2. Academic Validation
  3. Competitive profiling of celastrol targets in human cervical cancer HeLa cells via quantitative chemical proteomics

Competitive profiling of celastrol targets in human cervical cancer HeLa cells via quantitative chemical proteomics

  • Mol Biosyst. 2016 Dec 20;13(1):83-91. doi: 10.1039/c6mb00691d.
Yiqing Zhou 1,  Weichao Li 2,  Mingli Wang 3,  Xixi Zhang 4,  Haibing Zhang 5,  Xiaofeng Tong 6,  Youli Xiao 2
Affiliations

Affiliations

  • 1 CAS Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200032, China. ylxiao@sibs.ac.cn.
  • 2 CAS Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200032, China. ylxiao@sibs.ac.cn and University of Chinese Academy of Sciences, Beijing 100039, China.
  • 3 CAS Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200032, China. ylxiao@sibs.ac.cn and Department of Chemistry, East China University of Science and Technology, Shanghai 200001, China.
  • 4 University of Chinese Academy of Sciences, Beijing 100039, China and Institute for Nutritional Sciences, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200032, China.
  • 5 Institute for Nutritional Sciences, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200032, China.
  • 6 Department of Chemistry, East China University of Science and Technology, Shanghai 200001, China.
PMID: 27819370 DOI: 10.1039/c6mb00691d
Abstract

Celastrol, isolated from the traditional Chinese medicinal herb Tripterygium wilfordii Hook. f. (Thunder God's Vine), has been used to treat Cancer, chronic inflammatory, autoimmune and other human diseases. However, to date, the protein targets and the mechanism of action of celastrol have remained elusive. In this study, we find that celastrol can react with protein thiols in a unique covalent and reversible manner, while protein denaturing disrupts the interaction. Through a competitive chemoproteomics approach utilizing a cysteine-targeting activity-based probe, we report the proteome-wide quantitative profiling of cellular targets of celastrol in human cervical Cancer HeLa cells. Representative targets are further validated via in vitro binding experiments and/or enzymatic activity assays. Bioinformatics analysis results suggest that celastrol exerts its numerous therapeutic effects through interaction with promiscuous proteins involved in various biological processes and cellular pathways.

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