Proteasome inhibitors: The next generation of antimalarial drugs?

Proteasome inhibitors: The next generation of antimalarial drugs?
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蛋白酶体抑制剂:下一代抗疟药?

DOI:
10.1016/j.chembiol.2023.04.013
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发表时间:
2023
影响因子:
8.6
通讯作者:
Rosenthal,PhilipJ
Rosenthal,PhilipJ
中科院分区:
生物学1区
文献类型:
--
作者:
Rosenthal,PhilipJ

文献摘要

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恶性疟原虫蛋白酶体是新型抗疟药物的一个有希望的靶点。多种抑制剂已显示出有效的抗疟活性和与青蒿素的协同作用。强有力的不可逆肽乙烯砜提供协同作用,最小的阻力选择,和缺乏交叉阻力。这些和其他蛋白酶体抑制剂有望成为新的联合抗疟方案的组成部分。
Among promising targets for new antimalarials is thePlasmodium falciparumproteasome. 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.