Review Article

酪蛋白激酶1δ抑制剂作为神经退行性疾病的有前途的治疗剂

卷 29, 期 27, 2022

发表于: 05 April, 2022

页: [4698 - 4737] 页: 40

弟呕挨: 10.2174/0929867329666220301115124

价格: $65

摘要

酪蛋白激酶1(CK1)属于丝氨酸 - 苏氨酸激酶家族,在所有真核生物中表达。至少六种CK1的人种亚型(称为α,γ1-3,δ和ε)已被克隆和表征。CK1δ亚型调节几种生理过程,包括DNA损伤修复,昼夜节律,细胞增殖和凋亡。因此,CK1δ功能障碍可能引发多种病理,如癌症、炎症和中枢神经系统疾病。CK1δ的过表达和异常活性与与神经退行性疾病发展有关的关键蛋白质的过度磷酸化有关,例如帕金森氏症和阿尔茨海默病以及肌萎缩性侧索硬化症。因此,CK1δ抑制剂作为这些病理学的潜在药物引起了人们的关注,并且已经从天然来源合成或分离了几种化合物,以评估其CK1δ抑制活性。本文综述了CK1δ抑制剂的开发情况,特别强调了结构-活性关系和计算研究,为新型抑制剂的设计提供了有用的见解。

关键词: 酪蛋白激酶1δ,酪蛋白激酶1δ抑制剂,神经保护剂,抗癌剂,小分子,天然抑制剂,药物设计。

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