Synthesis of glutaminyl adenylate analogues that are inhibitors of glutaminyl-tRNA synthetase.
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.
Bernier
S
S
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.
Dubois
D Y
DY
Therrien
M
M
Lapointe
J
J
Chênevert
R
R
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
D004791:Enzyme Inhibitors; D000604:Amino Acyl-tRNA Synthetases; C020659:glutaminyl-tRNA synthetase; D000225:Adenine