Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors

Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors

Prolyl-tRNA synthetase (PRS) is a clinically validated antimalarial target. Screening of a set of PRS ATP-site binders, initially designed for human indications, led to identification of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives representing a novel antimalarial scaffold. Evidence designates cyto...

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Bibliographic Details
Main Authors: Okaniwa, Masanori, Shibata, Akira, Ochida, Atsuko, Akao, Yuichiro, White, Karen L, Shackleford, David M, Duffy, Sandra, Lucantoni, Leonardo, Dey, Sumanta, Striepen, Josefine, Yeo, Tomas, Mok, Sachel, Aguiar, Anna Caroline C, Sturm, Angelika, Crespo, Benigno, Sanz, Laura M, Churchyard, Alisje, Baum, Jake, Pereira, Dhelio B, Guido, Rafael VC, Dechering, Koen J, Wittlin, Sergio, Uhlemann, Anne-Catrin, Fidock, David A, Niles, Jacquin C, Avery, Vicky M, Charman, Susan A, Laleu, Benoît
Other Authors: Massachusetts Institute of Technology. Department of Biological Engineering
Format: Article
Language:English
Published: American Chemical Society (ACS) 2021
Online Access:https://hdl.handle.net/1721.1/133582

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