Article
Inhibition of methionyl-tRNA synthetase by REP8839 and effects of resistance mutations on enzyme activity.
Antimicrobial agents and chemotherapy - 1 Jan 2009
Green Louis S, Bullard James M, Ribble Wendy, Dean Frank, Ayers David F, Ochsner Urs A, Janjic Nebojsa, Jarvis Thale C
Abstract excerpt
REP8839 is a selective inhibitor of methionyl-tRNA synthetase (MetRS) with antibacterial activity against a variety of gram-positive organisms. We determined REP8839 potency against Staphylococcus aureus MetRS and assessed its selectivity for bacterial versus human orthologs of MetRS. The inhibition constant (K(i)) of REP8839 was 10 pM for Staphylococcus aureus MetRS. Inhibition of MetRS by REP8839 was...
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