Trypanocidal activity of peptidyl vinyl ester derivatives selective for inhibition of mammalian proteasome trypsin-like activity

Dietmar Steverding, Anna Baldisserotto, Xia Wang, Mauro Marastoni

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    13 Citations (Scopus)

    Abstract

    Nine vinyl ester tripeptides selective for inhibition of mammalian proteasome trypsin-like activity were tested for in vitro activity against Trypanosoma brucei. Interestingly, two compounds showed trypanocidal activity in the low micromolar range without displaying cytotoxicity against human cells. However, the compounds did not inhibit the trypsin-like activity of the trypanosome proteasome although their effect correlates with inactivation of the chymotrypsin-like activity. This finding shows that the inhibitor sensitivities between mammalian and trypanosome proteasome are distinct. This difference may be exploited for rational anti-trypanosomal drug development.
    Original languageEnglish
    Pages (from-to)444-447
    Number of pages4
    JournalExperimental Parasitology
    Volume128
    Issue number4
    DOIs
    Publication statusPublished - Aug 2011

    Keywords

    • Proteasome
    • Sleeping sickness
    • Trypanosoma brucei
    • Vinyl ester tripeptides

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