Protocol for analysis of intracellular conversion of artezomib molecules into new proteasome inhibitors in Plasmodium falciparum parasites.
Protocol for analysis of intracellular conversion of artezomib molecules into new proteasome inhibitors in Plasmodium falciparum parasites.
复制标题
恶性疟原虫寄生虫中阿替佐米分子细胞内转化为新型蛋白酶体抑制剂的分析方案。
DOI：
10.1016/j.xpro.2024.102896
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发表时间：
2024
期刊：
影响因子：
--
通讯作者：
Lin,Gang
中科院分区：
文献类型：
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作者：
Zhan,Wenhu;Liu,YiJing;Kirkman,LauraA;Lin,Gang
Artezomibs (ATZs) 是由青蒿素和寄生虫蛋白酶体抑制剂组成的双药效团分子，劫持寄生虫泛素蛋白酶体系统，在血红素激活青蒿素后转化为新的蛋白酶体抑制剂。1在这里，我们提出了一种使用基于荧光活性的广谱蛋白酶体抑制剂探针来研究 ATZ 分子在疟原虫中细胞内转化为新型蛋白酶体抑制剂的方案。我们描述了药物治疗和清洗、寄生虫裂解、蛋白酶体标记和可视化的步骤。有关该协议的使用和执行的完整详细信息，请参阅 Zhan 等人1
Artezomibs (ATZs), dual-pharmacophore molecules comprising of artemisinin and a parasite proteasome inhibitor, hijack parasite ubiquitin proteasome system to transform into new proteasome inhibitors following the activation of artemisinin by heme.1Here, we present a protocol for using a fluorescent activity-based broad-spectrum proteasome inhibitor probe to study intracellular conversion of ATZ molecules into new proteasome inhibitors in malaria parasites. We describe steps for drug treatment and washout, parasite lysis, proteasome labeling, and visualization.For complete details on the use and execution of this protocol, please refer to Zhan et al.1