Typanocidal activity of the proteasome inhibitor and anti-cancer drug bortezomib

Steverding, Dietmar and Wang, Xia (2009) Typanocidal activity of the proteasome inhibitor and anti-cancer drug bortezomib. Parasites & Vectors, 2. ISSN 1756-3305

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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:	24 Oct 2022 00:29
URI:	https://ueaeprints.uea.ac.uk/id/eprint/15094
DOI:	10.1186/1756-3305-2-29

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