CA-074, but not its methyl ester CA-074Me,is a selective inhibitor of cathepsin B within living cells |
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Authors: | Montaser Metwally Lalmanach Gilles Mach Lukas |
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Affiliation: | Zentrum für Angewandte Genetik, Universit?t für Bodenkultur Wien, Austria. |
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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. |
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