蛋白质激酶在生命过程中起着关键的调节作用，蛋白质激酶的异常往往会导致恶性疾病如癌症的发生。靶向蛋白质激酶的小分子抑制剂为相关疾病的治疗提供了切实可行的方案，因此研究蛋白质激酶-小 分子的相互作用对于靶向药物的开发具有重要作用。质谱作为一种高精度、高通量、高灵敏度的分析仪器，在 蛋白质-小分子相互作用研究领域的应用得到了快速发展。本综述总结了质谱技术应用于蛋白质激酶-小分 子相互作用研究的主要策略和最新进展，探讨比较各种方法的优缺点。基于质谱的分析方法将有助于从分子 水平上深刻揭示蛋白质激酶-小分子的相互作用机理，为靶向药物的设计开发提供新的思路。

Protein kinases are crucial regulators in many cellular processes, and their aberrance usually lead to serious diseases like cancer. Small molecule inhibitors specifically targeted to protein kinases can provide an efficient solution to the treatment of these diseases. Thus, it is particularly important to elucidate the mechanisms of protein kinase-small molecule interactions. Mass spectrometry (MS) has been widely applied to the field of protein-small molecule interaction analysis due to its high sensitivity, high accuracy and high throughput. This review summarizes the recent developments of MS-based strategies for investigating protein kinase-small molecule interactions. We also discussed the advantages and disadvantages of these MS-based methods. These MS-based strategies are helpful to study the protein kinase-small molecule interactions at molecular level, which can promote the development of new targeted drugs.

国家科技部重点基础研究发展计划（2013CB911203）：整体蛋白质多种修饰的分析方法研究，负责人：王方军