中文摘要：

众多物种基因组解码工作的完成极大地丰富了我们对这些生命体系组成复杂度的认知，然而下一个更为严峻的挑战是如何快速准确地解析这些基因编码蛋白的分子功能，这也是当前蛋白质组学领域亟待解决的一个重要科学问题．基于活性的蛋白质组分析是近些年来一项新兴的技术平台，它致力于在复杂的生命体系中系统地鉴定某类具有特定功能的蛋白质分子．在本篇短综述中，我们将对该化学生物学技术的发展做一个简要的回顾，重点介绍该技术在未知蛋白的功能解析、小分子抑制剂的筛选以及活性小分子靶标蛋白的鉴定等方面的工作，最后将对该技术未来发展的走向及其拓展应用做前瞻性的讨论．

英文摘要：

Genome sequencing projects have revolutionized our view of the complexity of prokaryotic and eukaryotic pro- teomes, however, we are also left with a daunting challenge of functionally annotating these large number of predicted pro- teins. Activity-based protein profiling （ABPP） has been developed as a powerful chemoproteomic tool aiming at systemati- cally discovering and assigning functions of uncharacterized enzymes directly from native proteomes. Here, we reviewed the development and application of this emerging technique, mainly focusing on how it was applied for functional annotation of unknown enzymes, screening and optimization of small-molecule inhibitors, and target identification of bio-active small molecules.