典型文献
Parthenolide reveals an allosteric mode to inhibit the delSGylation activity of SARS-CoV-2 papain-like protease
文献摘要：
The coronavirus papain-like protease(PLpro)of severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)is responsible for viral polypeptide cleavage and the delSGylation of interferon-stimulated gene 15(ISG15),which enable it to participate in virus replication and host innate immune pathways.Therefore,PLpro is considered an attractive antiviral drug target.Here,we show that parthenolide,a germacrane sesquiterpene lactone,has SARS-CoV-2 PLpro inhibitory activity.Parthenolide covalently binds to Cys-191 or Cys-194 of the PLpro protein,but not the Cys-111 at the PLpro catalytic site.Mutation of Cys-191 or Cys-194 reduces the activity of PLpro.Molecular docking studies show that parthenolide may also form hydrogen bonds with Lys-192,Thr-193,and Gln-231.Furthermore,parthenolide inhibits the delSGylation but not the deubiquitinating activity of PLpro in vitro.These results reveal that parthenolide inhibits PLpro activity by allosteric regulation.
文献关键词：
中图分类号：
作者姓名：
Zhihui Zou;Huizhuang Shan;Demeng Sun;Li Xia;Yulong Shi;Jiahui Wan;Aiwu Zhou;Yunzhao Wu;Hanzhang Xu;Hu Lei;Zhijian Xu;Yingli Wu
作者机构：
Hongqiao International Institute of Medicine,Shanghai Tongren Hospital/Faculty of Basic Medicine,Chemical Biology Division of Shanghai Universities E-Institutes,Key Laboratory of Cell Differentiation and Apoptosis of the Chinese Ministry of Education,Chinese Academy of Medical Sciences Research Unit 2019RU043,Shanghai Jiao Tong University School of Medicine(SJTU-SM),Shanghai 200025,China;Laboratory Medicine,Guangdong Provincial People's Hospital,Guangdong Academy of Medical Sciences,Guangzhou,Guangdong 510000,China;Tsinghua-Peking Center for Life Sciences,Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology(Ministry of Education),Beijing Advanced Innovation Center for Structural Biology,Department of Chemistry,Tsinghua University,Beijing 100084,China;CAS Key Laboratory of Receptor Research,Drug Discovery and Design Center,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China
文献出处：
引用格式：
[1]Zhihui Zou;Huizhuang Shan;Demeng Sun;Li Xia;Yulong Shi;Jiahui Wan;Aiwu Zhou;Yunzhao Wu;Hanzhang Xu;Hu Lei;Zhijian Xu;Yingli Wu-.Parthenolide reveals an allosteric mode to inhibit the delSGylation activity of SARS-CoV-2 papain-like protease)[J].生物化学与生物物理学报（英文版）,2022(08):1133-1139
A类：
delSGylation,germacrane
B类：
Parthenolide,reveals,allosteric,mode,activity,SARS,CoV,papain,like,protease,coronavirus,PLpro,severe,acute,respiratory,syndrome,is,responsible,polypeptide,cleavage,interferon,stimulated,gene,ISG15,which,enable,participate,replication,host,innate,immune,pathways,Therefore,considered,attractive,antiviral,drug,target,Here,we,show,that,parthenolide,sesquiterpene,lactone,has,inhibitory,covalently,binds,Cys,protein,but,not,catalytic,site,Mutation,reduces,Molecular,docking,studies,may,also,form,hydrogen,bonds,Lys,Thr,Gln,Furthermore,inhibits,deubiquitinating,vitro,These,results,by,regulation
AB值：
0.539227
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机标中图分类号，由域田数据科技根据网络公开资料自动分析生成，仅供学习研究参考。
