Chemoproteomic approaches to drug target identification and drug profiling
Chemoproteomic approaches to drug target identification and drug profiling
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DOI：
10.1016/j.bmc.2011.11.003
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发表时间：
2012-03-15
影响因子：
3.5
通讯作者：
Drewes, Gerard
中科院分区：
文献类型：
--
作者：
Bantscheff, Marcus;Drewes, Gerard
化学蛋白质组学代表了药物化学、生物化学和细胞生物学交叉领域的一门新的研究学科，重点研究药物和其他生物活性小分子的分子作用机制。研究策略经常将表型筛选与随后的靶点识别相结合，旨在对药物诱导的细胞蛋白表达和翻译后修饰变化进行全蛋白质组表征。近年来，定量质谱分析已成为许多此类方法的中心舞台。这篇综述描述了当前化学蛋白质组学研究中的实验策略，讨论了最近成功应用的例子，并重点介绍了药物发现领域，在这些领域中，使用天然内源蛋白进行基于化学蛋白质组学的测定预计将产生重大影响。 (C) 2011 Elsevier Ltd. 保留所有权利。
Chemoproteomics represents a new research discipline at the interface of medicinal chemistry, biochemistry, and cell biology focused on studying the molecular mechanisms of action of drugs and other bioactive small molecules. Research strategies frequently combine phenotypic screening with subsequent target identification, and aim at a proteome-wide characterization of drug-induced changes in cellular protein expression and post-translational modifications. In recent years quantitative mass spectrometry has taken center stage in many of these approaches. This review describes experimental strategies in current chemical proteomics research, discusses recent examples of successful applications, and highlights areas in drug discovery where chemical proteomics-based assays using native endogenous proteins are expected to have substantial impact. (C) 2011 Elsevier Ltd. All rights reserved.