Document Detail


Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness.
MedLine Citation:
PMID:  16962325     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Michael D Urbaniak; Jioji N Tabudravu; Aichi Msaki; Kathy Mansfield Matera; Ruth Brenk; Marcel Jaspars; Michael A J Ferguson
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Validation Studies     Date:  2006-09-07
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  16     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2006 Nov 
Date Detail:
Created Date:  2006-10-09     Completed Date:  2007-01-03     Revised Date:  2007-08-13    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  5744-7     Citation Subset:  IM    
Affiliation:
Division of Biological Chemistry and Molecular Microbiology, School of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, UK.
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MeSH Terms
Descriptor/Qualifier:
Animals
Enzyme Inhibitors / chemistry,  pharmacology*
Humans
Models, Chemical
Trypanocidal Agents / chemistry,  pharmacology*,  therapeutic use
Trypanosoma brucei brucei / drug effects*,  growth & development
Trypanosomiasis, African / drug therapy*
UDPglucose 4-Epimerase / antagonists & inhibitors*
Grant Support
ID/Acronym/Agency:
071463//Wellcome Trust
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Trypanocidal Agents; EC 5.1.3.2/UDPglucose 4-Epimerase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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