Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance

We describe noncovalent, reversible asparagine ethylenediamine (AsnEDA) inhibitors of the Plasmodium falciparum proteasome (Pf20S) β5 subunit that spare all active subunits of human constitutive and immuno-proteasomes. The compounds are active against erythrocytic, sexual, and liver-stage parasites,...

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Detalles Bibliográficos
Autores principales: Kirkman, Laura A., Zhan, Wenhu, Visone, Joseph, Dziedziech, Alexis, Singh, Pradeep K., Fan, Hao, Tong, Xinran, Bruzual, Igor, Hara, Ryoma, Kawasaki, Masanori, Imaeda, Toshihiro, Okamoto, Rei, Sato, Kenjiro, Michino, Mayako, Alvaro, Elena Fernandez, Guiang, Liselle F., Sanz, Laura, Mota, Daniel J., Govindasamy, Kavitha, Wang, Rong, Ling, Yan, Tumwebaze, Patrick K., Sukenick, George, Shi, Lei, Vendome, Jeremie, Bhanot, Purnima, Rosenthal, Philip J., Aso, Kazuyoshi, Foley, Michael A., Cooper, Roland A., Kafsack, Bjorn, Doggett, J. Stone, Nathan, Carl F., Lin, Gang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Academy of Sciences 2018
Materias:
PNAS Plus
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6055138/
https://www.ncbi.nlm.nih.gov/pubmed/29967165
http://dx.doi.org/10.1073/pnas.1806109115

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