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Review Article

酪蛋白激酶1抑制剂开发的最新进展

卷 28, 期 8, 2021

发表于: 13 July, 2020

页: [1585 - 1604] 页: 20

弟呕挨: 10.2174/0929867327666200713185413

价格: $65

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摘要

背景：酪蛋白激酶1（CK1）家族参与调节许多细胞过程，包括膜运输，DNA损伤修复，细胞骨架动力学，细胞骨架维持和细胞凋亡。 CK1亚型，尤其是CK1δ和CK1ε已成为严重疾病的重要治疗靶标，例如阿尔茨海默氏病（AD），肌萎缩性侧索硬化症（ALS），家族性晚期睡眠期综合征和癌症。由于CK1在疾病的发病机理中的重要性，因此人们对CK1抑制剂的开发非常感兴趣。 方法：使用SciFinderR作为工具，对有关CK1生物学和CK1抑制剂最新发展的出版物进行了调查，但不包括以专利形式发表的出版物。 结果：这篇综述介绍了CK1抑制剂发展的最新知识，包括根据结构特征分为7类的合成小分子抑制剂和天然化合物。概述了CK1抑制剂的研究进展，并介绍了各种现有的CK1抑制剂，它们的抑制活性以及构效关系。 结论：通过理化特性和生物学研究，可能了解CK1抑制剂的结构-活性关系，这将有助于更好地设计和发现有效的和选择性的CK1抑制剂，作为严重疾病如AD，ALS和癌症的潜在药物。

关键词: 酪蛋白激酶1（CK1）、抑制剂、化学物质、小分子、抗癌药物、药物设计。

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