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

Urbaniak, Michael D. and Tabudravu, Jioji N. and Msaki, Aichi and Matera, Kathy Mansfield and Brenk, Ruth and 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). 5744 - 5747. ISSN 0960-894X

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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.

Item Type: Journal Article
Additional Information: Journal Supports Open Access
Uncontrolled Keywords: Trypanosome
Subjects: Q Science > QD Chemistry
R Medicine > R Medicine (General)
Divisions: Faculty of Science, Technology and Environment (FSTE) > School of Biological and Chemical Sciences
Depositing User: Repo Editor
Date Deposited: 09 Jun 2017 12:00
Last Modified: 09 Jun 2017 12:00
URI: http://repository.usp.ac.fj/id/eprint/9925
UNSPECIFIED

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