2. Academic Validation
  3. Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness

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

  • Bioorg Med Chem Lett. 2006 Nov 15;16(22):5744-7. doi: 10.1016/j.bmcl.2006.08.091.
Michael D Urbaniak 1,  Jioji N Tabudravu,  Aichi Msaki,  Kathy Mansfield Matera,  Ruth Brenk,  Marcel Jaspars,  Michael A J Ferguson
Affiliations

Affiliation

  • 1 Division of Biological Chemistry and Molecular Microbiology, School of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, UK.
PMID: 16962325 DOI: 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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