Ontology highlight
ABSTRACT:
SUBMITTER: Hewitt SN
PROVIDER: S-EPMC5241706 | biostudies-literature | 2017 Jan
REPOSITORIES: biostudies-literature
Hewitt Stephen Nakazawa SN Dranow David M DM Horst Benjamin G BG Abendroth Jan A JA Forte Barbara B Hallyburton Irene I Jansen Chimed C Baragaña Beatriz B Choi Ryan R Rivas Kasey L KL Hulverson Matthew A MA Dumais Mitchell M Edwards Thomas E TE Lorimer Donald D DD Fairlamb Alan H AH Gray David W DW Read Kevin D KD Lehane Adele M AM Kirk Kiaran K Myler Peter J PJ Wernimont Amy A Walpole Chris C Stacy Robin R Barrett Lynn K LK Gilbert Ian H IH Van Voorhis Wesley C WC
ACS infectious diseases 20161116 1
Plasmodium falciparum (Pf) prolyl-tRNA synthetase (ProRS) is one of the few chemical-genetically validated drug targets for malaria, yet highly selective inhibitors have not been described. In this paper, approximately 40,000 compounds were screened to identify compounds that selectively inhibit PfProRS enzyme activity versus Homo sapiens (Hs) ProRS. X-ray crystallography structures were solved for apo, as well as substrate- and inhibitor-bound forms of PfProRS. We identified two new inhibitors ...[more]