典型文献
A bifunctional vinyl-sulfonium tethered peptide induced by thio-Michael-type addition reaction
文献摘要：
The modification and functionalization of peptides is of great significance in modern biotechnology and drug development.Here we report a highly reactive Michael-type warhead for the covalently modification of cysteine on peptide and protein.By installing a vinyl group onto a methionine residue of peptide,the produced vinyl sulfonium can be efficiently nucleophilic added by appropriate cysteine residue of this peptide,and thus yield a cyclized peptide.This peptide cyclization strategy was proven to exhibit improved cell penetration and good stability.Moreover,a peptide ligand bearing vinyl sulfonium could covalently bind to the cysteine in the target protein,indicating the potential of vinyl sulfonium as a novel warhead for developing covalent peptide inhibitor.
文献关键词：
中图分类号：
作者姓名：
Hongkun Xu;Xuan Qin;Yaping Zhang;Chuan Wan;Rui Wang;Zhanfeng Hou;Xiaofeng Ding;Hailing Chen;Ziyuan Zhou;Yang Li;Chenshan Lian;Feng Yin;Zigang Li
作者机构：
State Key Laboratory of Chemical Oncogenomics,School of Chemical Biology and Biotechnology,Peking University Shenzhen Graduate School,Shenzhen 518055,China;Pingshan translational medicine center,Shenzhen Bay Laboratory,Shenzhen 518055,China;Anhui Medical University,Hefei 230032,China;Cancer Hospital Chinese Academy of Medical Sciences,Shenzhen Center,Shenzhen 518000,China
文献出处：
引用格式：
[1]Hongkun Xu;Xuan Qin;Yaping Zhang;Chuan Wan;Rui Wang;Zhanfeng Hou;Xiaofeng Ding;Hailing Chen;Ziyuan Zhou;Yang Li;Chenshan Lian;Feng Yin;Zigang Li-.A bifunctional vinyl-sulfonium tethered peptide induced by thio-Michael-type addition reaction)[J].中国化学快报（英文版）,2022(04):2001-2004
A类：
sulfonium,warhead,cyclized
B类：
bifunctional,vinyl,tethered,induced,by,Michael,type,addition,reaction,modification,functionalization,peptides,great,significance,modern,biotechnology,drug,development,Here,we,report,highly,reactive,covalently,cysteine,protein,By,installing,group,onto,methionine,residue,produced,efficiently,nucleophilic,added,appropriate,this,thus,yield,This,cyclization,strategy,was,proven,exhibit,improved,cell,penetration,good,stability,Moreover,ligand,bearing,could,bind,target,indicating,potential,novel,developing,inhibitor
AB值：
0.542096
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