L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L.

@article{Barrett1982LtransEpoxysuccinylleucylamido4gua,
  title={L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L.},
  author={Alan J. Barrett and A. A. Kembhavi and M A Brown and Heidrun Kirschke and C. Graham Knight and Masumi Tamai and Kentaro Hanada},
  journal={The Biochemical journal},
  year={1982},
  volume={201 1},
  pages={189-98}
}
1. L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) at a concentration of 0.5 mM had no effect on the serine proteinases plasma kallikrein and leucocyte elastase or the metalloproteinases thermolysin and clostridial collagenase. In contrast, 10 muM-E-64 rapidly inactivated the cysteine proteinases cathepsins B, H and L and papain (t0.5 = 0.1-17.3s). The streptococcal cysteine proteinase reacted much more slowly, and there was no irreversible inactivation of clostripain. The cysteine… CONTINUE READING
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