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[无需化学修饰的小分子药物靶蛋白鉴定技术及其应用:综述]

[Identification techniques of small molecule drug target proteins without chemical modification and its applications: a review].

作者信息

Ma Jie, Liu Qiang

机构信息

Department of Histoembryology, Genetics and Developmental Biology, Basic Medical College, Shanghai Key Laboratory of Reproductive Medicine, Shanghai Jiaotong University School of Medicine, Shanghai 200025, China.

出版信息

Sheng Wu Gong Cheng Xue Bao. 2021 Apr 25;37(4):1131-1138. doi: 10.13345/j.cjb.200426.

Abstract

Identification of the target proteins of small molecule drugs is crucial for understanding the mechanisms of drug actions and its side effects. Conventional methods require chemical modification, which might alter the activities of the drugs. Various label-free techniques have been developed to identify drug target proteins without chemical modifications. This includes drug affinity responsive target stability (DARTS), stability of proteins from rates of oxidation (SPROX), cellular thermal shift assay (CETSA), thermal proteome profiling (TPP) and many others. Here we review the principles and applications of these label-free techniques, their advantages and limitations, as well as the most recent advances.

摘要

识别小分子药物的靶蛋白对于理解药物作用机制及其副作用至关重要。传统方法需要化学修饰,这可能会改变药物的活性。已开发出各种无标记技术来识别未经化学修饰的药物靶蛋白。这包括药物亲和力响应靶标稳定性(DARTS)、基于氧化速率的蛋白质稳定性(SPROX)、细胞热位移分析(CETSA)、热蛋白质组分析(TPP)等。在此,我们综述这些无标记技术的原理与应用、它们的优缺点以及最新进展。

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