW3333 was confirmed in vivo after daily oral administration for 14 days to rats [2].
  • A new approach to reducing the effects of TNF- alpha is to decrease its synthesis by inhibiting TNF- alpha converting enzyme with GW3333 [3].
 

Analytical, diagnostic and therapeutic context of GW3333

References

  1. Inhibition of tumor necrosis factor-alpha (TNF-alpha) production and arthritis in the rat by GW3333, a dual inhibitor of TNF-alpha-converting enzyme and matrix metalloproteinases. Conway, J.G., Andrews, R.C., Beaudet, B., Bickett, D.M., Boncek, V., Brodie, T.A., Clark, R.L., Crumrine, R.C., Leenitzer, M.A., McDougald, D.L., Han, B., Hedeen, K., Lin, P., Milla, M., Moss, M., Pink, H., Rabinowitz, M.H., Tippin, T., Scates, P.W., Selph, J., Stimpson, S.A., Warner, J., Becherer, J.D. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  2. CYP3A induction by N-hydroxyformamide tumor necrosis factor-alpha converting enzyme/matrix metalloproteinase inhibitors use of a pregname X receptor activation assay and primary hepatocyte culture for assessing induction potential in humans. Tippin, T.K., Hamilton, G., Moore, L., Beaudet, E.J., Jolley, S., Brodie, T.A., Andrews, R.C., Becherer, J.D., McDougald, D.L., Gaul, M.D., Hoivik, D.J., Mellon-Kusibab, K., Lehmann, J., Kliewer, S., Novick, S., Laethem, R., Zhao, Z., LeCluyse, E.L. Drug Metab. Dispos. (2003) [Pubmed]
  3. TACE inhibition: a new approach to treating inflammation. Doggrell, S.A. Expert opinion on investigational drugs. (2002) [Pubmed]
 
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