Abstract
The lysosomal cysteine protease activity of Trypanosoma brucei comprises a cathepsin B enzyme (TbCATB) and a cathepsin L enzyme (TbCATL). Inhibition of the cysteine protease activity is lethal to bloodstream-form trypanosomes but it was not entirely clear which of the two enzymes are essential for survival of the parasites. Here we show that the vinyl sulfone compound LU-102 selectively inhibits TbCATL without affecting TbCATB and the proteasomal trypsin-like activity within trypanosomes. Therefore, the trypanocidal activity displayed by LU-102 can be attributed solely to the inhibition of TbCATL demonstrating that this enzyme is essential to the survival of T. brucei.
Original language | English |
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Article number | 111246 |
Number of pages | 4 |
Journal | Molecular and Biochemical Parasitology |
Volume | 235 |
Early online date | 16 Nov 2019 |
DOIs | |
Publication status | Published - Jan 2020 |
Profiles
-
Stuart Rushworth
- Norwich Medical School - Professor
- Metabolic Health - Director
- Cancer Studies - Member
Person: Research Group Member, Academic, Teaching & Research