Nucleoside triphosphate mimicry: a sugar triazolyl nucleoside as an ATP-competitive inhibitor of B. anthracis pantothenate kinase

The synthesis of a library of nucleoside triphosphate mimetics is described where the Mg(2+) chelated triphosphate sidechain is replaced by an uncharged methylene-triazole linked monosaccharide sidechain. The compounds have been evaluated as inhibitors of Bacillus anthracis pantothenate kinase and a...

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Veröffentlicht in:	Organic & biomolecular chemistry 2009-10, Vol.7 (19), p.4029-4036
Hauptverfasser:	Rowan, Andrew S, Nicely, Nathan I, Cochrane, Nicola, Wlassoff, Wjatschesslaw A, Claiborne, Al, Hamilton, Chris J
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphate - metabolism Bacillus anthracis - enzymology Binding, Competitive Biomimetics Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Kinetics Nucleosides - chemistry Phosphotransferases (Alcohol Group Acceptor) - antagonists & inhibitors Phosphotransferases (Alcohol Group Acceptor) - metabolism Polyphosphates - chemical synthesis Polyphosphates - chemistry Polyphosphates - metabolism Polyphosphates - pharmacology Triazoles - chemistry
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Beschreibung
Zusammenfassung:	The synthesis of a library of nucleoside triphosphate mimetics is described where the Mg(2+) chelated triphosphate sidechain is replaced by an uncharged methylene-triazole linked monosaccharide sidechain. The compounds have been evaluated as inhibitors of Bacillus anthracis pantothenate kinase and a competitive inhibitor has been identified with a K(i) that is 3-fold lower than the K(m) value of ATP.
ISSN:	1477-0520 1477-0539
DOI:	10.1039/b909729e