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

Urbaniak, Michael D., Tabudravu, Jioji orcid iconORCID: 0000-0002-6930-6572, Msaki, Aichi, Matera, Kathy Mansfield, Brenk, Ruth, Jaspars, Marcel and Ferguson, Michael A.J. (2006) Identification of novel inhibitors of UDP-Glc 4′-epimerase, a validated drug target for african sleeping sickness. Bioorganic & Medicinal Chemistry Letters, 16 (22). pp. 5744-5747. ISSN 0960-894X

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Official URL: https://doi.org/10.1016/j.bmcl.2006.08.091

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.


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