Activity-based protein profiling (ABPP) has become an emerging chemical proteomic approach to illustrate the interaction mechanisms between compounds and proteins. This approach has combined organic synthesis, biochemistry, cell biology, biophysics and bioinformatics to accelerate the process of drug discovery in target identification and validation, as well as in the stage of lead discovery and optimization. This review will summarize new developments and applications of ABPP in medicinal chemistry. Here, we mainly described the design principles of activity-base probes (ABPs) and general workflows of ABPP approach. Moreover, we discussed various basic and advanced ABPP strategies and their applications in medicinal chemistry, including competitive and comparative ABPP, two-step ABPP, fluorescence polarization ABPP (FluoPol-ABPP) and ABPs for visualization. In conclusion, this review will give a general overview of the applications of ABPP as a powerful and efficient technique in medicinal chemistry.

中文翻译：

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基于活动的蛋白质谱分析：药物化学的最新进展。

基于活性的蛋白质谱分析（ABPP）已成为一种新兴的化学蛋白质组学方法，用以说明化合物与蛋白质之间的相互作用机理。这种方法将有机合成，生物化学，细胞生物学，生物物理学和生物信息学相结合，以加快目标识别和验证以及潜在客户发现和优化阶段的药物发现过程。这篇综述将总结ABPP在药物化学中的新发展和应用。在这里，我们主要介绍了基于活动的探针（ABP）的设计原理和ABPP方法的一般工作流程。此外，我们讨论了各种基本和高级ABPP策略及其在药物化学中的应用，包括竞争性ABAB和比较ABPP，两步ABPP，荧光偏振ABPP（FluoPol-ABPP）和ABP用于可视化。总之，本综述将概述ABPP作为一种强大而有效的药物化学技术的应用。