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Chemical Compound Review

CHEMBL374508     (2S,3S)-3-[[(1S)-1-[4- (diaminomethylidenea...

Synonyms: e-64, CHEBI:30270, ANW-71599, KST-1A7499, AC1L3XOG, ...
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Disease relevance of BRN 1405664


Psychiatry related information on BRN 1405664


High impact information on BRN 1405664


Biological context of BRN 1405664


Anatomical context of BRN 1405664


Associations of BRN 1405664 with other chemical compounds


Gene context of BRN 1405664

  • The activities of Z-Phe-Arg-NMec(ZPA) hydrolase, cathepsin B and cathepsin H and the concentration of endogenous thiol protease inhibitor in fibroblasts from patients with galactosialidosis were found not to be significantly different from those in control fibroblasts [25].
  • For this purpose GST was linked via a flexible spacer to the C-terminus of the thiol-protease inhibitor cystatin, whose binding properties for papain were to be studied [26].
  • The calcium-induced release of alpha-actinin was not diminished in the muscle with in vivo-injection of a thiol protease inhibitor, E-64-c. Intramuscular concentrations of E-64-c were also measured after pulse labeling with [3H]E-64-c followed by subcellular fractionation [27].
  • By employing a cell penetrating thiol protease inhibitor, EST: ethyl(+)-(2S,3S)-3-[(S)-3-methyl-1-(3-methylbutylcarbamoyl)buty lcarbamoyl]- 2-oxiranecarboxylate, the role of calpain, a major thiol protease in platelets, on 20K protein (myosin light chain) phosphorylation was examined in intact human platelets [15].
  • The cathepsin B and L substrate Z-Phe-Arg-NMec was similarly degraded by all species, and activity was abolished by the cysteine proteinase inhibitor E-64 [28].

Analytical, diagnostic and therapeutic context of BRN 1405664


  1. A thiol protease inhibitor released from cultured human malignant melanoma cells. Nishida, Y., Sumi, H., Mihara, H. Cancer Res. (1984) [Pubmed]
  2. Antiviral effects of a thiol protease inhibitor on foot-and-mouth disease virus. Kleina, L.G., Grubman, M.J. J. Virol. (1992) [Pubmed]
  3. Role of the Entamoeba histolytica cysteine proteinase in amebic liver abscess formation in severe combined immunodeficient mice. Stanley, S.L., Zhang, T., Rubin, D., Li, E. Infect. Immun. (1995) [Pubmed]
  4. Age-related changes and tissue distribution of parvalbumin in normal and dystrophic mice of strain 129 ReJ. Greaves, D.S., Dufresne, M.J., Fackrell, H.B., Warner, A.H. Muscle Nerve (1991) [Pubmed]
  5. Olfactory discrimination learning is blocked by leupeptin, a thiol protease inhibitor. Stäubli, U., Baudry, M., Lynch, G. Brain Res. (1985) [Pubmed]
  6. Dynorphin converting enzyme with unusual specificity from rat brain. Devi, L., Goldstein, A. Proc. Natl. Acad. Sci. U.S.A. (1984) [Pubmed]
  7. The 1.8-A crystal structure of human tear lipocalin reveals an extended branched cavity with capacity for multiple ligands. Breustedt, D.A., Korndörfer, I.P., Redl, B., Skerra, A. J. Biol. Chem. (2005) [Pubmed]
  8. Degradation of epidermal growth factor receptor in rat liver. Membrane topology through the lysosomal pathway. Renfrew, C.A., Hubbard, A.L. J. Biol. Chem. (1991) [Pubmed]
  9. Yeast cysteine proteinase gene ycp1 induces resistance to bleomycin in mammalian cells. Pei, Z., Calmels, T.P., Creutz, C.E., Sebti, S.M. Mol. Pharmacol. (1995) [Pubmed]
  10. Complex interactions between polyamines and calpain-mediated proteolysis in rat brain. Najm, I., Vanderklish, P., Etebari, A., Lynch, G., Baudry, M. J. Neurochem. (1991) [Pubmed]
  11. CD83 localization in a recycling compartment of immature human monocyte-derived dendritic cells. Klein, E., Koch, S., Borm, B., Neumann, J., Herzog, V., Koch, N., Bieber, T. Int. Immunol. (2005) [Pubmed]
  12. Effect of E-64, a thiol protease inhibitor, on antibody formation in mice. Amamoto, T., Okazaki, T., Komurasaki, T., Hanada, K., Omura, S. Biochem. Biophys. Res. Commun. (1984) [Pubmed]
  13. Calpain inhibitors and serine protease inhibitors can produce apoptosis in HL-60 cells. Lu, Q., Mellgren, R.L. Arch. Biochem. Biophys. (1996) [Pubmed]
  14. The insulin-induced down-regulation of IRS-1 in 3T3-L1 adipocytes is mediated by a calcium-dependent thiol protease. Smith, L.K., Rice, K.M., Garner, C.W. Mol. Cell. Endocrinol. (1996) [Pubmed]
  15. Studies on myosin light chain phosphorylation in intact platelets, utilizing a cell-penetrating thiol protease inhibitor. Tsujinaka, T., Kajiwara, Y., Kambayashi, J., Sakon, M., Mori, T. Thromb. Res. (1988) [Pubmed]
  16. Effect of starvation or treatment with corticosterone on the amount of easily releasable myofilaments in rat skeletal muscles. Dahlmann, B., Rutschmann, M., Reinauer, H. Biochem. J. (1986) [Pubmed]
  17. Localization and inhibition of calcium-activated neutral protease (CANP) in primate skeletal muscle and peripheral nerve. Badalamente, M.A., Hurst, L.C., Stracher, A. Exp. Neurol. (1987) [Pubmed]
  18. Suppression of calcium-induced removal of the Z-line by a thiol-protease inhibitor, E-64-c. Ishiura, S., Nonaka, I., Sugita, H. J. Biochem. (1981) [Pubmed]
  19. Experimental approach to a role of the increased T-kininogen level in carrageenin-induced pleurisy of rats. Oh-ishi, S., Tsuji, N., Hayashi, I. Jpn. J. Pharmacol. (1989) [Pubmed]
  20. Abrogation of the invasion of human bladder tumor cells by using protease inhibitor(s). Redwood, S.M., Liu, B.C., Weiss, R.E., Hodge, D.E., Droller, M.J. Cancer (1992) [Pubmed]
  21. Subcellular localization, partial purification, and characterization of a dynorphin processing endopeptidase from bovine pituitary. Devi, L., Gupta, P., Fricker, L.D. J. Neurochem. (1991) [Pubmed]
  22. Effects of protease inhibitors on postischemic recovery of the heart. Shibata, T., Yamamoto, F., Suehiro, S., Kinoshita, H. Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy. (1997) [Pubmed]
  23. Unfolding during urea denaturation of a low molecular weight phytocystatin (thiol protease inhibitor) purified from Phaseolus mungo (Urd). Sharma, S., Rashid, F., Bano, B. Protein Pept. Lett. (2006) [Pubmed]
  24. Evidence for the probable oil body association of a thiol-protease, leading to oleosin degradation in sunflower seedling cotyledons. Vandana, S., Bhatla, S.C. Plant Physiol. Biochem. (2006) [Pubmed]
  25. Involvement of thiol proteases in galactosialidosis. Takeda, E., Kuroda, Y., Toshima, K., Naito, E., Ito, M., Miyao, M., Kominami, E., Katunuma, N. Clin. Chim. Acta (1986) [Pubmed]
  26. Glutathione S-transferase can be used as a C-terminal, enzymatically active dimerization module for a recombinant protease inhibitor, and functionally secreted into the periplasm of Escherichia coli. Tudyka, T., Skerra, A. Protein Sci. (1997) [Pubmed]
  27. The effect of an in vivo-injected thiol protease inhibitor, E-64-c, on the calcium-induced degeneration of myofilaments. Ishiura, S., Hanada, K., Tamai, M., Kashiwagi, K., Sugita, H. J. Biochem. (1981) [Pubmed]
  28. Schistosoma japonicum, S. mansoni, S. haematobium, S. intercalatum, and S. rodhaini: cysteine-class cathepsin activities in the vomitus of adult worms. Caffrey, C.R., Rheinberg, C.E., Moné, H., Jourdane, J., Li, Y.L., Ruppel, A. Parasitol. Res. (1997) [Pubmed]
  29. Purification, molecular cloning, and sequencing of salivary cystatin SA-1. Al-Hashimi, I., Dickinson, D.P., Levine, M.J. J. Biol. Chem. (1988) [Pubmed]
  30. Metabolic fate of loxistatin in rat. Fukushima, K., Arai, M., Tamai, M., Yokoo, C., Murata, M., Suwa, T., Satoh, T. Xenobiotica (1990) [Pubmed]
  31. Purification and partial characterization of thiol protease inhibitors from embryos of the brine shrimp Artemia. Warner, A.H., Sonnenfeld-Karcz, M.J. Biochem. Cell Biol. (1992) [Pubmed]
  32. Cytoplasmic accumulations in rat primary brain cell cultures following treatment with E-64, a thiol protease inhibitor. Matsui, K., Shirasawa, N., Eto, Y. Dev. Neurosci. (1990) [Pubmed]
  33. Improved purification and some properties of bovine lysosomal carboxypeptidase B. Lipperheide, C., Otto, K. Biochim. Biophys. Acta (1986) [Pubmed]
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