Jump to main content
Jump to site search

Issue 1, 2017
Previous Article Next Article

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

Author affiliations

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.

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

Back to tab navigation

Supplementary files

Publication details

The article was received on 05 Oct 2016, accepted on 01 Nov 2016 and first published on 07 Nov 2016


Article type: Communication
DOI: 10.1039/C6MB00691D
Citation: Mol. BioSyst., 2017,13, 83-91
  •   Request permissions

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

    Y. Zhou, W. Li, M. Wang, X. Zhang, H. Zhang, X. Tong and Y. Xiao, Mol. BioSyst., 2017, 13, 83
    DOI: 10.1039/C6MB00691D

Search articles by author

Spotlight

Advertisements