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

Research output: Contribution to journalJournal article

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  • Michael D. Urbaniak
  • Jioji N. Tabudravu
  • Aichi Msaki
  • Kathy Mansfield Matera
  • Ruth Brenk
  • Marcel Jaspars
  • Michael A. J. Ferguson
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<mark>Journal publication date</mark>15/11/2006
<mark>Journal</mark>Bioorganic and Medicinal Chemistry Letters
Issue number22
Volume16
Number of pages4
Pages (from-to)5744-5747
<mark>State</mark>Published
<mark>Original language</mark>English

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.