Ontology highlight
ABSTRACT:
SUBMITTER: Torrie LS
PROVIDER: S-EPMC5663395 | biostudies-literature | 2017 Oct
REPOSITORIES: biostudies-literature
Torrie Leah S LS Brand Stephen S Robinson David A DA Ko Eun Jung EJ Stojanovski Laste L Simeons Frederick R C FRC Wyllie Susan S Thomas John J Ellis Lucy L Osuna-Cabello Maria M Epemolu Ola O Nühs Andrea A Riley Jennifer J MacLean Lorna L Manthri Sujatha S Read Kevin D KD Gilbert Ian H IH Fairlamb Alan H AH De Rycker Manu M
ACS infectious diseases 20171002 10
Methionyl-tRNA synthetase (MetRS) has been chemically validated as a drug target in the kinetoplastid parasite Trypanosoma brucei. In the present study, we investigate the validity of this target in the related trypanosomatid Leishmania donovani. Following development of a robust high-throughput compatible biochemical assay, a compound screen identified DDD806905 as a highly potent inhibitor of LdMetRS (K<sub>i</sub> of 18 nM). Crystallography revealed this compound binds to the methionine pocke ...[more]