Tools
ToolsSteverding, D (2011) The cathepsin B-selective inhibitors CA-074 and CA-074Me inactivate cathepsin L under reducing conditions. The Open Enzyme Inhibition Journal, 4 (1). pp. 11-16. ISSN 1874-9402
Full text not available from this repository. (Request a copy)Abstract
The inhibitor CA-074 and its membrane-permeable derivative CA-074Me have been widely employed to study the biological function of cathepsin B. These compounds have been described as selective inactivators of cathepsin B with barely detectable action on other cathepsins. However, in this study it is demonstrated that CA-074 and CA-074Me also inactivate cathepsin L in the presence of the thiol reagents dithiothreitol and glutathione. In addition, it is also found that CA-074Me inactivates cathepsin B in the presence of dithiothreitol, an inhibition reaction previously not described. Furthermore, it is shown that CA-074 and CA-074Me are able to inhibit cathepsin L within living HL-60 cells and bloodstream forms of Trypanosoma brucei brucei. For HL-60 cells it is also shown that the inhibition of cathepsin L by the inhibitors is due to the reducing intracellular environment. These results suggest that CA-074 and CA-074Me are not suitable to discriminate between cathepsin B and L in vivo. Accordingly, previous demonstrations of the involvement of cathepsin B in physiological and pathological processes probably need re-evaluation.
| Item Type: | Article |
|---|---|
| Faculty \ School: | Faculty of Medicine and Health Sciences > Norwich Medical School |
| UEA Research Groups: | Faculty of Medicine and Health Sciences > Research Groups > Gastroenterology and Gut Biology |
| Depositing User: | Rhiannon Harvey |
| Date Deposited: | 12 Dec 2011 15:07 |
| Last Modified: | 21 Dec 2022 15:32 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/35697 |
| DOI: | 10.2174/1874940201104010011 |
Actions (login required)
 |
View Item |