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小分子生物活性探针在细胞靶点鉴定中的应用

[The application of small molecule bioactive probes in the identification of cellular targets].

作者信息

Zhang Jiong, Zhou Hu-Chen

机构信息

School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.

出版信息

Yao Xue Xue Bao. 2012 Mar;47(3):299-306.

Abstract

Identification of the cellular targets of bioactive compounds is a major challenge and a key issue in chemical biology and drug discovery. As an important technology in functional proteomics, small molecule probes play a pivotal role in the identification of cellular targets of bioactive compounds. This review is intended to introduce the application principles and structural design philosophy of chemical probes for the purpose of mechanistic study. Recent cases of successful application were also discussed to further demonstrate the principles and significance ofbioactive small molecule-based probes.

摘要

确定生物活性化合物的细胞靶点是化学生物学和药物发现中的一项重大挑战和关键问题。作为功能蛋白质组学中的一项重要技术,小分子探针在生物活性化合物细胞靶点的鉴定中起着关键作用。本综述旨在介绍用于机理研究的化学探针的应用原理和结构设计理念。还讨论了最近成功应用的案例,以进一步证明基于生物活性小分子的探针的原理和意义。

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