Aix Marseille Univ, CNRS, ICR UMR 7273, Equipe Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 13385 Marseille CEDEX 05, France.
Molecules. 2020 Dec 15;25(24):5949. doi: 10.3390/molecules25245949.
Recent progress in reducing malaria cases and ensuing deaths is threatened by factors like mutations that induce resistance to artemisinin derivatives. Multiple drugs are currently in clinical trials for malaria treatment, including some with novel mechanisms of action. One of these, MMV390048, is a plasmodial kinase inhibitor. This review lists the recently developed molecules which target plasmodial kinases. A systematic review of the literature was performed using CAPLUS and MEDLINE databases from 2005 to 2020. It covers a total of 60 articles and describes about one hundred compounds targeting 22 plasmodial kinases. This work highlights the strong potential of compounds targeting plasmodial kinases for future drug therapies. However, the majority of the kinome remains to be explored.
近年来，疟疾病例和相关死亡人数有所减少，但抗青蒿素衍生物的突变等因素对这一进展构成了威胁。目前有多种药物正在进行临床试验以治疗疟疾，其中一些具有新颖的作用机制。其中一种是疟原虫蛋白激酶抑制剂 MMV390048。本文列出了最近开发的针对疟原虫蛋白激酶的分子。使用 CAPLUS 和 MEDLINE 数据库，对 2005 年至 2020 年的文献进行了系统综述。共涉及 60 篇文章，描述了约 100 种针对 22 种疟原虫蛋白激酶的化合物。这项工作强调了针对疟原虫蛋白激酶的化合物在未来药物治疗方面的巨大潜力。然而，激酶组的大部分仍有待探索。
