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CA-074, But Not Its Methyl Ester CA-074Me, Is a Selective Inhibitor of Cathepsin B within Living Cells
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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Cited by
Rajamäki, K., Lappalainen, J., Öörni, K., Välimäki, E., Matikainen, S., Kovanen, P. T., & Eklund, K. K. (2010) · PLoS ONE · doi:10.1371/journal.pone.0011765 · Cited by 1,039
Inflammasome-derived IL-1β production induces nitric oxide–mediated resistance to Leishmania
Lima-Junior, D. S., Costa, D. L., Carregaro, V., Cunha, L. D., Silva, A. L. N., Mineo, T. W. P., Gutierrez, F. R. S., Bellio, M., Bortoluci, K. R., Flavell, R. A., et al. (2013) · Nature Medicine · doi:10.1038/nm.3221 · Cited by 360
Multiple cathepsins promote pro-IL-1β synthesis and NLRP3-mediated IL-1β activation
Orlowski, G. M., Colbert, J. D., Sharma, S., Bogyo, M., Robertson, S. A., & Rock, K. L. (2015) · The Journal of Immunology · doi:10.4049/jimmunol.1500509 · Cited by 268
Sun, B., Zhou, Y., Halabisky, B., Lo, I., Cho, S.-H., Mueller-Steiner, S., Devidze, N., Wang, X., Grubb, A., & Gan, L. (2008) · Neuron · doi:10.1016/j.neuron.2008.10.001 · Cited by 231
The role of lysosomal cysteine cathepsins in NLRP3 inflammasome activation
Campden, R. I., & Zhang, Y. (2019) · Archives of Biochemistry and Biophysics · doi:10.1016/j.abb.2019.02.015 · Cited by 203
Metadata
- Authors
- Montaser, M., Lalmanach, G., & Mach, L.
- Venue
- Biological Chemistry
- Publisher
- Walter de Gruyter GmbH
- Published
- 2002-01-27
- Volume
- 383
- Issue
- 7-8
- Pages
- 1305-8
- ISSN
- 1431-6730 (ISSN-L)
- OpenAlex
- W2158764891
- Cited by
- 167
- References
- 0
- FWCI
- 1.19
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: CA-074, But Not Its Methyl Ester CA-074Me, Is a Selective Inhibitor of Cathepsin B within Living Cells. https://app.cochat.ai/papers/10.1515/bc.2002.147
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- Montaser, M., Lalmanach, G., & Mach, L. (2002). CA-074, But Not Its Methyl Ester CA-074Me, Is a Selective Inhibitor of Cathepsin B within Living Cells. Biological Chemistry. https://doi.org/10.1515/bc.2002.147
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