Activity- and reactivity-based proteomics: Recent technological advances and applications in drug discovery.
Activity- and reactivity-based proteomics: Recent technological advances and applications in drug discovery.
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DOI：
10.1016/j.cbpa.2020.06.011
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发表时间：
2021-02-01
影响因子：
7.8
通讯作者：
Child, Matthew Andrew
中科院分区：
文献类型：
--
作者：
Benns, Henry James;Wincott, Ceire Joanne;Child, Matthew Andrew
基于活性的蛋白质谱分析（ABPP）被认为是一种强大而通用的化学蛋白质组学技术。ABPP的核心是使用基于活性的探针来报告复杂生物系统中特定酶的活性或氨基酸类型的反应性。在过去的二十年中，ABPP促进了新药物靶点的鉴定和人类疾病和传染病中先导化合物的发现。此外，作为阐明可药物蛋白质组的持续全球努力的一部分，近年来，基于活性的探针可寻址的目标类别已大大扩展。在这里，我们提供了ABPP的概述，并总结了主要的技术进步，重点是探针的发展。
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.