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While significant advancements have been made in recent years in target identification and drug discovery, there is a general lack of validated targets for diseases. In the meantime, the number of new molecular entities approved per year has dramatically declined over the past decades. There is still much room for further improvement to optimize the drug discovery process. Activity-based protein profiling (ABPP) is a chemical proteomic method for functional investigation of complex proteomes directly in native biological systems. ABPP is widely used for target identification and drug discovery by using chemical probes that label active site residues in proteins. This review summarizes the design strategy of ABPP and introduces the related applications of ABPP technology in the field of target identification and drug discovery.

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尽管近年来靶点鉴定和药物发现领域取得了重要进展，但目前仍缺乏有效的疾病治疗靶点。与此同时，在过去几十年里，每年获批的新分子实体数量急剧下降，如何更好地进行药物发现仍有很大的改进空间。基于活性的蛋白质组学分析（activity-based protein profiling, ABPP）是一种直接在真实生物环境中研究复杂蛋白质组功能的化学蛋白质组学方法，主要通过使用化学探针标记蛋白质活性位点的氨基酸残基，被广泛用于靶点鉴定和药物发现。本文总结了ABPP的设计策略，并介绍了ABPP技术在靶点鉴定和药物发现领域的相关应用实例。

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牛乐，女，硕士研究生，研究方向：药物化学。E-mail: 13773044101@163.com。

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牛乐，女，硕士研究生，研究方向：药物化学。E-mail: 13773044101@163.com。

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