Cellzome AG, Meyerhofstrasse 1, D-69117 Heidelberg, Germany.
Bioorg Med Chem. 2012 Mar 15;20(6):1973-8. doi: 10.1016/j.bmc.2011.11.003. Epub 2011 Nov 9.
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.
化学生物组学是一门新兴的研究学科，处于医学化学、生物化学和细胞生物学的交叉点，专注于研究药物和其他生物活性小分子的作用分子机制。研究策略通常将表型筛选与后续的靶标鉴定相结合，旨在对药物诱导的细胞蛋白表达和翻译后修饰的变化进行全蛋白质组学特征描述。近年来，定量质谱分析在这些方法中占据了核心地位。本文描述了当前化学生物组学研究中的实验策略，讨论了最近成功应用的实例，并强调了在药物发现中，使用天然内源性蛋白质的基于化学生物组学的测定方法有望产生重大影响的领域。
