Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase.
5'-O-[N-(L-glutamyl)-sulfamoyl] adenosine is a potent competitive inhibitor of E. coli glutamyl-tRNA synthetase with respect to glutamic acid (K(i) = 2.8 nM) and is the best inhibitor of this enzyme. It is a weaker inhibitor of mammalian glutamyl-tRNA synthetase (K(i) = 70 nM). The corresponding 5'-O-[N-(L-pyroglutamyl)-sulfamoyl] adenosine is a weak inhibitor (K(i) = 15 microM) of the E. coli enzyme.
Bernier
Stéphane
S
Département de chimie, Faculté des sciences et de génie, Centre de recherche sur la fonction, la structure et l'ingénierie des protéines (CREFSIP), Université Laval, Québec, Canada G1K 7P4.
Dubois
Daniel Y
DY
Habegger-Polomat
Charlotte
C
Gagnon
Louis-Patrick
LP
Lapointe
Jacques
J
Chênevert
Robert
R
D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004926:Escherichia coli / Q000201:enzymology*; D005975:Glutamate-tRNA Ligase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008099:Liver / Q000201:enzymology; D051379:Mice; D012352:RNA, Transfer, Glu / Q000378:metabolism; D013379:Substrate Specificity
D004791:Enzyme Inhibitors; D012352:RNA, Transfer, Glu; D005975:Glutamate-tRNA Ligase; D000241:Adenosine