Activity-based protein profiling: Recent advances in medicinal chemistry

IF 6 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2020-04-01 DOI:10.1016/j.ejmech.2020.112151
Hui Deng , Qian Lei , Yangping Wu , Yang He , Weimin Li
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引用次数: 49

Abstract

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.

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基于活性的蛋白质谱分析: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,用于阐明化合物与蛋白质之间的相互作用机制。该方法结合了有机合成、生物化学、细胞生物学、生物物理学和生物信息学,加快了药物在靶点鉴定和验证以及先导物发现和优化阶段的发现过程。本文就ABPP在药物化学中的最新进展及其应用进行综述。在这里,我们主要描述了基于活动的探针(abp)的设计原则和ABPP方法的一般工作流程。此外,我们还讨论了各种基本和先进的ABPP策略及其在药物化学中的应用,包括竞争ABPP和比较ABPP、两步ABPP、荧光极化ABPP (flupol -ABPP)和可视化ABPP。综上所述,本文将对ABPP作为一种强大而高效的技术在药物化学中的应用进行综述。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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