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- W4377014543 abstract "Among promising targets for new antimalarials is the Plasmodium falciparum proteasome. Multiple inhibitors have demonstrated potent antimalarial activity and synergy with artemisinins. Potent irreversible peptide vinyl sulfones offer synergy, minimal resistance selection, and lack of cross-resistance. These and other proteasome inhibitors have promise as components of new combination antimalarial regimens. Among promising targets for new antimalarials is the Plasmodium falciparum proteasome. Multiple inhibitors have demonstrated potent antimalarial activity and synergy with artemisinins. Potent irreversible peptide vinyl sulfones offer synergy, minimal resistance selection, and lack of cross-resistance. These and other proteasome inhibitors have promise as components of new combination antimalarial regimens. Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasomeDeni et al.Cell Chemical BiologyMarch 23, 2023In BriefInhibitors of the Plasmodium falciparum proteasome have emerged as leading antimalarial candidates. Herein, Deni and Stokes et al. profile a range of diverse chemotypes and identify the vinyl sulfone WLL as the least susceptible to resistance, likely attributable to its covalent, irreversible binding to the β2 and β5 catalytic subunits. Full-Text PDF Open Access" @default.
- W4377014543 created "2023-05-19" @default.
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- W4377014543 date "2023-05-01" @default.
- W4377014543 modified "2023-09-28" @default.
- W4377014543 title "Proteasome inhibitors: The next generation of antimalarial drugs?" @default.
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- W4377014543 doi "https://doi.org/10.1016/j.chembiol.2023.04.013" @default.
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