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Steverding, Dietmar and Wang, Xia 
ORCID: https://orcid.org/0000-0001-6915-2588
(2009)
Typanocidal activity of the proteasome inhibitor and anti-cancer drug bortezomib.
Parasites & Vectors, 2.
ISSN 1756-3305
Abstract
The proteasome inhibitor and anti-cancer drug bortezomib was tested for in vitro activity against bloodstream forms of Trypanosoma brucei. The concentrations of bortezomib required to reduce the growth rate by 50% and to kill all trypanosomes were 3.3 nM and 10 nM, respectively. In addition, bortezomib was 10 times more toxic to trypanosomes than to human HL-60 cells. Moreover, exposure of trypanosomes to 10 nM bortezomib for 16 h was enough to kill 90% of the parasites following incubation in fresh medium. However, proteasomal peptidase activities of trypanosomes exposed to bortezomib were only inhibited by 10% and 30% indicating that the proteasome is not the main target of the drug. The results suggest that bortezomib may be useful as drug for the treatment of human African trypanosomiasis.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being |
| 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: | EPrints Services |
| Date Deposited: | 25 Nov 2010 11:13 |
| Last Modified: | 17 Nov 2024 07:30 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/15094 |
| DOI: | 10.1186/1756-3305-2-29 |
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