Identification of novel inhibitors of UDP-Glc4/-epimerase, a validated drug target for african sleeping sickness

M. D. Urbaniak, Jioji Natadra Tabudravu, A. Msaki, K. Mansfield Matera, R. Brenk, Marcel Jaspars, M. A. J. Ferguson

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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 pages3
JournalBioorganic & Medicinal Chemistry
Volume16
DOIs
Publication statusPublished - 2006

Keywords

  • epimerase
  • UDP-Glc 4 '-epimerase
  • UDP-glucose
  • UDP-galactose
  • Trypanosoma brucei
  • trypanosome
  • POLY-N-ACETYLLACTOSAMINE
  • TRYPANOSOMA-BRUCEI
  • GALACTOSE METABOLISM
  • GLYCOSYLATION
  • GLYCOPROTEINS

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