Department of Microbiology and Parasitology, Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences & School of Basic Medicine, Peking Union Medical College, 5# Dong Dan San Tiao, Beijing, 100005, China.
Chem Commun (Camb). 2019 Aug 7;55(64):9535-9538. doi: 10.1039/c9cc03719e.
Endoperoxide-containing antimalarials, such as artemisinin and the synthetic trioxolane OZ439, are prodrugs activated by heme to generate primary and secondary carbon-centered radicals. We employed activity-based protein profiling (ABPP) to show that the secondary-carbon-centered radical of 1,2,4-trioxolanes is primarily responsible for protein labeling in malaria parasites.
含内过氧化物的抗疟药物，如青蒿素和合成的三氧杂环烷 OZ439，是前药，通过血红素激活生成初级和次级碳中心自由基。我们采用基于活性的蛋白质谱分析（ABPP）表明，1,2,4-三氧杂环烷的次级碳中心自由基主要负责疟原虫中的蛋白质标记。
