Elucidating the path to Plasmodium prolyl-tRNA synthetase inhibitors that overcome halofuginone resistance
oleh: Mark A. Tye, N. Connor Payne, Catrine Johansson, Kritika Singh, Sofia A. Santos, Lọla Fagbami, Akansha Pant, Kayla Sylvester, Madeline R. Luth, Sofia Marques, Malcolm Whitman, Maria M. Mota, Elizabeth A. Winzeler, Amanda K. Lukens, Emily R. Derbyshire, Udo Oppermann, Dyann F. Wirth, Ralph Mazitschek
| Format: | Article |
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| Diterbitkan: | Nature Portfolio 2022-08-01 |
Deskripsi
The development of antimalarials against the human liver and asexual blood stages is one of the top public health challenges. Here, the authors report a single-step biochemical assay for the characterization of prolyl-tRNA synthetase inhibitors, and develop high-affinity inhibitors for the enzyme, including elusive triple-site ligands.