title: Nucleoside triphosphate mimicry: a sugar triazolyl nucleoside as an ATP-competitive inhibitor of B. anthracis pantothenate kinase.
abstract: 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.
authors.affiliation: School of Chemistry and Chemical Engineering, David Keir Building, Stranmillis Road, Queen's University Belfast, Belfast, BT9 5AG.
authors.forename: Andrew S
authors.initials: AS
authors.lastname: Rowan
authors.forename: Nathan I
authors.initials: NI
authors.lastname: Nicely
authors.forename: Nicola
authors.initials: N
authors.lastname: Cochrane
authors.forename: Wjatschesslaw A
authors.initials: WA
authors.lastname: Wlassoff
authors.forename: Al
authors.initials: A
authors.lastname: Claiborne
authors.forename: Chris J
authors.initials: CJ
authors.lastname: Hamilton
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism*; D001408:Bacillus anthracis / Q000201:enzymology*; D001667:Binding, Competitive; D032701:Biomimetics; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D007700:Kinetics; D009705:Nucleosides / Q000737:chemistry*; D017853:Phosphotransferases (Alcohol Group Acceptor) / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011122:Polyphosphates / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D009705:Nucleosides; D011122:Polyphosphates; D014230:Triazoles; D000255:Adenosine Triphosphate; D017853:Phosphotransferases (Alcohol Group Acceptor); C023088:pantothenate kinase; C005692:triphosphoric acid