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Chemical Compound Review

Zfa-fmk     benzylN-[1-[(4-fluoro-3-oxo- butan-2...

Synonyms: Z-FA-FMK, Z-Phe-ala-fmk, Z-Phe-ala-CH2F, Z-Phe-AlaCH2F, FK029, ...
 
 
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High impact information on Zfa-fmk

  • A control peptidic fluoromethylketone (boc-Thr-CH2F), and inhibitors to calpain (Ac-Leu-Leu-norleucinal), cathepsin B (Z-Phe-Ala-CH2F), and CPP32-like proteases (Z-DEVD-CH2F), failed to prevent apoptotic death [1].
  • Secretion of degradative activity, the optimal pH, and the inhibition by E-64 and Z-Phe-Ala-CH2F indicates that cysteine proteinase activity is predominantly responsible for the degradation of human IgA by E. histolytica [2].
  • Slices from rat hippocampus were incubated with the caspase-3 inhibitor N-benzyloxycarbonyl-Asp-Glu-Val-Asp fluoromethylketone (Z-DEVD-FMK) or with the inactive peptide N-benzyloxycarbonyl-Phe-Ala fluoromethylketone (Z-Phe-Ala-FMK) for 30 min [3].
  • The effect of Z-Phe-Ala-FMK on molting was time and dose dependent [4].
  • A peptidyl fluoromethyl ketone (Z-Phe-Ala CH2F) was found to be an effective compound in a time dependent inactivation of cathepsin B isozymes from a number of tissues including human tumors [5].

References

  1. Inhibition of the interleukin-1 beta converting enzyme family rescues neurons from apoptotic death. Lynch, T., Vasilakos, J.P., Raser, K., Keane, K.M., Shivers, B.D. Mol. Psychiatry (1997) [Pubmed]
  2. Degradation of human IgA by Entamoeba histolytica. Kelsall, B.L., Ravdin, J.I. J. Infect. Dis. (1993) [Pubmed]
  3. Caspase activity is essential for long-term potentiation. Gulyaeva, N.V., Kudryashov, I.E., Kudryashova, I.V. J. Neurosci. Res. (2003) [Pubmed]
  4. Effect of protease class-specific inhibitors on in vitro development of the third- to fourth-stage larvae of Ascaris suum. Rhoads, M.L., Fetterer, R.H., Urban, J.F. J. Parasitol. (1998) [Pubmed]
  5. Visualization of time-dependent inactivation of human tumor cathepsin B isozymes by a peptidyl fluoromethyl ketone using a fluorescent print technique. Smith, R.E., Rasnick, D., Burdick, C.O., Cho, K.J., Rose, J.C., Vahratian, A. Anticancer Res. (1988) [Pubmed]
 
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