E-64 [L-trans-epoxysuccinyl-leucyl-amido(4-guanidino)butane] and related epoxides as inhibitors of cysteine proteinases.

  title={E-64 [L-trans-epoxysuccinyl-leucyl-amido(4-guanidino)butane] and related epoxides as inhibitors of cysteine proteinases.},
  author={Alan J. Barrett and A. A. Kembhavi and Kentaro Hanada},
  journal={Acta biologica et medica Germanica},
  volume={40 10-11},
1. E-64 [L-trans-epoxysuccinyl-leucyl-amido(4-guanidino)butane] was found to be an active site directed irreversible inhibitor of all of the cysteine proteinases tested except clostripain, and not to affect other enzymes. Thus it seems to be a powerful selective inhibitor for cysteine proteinases in mammalian systems. 2. The very high rate of inactivation of some cysteine proteinases, including cathepsins B and L, allows the molarity of active enzyme to be determined by stoichiometric titration… CONTINUE READING