Glutamylsulfamoyladenosine and pyroglutamylsulfamoyladenosine are competitive inhibitors of E. coli glutamyl-tRNA synthetase

J Enzyme Inhib Med Chem. 2005 Feb;20(1):61-7. doi: 10.1080/14756360400002007.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / chemical synthesis
  • Adenosine / pharmacology
  • Animals
  • Binding Sites
  • Binding, Competitive
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Escherichia coli / enzymology*
  • Glutamate-tRNA Ligase / antagonists & inhibitors*
  • Glutamate-tRNA Ligase / metabolism
  • Liver / enzymology
  • Mice
  • RNA, Transfer, Glu / metabolism
  • Substrate Specificity

Substances

  • Enzyme Inhibitors
  • RNA, Transfer, Glu
  • Glutamate-tRNA Ligase
  • Adenosine