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 and Medicinal Chemistry Letters, 16 (22). pp. 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
Journal or Publication Title:
Bioorganic and Medicinal Chemistry Letters
Uncontrolled Keywords:
/dk/atira/pure/subjectarea/asjc/1300/1308
Subjects:
ID Code:
66397
Deposited By:
Deposited On:
17 Sep 2013 08:08
Refereed?:
Yes
Published?:
Published
Last Modified:
26 May 2020 03:18