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Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase

Nakazawa Hewitt, Stephen; Dranow, David M.; Horst, Benjamin G.; Abendroth, Jan A.; Forte, Barbara; Hallyburton, Irene; Jansen, Chimed; Baragana, Beatriz; Choi, Ryan; Lehane, Adele; Rivas, Kasey L.; Kirk, Kiaran; Fairlamb, Alan H.


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...[Show more]

CollectionsANU Research Publications
Date published: 2016-10-31
Type: Journal article
Source: ACS Infectious Diseases
DOI: 10.1021/acsinfecdis.6b00078
Access Rights: Open Access


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