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Review Article

Fyn激酶抑制剂在切换神经炎症通路中的作用

卷 29, 期 27, 2022

发表于: 12 January, 2022

页: [4738 - 4755] 页: 18

弟呕挨: 10.2174/0929867329666211221153719

价格: $65

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摘要

参与了从细胞增殖和分化到细胞粘附和细胞运动的多种信号通路，并且已经发现它在各种类型的癌症中过表达。在中枢神经系统中，Fyn发挥几种不同的功能，如轴突 - 神经胶质信号转导，少突胶质细胞成熟和髓鞘形成，并且它与神经炎症过程有关。基于这些前提，Fyn成为癌症和神经退行性疾病治疗，特别是阿尔茨海默病（AD）的有吸引力的靶点，其基础是Aβ通过细胞朊病毒蛋白激活及其与tau蛋白的相互作用。然而，Fyn也是一个具有挑战性的靶标，因为迄今为止发现的Fyn抑制剂，由于Fyn与其他激酶的相关同源性，遭受脱靶效应。本综述涵盖了过去十年中为鉴定和优化有效抑制Fyn的小分子所做的努力，无论是在酶法还是细胞测定中，包括药物重新定位实践，作为治疗性干预神经变性的机会。

关键词: Fyn激酶，神经变性，达沙替尼，酪氨酸激酶，fyn抑制剂，吡咯嘧啶。

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