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Biol Chem. 2002 Jul-Aug;383(7-8):1305-8.

CA-074, but not its methyl ester CA-074Me, is a selective inhibitor of cathepsin B within living cells.

Author information

1
Zentrum für Angewandte Genetik, Universität für Bodenkultur Wien, Austria.

Abstract

Studies using inhibitors that reportedly discriminate between cathepsin B and related lysosomal cysteine proteinases have implicated the enzyme in a wide range of physiological and pathological processes. The most popular substance to selectively inhibit cathepsin B in vivo is CA-074Me, the methyl ester of the E-64 derivative CA-074. However, we now have found that CA-074Me inactivates both cathepsin B and cathepsin L within murine fibroblasts. In contrast, exposure of these cells to the parental compound CA-074 leads to the selective inhibition of endogenous cathepsin B, while intracellular cathepsin L remains unaffected. These results indicate that CA-074 rather than CA-074Me should be used to specifically inactivate cathepsin B within living cells.

PMID:
12437121
DOI:
10.1515/BC.2002.147
[Indexed for MEDLINE]

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