Acta Chim. Sinica ›› 2015, Vol. 73 ›› Issue (7): 657-668.DOI: 10.6023/A15040223 Previous Articles     Next Articles



王初a,b,c,d,e, 陈南c   

  1. a 北京大学分子科学国家实验室, 北京 100871;
    b 生物有机与分子工程教育部重点实验室, 北京 100871;
    c 北京大学化学与分子工程学院, 北京 100871;
    d 合成与功能生物分子中心, 北京 100871;
    e 北大清华生命科学联合中心 北京 100871
  • 投稿日期:2015-04-02 发布日期:2015-05-22
  • 通讯作者: 王初
  • 基金资助:

    项目受国家自然科学基金委重大项目(No. 81490740)和面上项目(No. 21472008)资助.

Activity-based Protein Profiling

Wang Chua,b,c,d,e, Chen Nanc   

  1. a Beijing National Laboratory for Molecular Sciences, Beijing 100871;
    b Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Beijing 100871;
    c College of Chemistry and Molecular Engineering, Beijing 100871;
    d Synthetic and Functional Biomolecules Center, Beijing 100871;
    e Peking-Tsinghua Center for Life Sciences, Peking University, Beijing 100871
  • Received:2015-04-02 Published:2015-05-22
  • Supported by:

    Project supported by the Research grants (No. 81490740 and No. 21472008) from the National Natural Science Foundation of China.

Genome sequencing projects have revolutionized our view of the complexity of prokaryotic and eukaryotic proteomes, however, we are also left with a daunting challenge of functionally annotating these large number of predicted proteins. Activity-based protein profiling (ABPP) has been developed as a powerful chemoproteomic tool aiming at systematically 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.

Key words: activity-based probe, chemical proteomics, protein functional annotation, inhibitor development, target identification