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Review Article

针对寄生虫半胱氨酸蛋白酶为靶点的结构研究

卷 26, 期 23, 2019

页: [4435 - 4453] 页: 19

弟呕挨: 10.2174/0929867324666170810165302

价格: $65

摘要

半胱氨酸蛋白酶是存在于大多数生物体中的必需水解酶，包括病毒和单细胞寄生虫。 尽管这些蛋白质之间显示出很高的序列同一性，但跨不同物种的特定结构特征仍赋予这些生物分子以独特的功能，这些功能通常与病理状况有关。 因此，近几十年来，它们作为潜在的特异性抑制剂的有希望的靶标的相关性得到了强调，并偶尔得到了验证。 在这篇综述中，我们讨论了基于结构的运动的最新成果，这些运动的目的是发现新的针对克鲁萨因和福利帕星的抑制剂原型，分别作为南美锥虫病和疟疾治疗的替代治疗工具。 计算和合成方法已在点击优化策略上进行了组合，并在本文中进行了讨论。 这些理论被扩展到其他热带传染病和被忽视的病理，例如血吸虫病，利什曼病和巴贝虫病，还扩展到阿尔茨海默氏病，这是一种广泛存在的神经退行性疾病，目前无法通过药物进行有效管理，并且最近与人半胱氨酸蛋白酶的特殊生理病理作用有关。

关键词: 基于结构的策略，半胱氨酸蛋白酶，cruzain，falcipain，人组织蛋白酶，热带传染病，阿尔茨海默氏病。

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