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Trypanosoma brucei: Inhibition of cathepsin L is sufficient to kill bloodstream forms.
Molecular and Biochemical Parasitology ( IF 1.5 ) Pub Date : 2019-11-16 , DOI: 10.1016/j.molbiopara.2019.111246
Dietmar Steverding 1 , Stuart A Rushworth 1 , Bogdan I Florea 2 , Herman S Overkleeft 2
Affiliation  

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.



中文翻译:

布氏锥虫:组织蛋白酶L的抑制作用足以杀死血流形式。

布氏锥虫的溶酶体半胱氨酸蛋白酶活性包括组织蛋白酶B酶(Tb CATB)和组织蛋白酶L酶(Tb CATL)。半胱氨酸蛋白酶活性的抑制对血流形式的锥虫是致命的,但是尚不清楚两种酶中的哪一种对于寄生虫的生存至关重要。在这里,我们显示乙烯基砜化合物LU-102选择性抑制Tb CATL,而不会影响Tb CATB和锥虫体内的蛋白酶体类胰蛋白酶样活性。因此,LU-102表现出的锥虫杀虫活性可仅归因于对Tb CATL的抑制,表明该酶对布鲁氏杆菌的生存至关重要

更新日期:2019-11-16
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