Department of Life Sciences, London, UK; Department of Chemistry, Imperial College London, London, UK.
Department of Life Sciences, London, UK.
Curr Opin Chem Biol. 2021 Feb;60:20-29. doi: 10.1016/j.cbpa.2020.06.011. Epub 2020 Aug 5.
Activity-based protein profiling (ABPP) is recognized as a powerful and versatile chemoproteomic technology in drug discovery. Central to ABPP is the use of activity-based probes to report the activity of specific enzymes or reactivity of amino acid types in complex biological systems. Over the last two decades, ABPP has facilitated the identification of new drug targets and discovery of lead compounds in human and infectious disease. Furthermore, as part of a sustained global effort to illuminate the druggable proteome, the repertoire of target classes addressable with activity-based probes has vastly expanded in recent years. Here, we provide an overview of ABPP and summarise the major technological advances with an emphasis on probe development.
基于活性的蛋白质组学分析（ABPP）被认为是药物发现中一种强大且多功能的化学生物组学技术。ABPP 的核心是使用基于活性的探针来报告特定酶的活性或复杂生物系统中氨基酸类型的反应性。在过去的二十年中，ABPP 促进了新的药物靶点的鉴定和人类及传染病的先导化合物的发现。此外，作为全球持续努力阐明可成药蛋白质组的一部分，近年来，基于活性的探针可作用的靶类别的范围大大扩展。在这里，我们概述了 ABPP，并总结了主要的技术进展，重点介绍了探针的开发。
