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Review Article

半胱氨酸靶向的酪氨酸激酶的不可逆抑制剂和关键相互作用。

卷 26, 期 31, 2019

页: [5811 - 5824] 页: 14

弟呕挨: 10.2174/0929867325666180713124223

价格: $65

摘要

酪氨酸激酶是将磷酸基团从ATP转移到各种氨基酸残基的一大类蛋白激酶的子集。通过使酪氨酸残基磷酸化，酪氨酸激酶负责通过信号转导级联激活各种蛋白质，这是细胞信号转导的普遍机制。许多酪氨酸激酶抑制剂（TKIs）在临床上的成功应用以及蛋白激酶中的致病突变表明，大量激酶可能代表了治疗相关的靶标。迄今为止，大多数临床和临床前TKI都是ATP竞争性非共价抑制剂，它们通过识别特定蛋白激酶的独特特征来实现其选择性。现在，在科学界越来越感兴趣的是不可逆抑制剂的开发，该抑制剂与半胱氨酸或ATP结合口袋中的其他亲核残基形成共价键。不可逆的TKI具有许多潜在的优势，包括延长的药效学，合理的化合物设计适用性，高效力以及通过反应性半胱氨酸残基的突变来验证药理学特异性的能力。在这里，我们回顾了开发以半胱氨酸为目标的不可逆TKIs的最新努力，并讨论了其识别三磷酸腺苷结合口袋及其生物学活性的构型模式。

关键词: 半胱氨酸，TKI，抗癌剂，EGFR，不可逆的关键相互作用。

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