| Inhibition of L-fucokinase from rat liver by L-fucose analogues in vitro. | |
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MedLine Citation:
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PMID: 9208369 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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By investigating the effects of more than 15 different L-fucose analogues on the activity of L-fucokinase (EC 2.7.1.52) from rat liver in vitro, certain structural requirements for potent inhibition of this enzyme were established. Of the novel compounds, 4,6-dideoxy-L-xylo-hexopyranose (4) and methyl 4,6-dideoxy-4-iodo-L-glucopyranose (9) were found to be competitive inhibitors with Ki-values of 0.5 mM and 5.0 mM respectively. Thus 4,6-dideoxy-L-xylo-hexopyranose is a better inhibitor of L-fucokinase than methyl-alpha-L-fucoside (1). Uptake of L-fucose into rat hepatoma cells is reduced by 52% in the presence of the deoxy derivative (4), leading to a decrease of 45% in the incorporation of L-fucose into total cellular glycoproteins. |
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Authors:
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R Zeitler; S Danneschewski; T Lindhorst; J Thiem; W Reutter |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of enzyme inhibition Volume: 11 ISSN: 8755-5093 ISO Abbreviation: J. Enzym. Inhib. Publication Date: 1997 Feb |
Date Detail:
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Created Date: 1997-08-07 Completed Date: 1997-08-07 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8709734 Medline TA: J Enzyme Inhib Country: SWITZERLAND |
Other Details:
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Languages: eng Pagination: 265-73 Citation Subset: IM |
Affiliation:
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Institut für Molekularbiologie und Biochemie der Freien Universität Berlin, Germany. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Enzyme Inhibitors / pharmacology Fucose / analogs & derivatives*, pharmacology* Guanosine Diphosphate Fucose / biosynthesis Liver / enzymology* Liver Neoplasms, Experimental Phosphotransferases (Alcohol Group Acceptor) / antagonists & inhibitors* Rats Structure-Activity Relationship Tumor Cells, Cultured |
| Chemical | |
Reg. No./Substance:
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0/Enzyme Inhibitors; 15839-70-0/Guanosine Diphosphate Fucose; 3713-31-3/Fucose; EC 2.7.1.-/Phosphotransferases (Alcohol Group Acceptor); EC 2.7.1.52/fucokinase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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