title: Synthesis of glutaminyl adenylate analogues that are inhibitors of glutaminyl-tRNA synthetase.
abstract: Glutaminol adenylate 5 is a competitive inhibitor of glutaminyl-tRNA synthetase with respect to glutamine (Ki = 280 nM) and to ATP (Ki = 860 nM). The corresponding methyl phosphate ester 4 is a weaker inhibitor (Ki approximately 10 microM) with respect to glutamine.
authors.affiliation: Département de Chimie, Centre de Recherche sur la Fonction, la Structure et l'Ingénierie des Protéines (CREFSIP), Faculté des Sciences et de Génie, Université Laval, Québec, Canada.
authors.forename: S
authors.initials: S
authors.lastname: Bernier
authors.forename: D Y
authors.initials: DY
authors.lastname: Dubois
authors.forename: M
authors.initials: M
authors.lastname: Therrien
authors.forename: J
authors.initials: J
authors.lastname: Lapointe
authors.forename: R
authors.initials: R
authors.lastname: Chênevert
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000604:Amino Acyl-tRNA Synthetases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D007700:Kinetics; D015394:Molecular Structure
chemical_list: D004791:Enzyme Inhibitors; D000604:Amino Acyl-tRNA Synthetases; C020659:glutaminyl-tRNA synthetase; D000225:Adenine