| Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness. | |
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MedLine Citation:
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PMID: 16962325 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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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Authors:
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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:
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Type: Journal Article; Research Support, Non-U.S. Gov't; Validation Studies Date: 2006-09-07 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 16 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2006 Nov |
Date Detail:
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Created Date: 2006-10-09 Completed Date: 2007-01-03 Revised Date: 2007-08-13 |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 5744-7 Citation Subset: IM |
Affiliation:
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Division of Biological Chemistry and Molecular Microbiology, School of Life Sciences, University of Dundee, Dundee DD1 5EH, Scotland, UK. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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071463//Wellcome Trust |
| Chemical | |
Reg. No./Substance:
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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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