Identification of novel inhibitors of UDP-Glc 4 '-epimerase, a validated drug target for African sleeping sickness

Michael D. Urbaniak, Jioji N. Tabudravu, Aichi Msaki, Kathy Mansfield Matera, Ruth Brenk, Marcel Jaspars, Michael A. J. Ferguson

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    30 Citations (Scopus)

    Abstract

    Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells. (c) 2006 Elsevier Ltd. All rights reserved.

    Original languageEnglish
    Pages (from-to)5744-5747
    Number of pages4
    JournalBioorganic & Medicinal Chemistry Letters
    Volume16
    Issue number22
    DOIs
    Publication statusPublished - 15 Nov 2006

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