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Discovery of pentacyclic triterpenoids as potential entry inhibitors of influenza viruses
Yu M.1; Si L.1; Wang Y.1; Wu Y.1; Yu F.1,5; Jiao P.1; Shi Y.1; Wang H.1; Xiao S.1; Fu G.1; Tian K.2; Wang Y.3; Guo Z.4; Ye X.1; Zhang L.1; Zhou D.1
2014
Source PublicationJournal of Medicinal Chemistry
ISSN222623
Volume57Issue:23Pages:10058
Abstract

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. © 2014 American Chemical Society.

DOIhttp://doi.org/10.1021/jm5014067
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000346321200025
The Source to ArticleScopus
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Cited Times [WOS]:41   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorYu M.; Zhou D.
Affiliation1.State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China
2.Stanley Manne Children’s Research Institute, Northwestern University, 2430 Halsted Street, Chicago, Illinois 60614, United States
3.State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Avenida Wai, Long, Taipo, Macao
4.Department of Chemistry and Biotechnology Research Institute, The Hong Kong University of Science and Technology, Clear Water Bay, Hong Kong
5.Medical Faculty, Kunming University of Science and Technology, Kunming 650500, China
Recommended Citation
GB/T 7714
Yu M.,Si L.,Wang Y.,et al. Discovery of pentacyclic triterpenoids as potential entry inhibitors of influenza viruses[J]. Journal of Medicinal Chemistry,2014,57(23):10058.
APA Yu M..,Si L..,Wang Y..,Wu Y..,Yu F..,...&Zhou D..(2014).Discovery of pentacyclic triterpenoids as potential entry inhibitors of influenza viruses.Journal of Medicinal Chemistry,57(23),10058.
MLA Yu M.,et al."Discovery of pentacyclic triterpenoids as potential entry inhibitors of influenza viruses".Journal of Medicinal Chemistry 57.23(2014):10058.
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