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Discovery of Pentacyclic Triterpenoids as Potential Entry Inhibitors of Influenza Viruses
Yu, Maorong1; Si, Longlong1; Wang, Yufei1; Wu, Yiming1; Yu, Fei1,6; Jiao, Pingxuan1; Shi, Yongying1; Wang, Han1; Xiao, Sulong1; Fu, Ge1; Tian, Ke2; Wang, Yitao3; Guo, Zhihong4,5; Ye, Xinshan1; Zhang, Lihe1; Zhou, Demin1
刊名JOURNAL OF MEDICINAL CHEMISTRY
2014-12-11
DOI10.1021/jm5014067
57期:23页:10058-10071
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]OLEANANE-TYPE TRITERPENES ; HCV ENTRY ; A VIRUS ; ISOLATED WORLDWIDE ; RECEPTOR-BINDING ; AVIAN INFLUENZA ; MEMBRANE-FUSION ; HEMAGGLUTININ ; REPLICATION ; INFECTION
英文摘要

Entry inhibitors are of particular importance in current efforts to develop a new generation of anti-influenza virus drugs. Here we report certain pentacyclic triterpenes exhibiting conserved structure features and with in vitro anti-influenza virus activity comparable to and even higher than that of oseltamivir. Mechanistic studies indicated that these lead triterpenoids bind tightly to the viral envelope hemagglutinin (HA), disrupting the interaction of HA with the sialic acid receptor and thus the attachment of viruses to host cells. Docking studies suggest that the binding pocket within HA for sialic acid receptor potentially acts as a targeting domain, and this is supported by structure-activity data, sialic acid competition studies, and broad anti-influenza spectrum as well as less induction of drug resistance. Our study might establish the importance of triterpenoids for development of entry inhibitors of influenza viruses.

语种英语
WOS记录号WOS:000346321200025
项目编号2010CB12300 ; 813611680027 ; 81101239 ; 20932001 ; 91029711 ; 20852001 ; 81373271 ; 81202975 ; 074/2012/A3 ; 077/2011/A3
资助机构National Basic Research Program of China (973 Program) ; National Natural Science Foundation of China ; Science and Technology Development Fund of Macao ; Peking-Tsinghua Center for Life Sciences
引用统计
被引频次:26[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/59911
专题北京大学药学院_药物化学系
北京大学药学院
北京大学药学院_化学生物学系
北京大学药学院_药学院
作者单位1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Northwestern Univ, Stanley Manne Childrens Res Inst, Chicago, IL 60614 USA
3.Univ Macau, State Key Lab Qual Res Chinese Med, Long, Taipo, Peoples R China
4.Hong Kong Univ Sci & Technol, Dept Chem, Hong Kong, Hong Kong, Peoples R China
5.Hong Kong Univ Sci & Technol, Biotechnol Res Inst, Hong Kong, Hong Kong, Peoples R China
6.Kunming Univ Sci & Technol, Fac Med, Kunming 650500, Peoples R China
推荐引用方式
GB/T 7714
Yu, Maorong,Si, Longlong,Wang, Yufei,et al. Discovery of Pentacyclic Triterpenoids as Potential Entry Inhibitors of Influenza Viruses[J]. JOURNAL OF MEDICINAL CHEMISTRY,2014,57(23):10058-10071.
APA Yu, Maorong.,Si, Longlong.,Wang, Yufei.,Wu, Yiming.,Yu, Fei.,...&Zhou, Demin.(2014).Discovery of Pentacyclic Triterpenoids as Potential Entry Inhibitors of Influenza Viruses.JOURNAL OF MEDICINAL CHEMISTRY,57(23),10058-10071.
MLA Yu, Maorong,et al."Discovery of Pentacyclic Triterpenoids as Potential Entry Inhibitors of Influenza Viruses".JOURNAL OF MEDICINAL CHEMISTRY 57.23(2014):10058-10071.
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