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BioMed Central, Parasites and Vectors, 1(2), p. 29

DOI: 10.1186/1756-3305-2-29

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

Journal article published in 2009 by Dietmar Steverding ORCID, Xia Wang
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

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.