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Review Article

抗疟疾发现的新分子靶点和策略

卷 26, 期 23, 2019

页: [4380 - 4402] 页: 23

弟呕挨: 10.2174/0929867324666170830103003

价格: $65

摘要

疟疾仍然是一个主要的健康问题，特别是因为出现了对青蒿素衍生物具有抗药性的恶性疟原虫菌株。 在这种情况下，迫切需要安全和负担得起的抗疟药。 已经研究了新蛋白质作为具有明确作用机理的创新化合物的研究和开发的分子靶标。 在这篇综述中，我们着重介绍了经过基因和临床验证的疟原虫蛋白质作为下一代治疗药物的靶标。 本文所述的酶涉及血红蛋白水解，侵袭过程，蛋白质合成的延伸因子，嘧啶的生物合成，翻译后修饰如异戊烯基化，磷酸化和组蛋白乙酰化，线粒体中ATP的生成和RNA的氨基酰化。 蛋白质组学，遗传学，结构生物学，计算和生物物理方法的重大进步为这些药物靶标提供了宝贵的分子和结构信息。 基于此，已经应用了几种策略和模型来识别和改进先导化合物。 这篇综述介绍了抗疟药物候选者的最新研究进展，重点介绍了提供负担得起的，安全的和低剂量的单药来治疗疟疾的方法，挑战和观点。

关键词: 疟原虫，疟疾，酶，分子靶标，抗疟疾，抑制剂。

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