Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome

The Plasmodium falciparum proteasome is a potential antimalarial drug target. We have identified a series of amino-amide boronates that are potent and specific inhibitors of the P. falciparum 20S proteasome (Pf20S) β5 active site and that exhibit fast-acting antimalarial activity. They selectively i...

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Detalles Bibliográficos
Autores principales: Xie, Stanley C., Metcalfe, Riley D., Mizutani, Hirotake, Puhalovich, Tanya, Hanssen, Eric, Morton, Craig J., Du, Yawei, Dogovski, Con, Huang, Shih-Chung, Ciavarri, Jeffrey, Hales, Paul, Griffin, Robert J., Cohen, Lawrence H., Chuang, Bei-Ching, Wittlin, Sergio, Deni, Ioanna, Yeo, Tomas, Ward, Kurt E., Barry, Daniel C., Liu, Boyin, Gillett, David L., Crespo-Fernandez, Benigno F., Ottilie, Sabine, Mittal, Nimisha, Churchyard, Alisje, Ferguson, Daniel, Aguiar, Anna Caroline C., Guido, Rafael V. C., Baum, Jake, Hanson, Kirsten K., Winzeler, Elizabeth A., Gamo, Francisco-Javier, Fidock, David A., Baud, Delphine, Parker, Michael W., Brand, Stephen, Dick, Lawrence R., Griffin, Michael D. W., Gould, Alexandra E., Tilley, Leann
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Academy of Sciences 2021
Materias:
Biological Sciences
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8488693/
https://www.ncbi.nlm.nih.gov/pubmed/34548400
http://dx.doi.org/10.1073/pnas.2107213118

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8488693/
https://www.ncbi.nlm.nih.gov/pubmed/34548400
http://dx.doi.org/10.1073/pnas.2107213118

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