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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Detalhes bibliográficos
Publicado no:Proc Natl Acad Sci U S A
Main Authors: 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: Artigo
Idioma:Inglês
Publicado em: National Academy of Sciences 2018
Assuntos:
PNAS Plus
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6055138/
https://ncbi.nlm.nih.gov/pubmed/29967165
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1806109115
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