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论文题目: Competitive profiling of celastrol targets in human cervical cancer HeLa cells via quantitative chemical proteomics
英文论文题目: Competitive profiling of celastrol targets in human cervical cancer HeLa cells via quantitative chemical proteomics
第一作者: Zhou, YQ; Li, WC; Wang, ML; Zhang, XX; Zhang, HB; Tong, XF; Xiao, YL
英文第一作者: Zhou, YQ; Li, WC; Wang, ML; Zhang, XX; Zhang, HB; Tong, XF; Xiao, YL
联系作者: Xiao, YL (reprint author), Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Plant Physiol & Ecol, CAS Ctr Excellence Mol Plant Sci,CAS Key Lab Synt, Shanghai 200032, Peoples R China.
英文联系作者: Xiao, YL (reprint author), Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Plant Physiol & Ecol, CAS Ctr Excellence Mol Plant Sci,CAS Key Lab Synt, Shanghai 200032, Peoples R China.
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发表年度: 2017
卷: 13
期: 1
页码: 83-91
摘要: 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.
英文摘要: 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.
刊物名称: MOLECULAR BIOSYSTEMS
英文刊物名称: MOLECULAR BIOSYSTEMS
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学科: Biochemistry & Molecular Biology
英文学科: Biochemistry & Molecular Biology
影响因子: 2.781
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论文类别: Article
英文论文类别: Article
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