Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362

[Image: see text] Plasmepsin X (PMX) is an essential aspartyl protease controlling malaria parasite egress and invasion of erythrocytes, development of functional liver merozoites (prophylactic activity), and blocking transmission to mosquitoes, making it a potential multistage drug target. We repor...

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Autores principales: Lowe, Martin A., Cardenas, Alvaro, Valentin, Jean-Pierre, Zhu, Zhaoning, Abendroth, Jan, Castro, Jose L., Class, Reiner, Delaunois, Annie, Fleurance, Renaud, Gerets, Helga, Gryshkova, Vitalina, King, Lloyd, Lorimer, Donald D., MacCoss, Malcolm, Rowley, Julian H., Rosseels, Marie-Luce, Royer, Leandro, Taylor, Richard D., Wong, Melanie, Zaccheo, Oliver, Chavan, Vishal P., Ghule, Gokul A., Tapkir, Bapusaheb K., Burrows, Jeremy N., Duffey, Maëlle, Rottmann, Matthias, Wittlin, Sergio, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Striepen, Josefine, Fairhurst, Kate J., Yeo, Tomas, Fidock, David A., Cowman, Alan F., Favuzza, Paola, Crespo-Fernandez, Benigno, Gamo, Francisco Javier, Goldberg, Daniel E., Soldati-Favre, Dominique, Laleu, Benoît, de Haro, Teresa
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9620073/
https://www.ncbi.nlm.nih.gov/pubmed/36216349
http://dx.doi.org/10.1021/acs.jmedchem.2c01336

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