Drug Discovery of Host CLK1 Inhibitors for Influenza Treatment
文献类型：期刊论文
| 作者 | Zu M(祖勉) ; Zu, M; Li, C; Fang, JS; Lian, WW; Liu, AL; Zheng, LS; Du, GH
|
| 刊名 | MOLECULES
 |
| 出版日期 | 2015 |
| 卷号 | 20期号:11页码:19735-19747 |
| 关键词 | influenza A virus CLK1 inhibitor CPE assay baculovirus coinfection protein expression and purification rational screening |
| 英文摘要 | The rapid evolution of influenza virus makes antiviral drugs less effective, which is considered to be a major bottleneck in antiviral therapy. The key proteins in the host cells, which are related with the replication cycle of influenza virus, are regarded as potential drug targets due to their distinct advantage of lack of evolution and drug resistance. Cdc2-like kinase 1 (CLK1) in the host cells is responsible for alternative splicing of the M2 gene of influenza virus during influenza infection and replication. In this study, we carried out baculovirus-mediated expression and purification of CLK1 and established a reliable screening assay for CLK1 inhibitors. After a virtual screening of CLK1 inhibitors was performed, the activities of the selected compounds were evaluated. Finally, several compounds with strong inhibitory activity against CLK1 were discovered and their in vitro anti-influenza virus activities were validated using a cytopathic effect (CPE) reduction assay. The assay results showed that clypearin, corilagin, and pinosylvine were the most potential anti-influenza virus compounds as CLK1 inhibitors among the compounds tested. These findings will provide important information for new drug design and development in influenza treatment, and CLK1 may be a potent drug target for anti-influenza drug screening and discovery. |
| 学科主题 | Chemistry |
| 类目[WOS] | Chemistry, Organic |
| 收录类别 | SCI ; MEDLINE |
| WOS记录号 | WOS:000365924800007 |
| 公开日期 | 2016-05-03 |
| 源URL | [http://ir.ihep.ac.cn/handle/311005/228860]  |
| 专题 | 中国科学院高能物理研究所 |
| 推荐引用方式 GB/T 7714 | Zu M,Zu, M,Li, C,et al. Drug Discovery of Host CLK1 Inhibitors for Influenza Treatment[J]. MOLECULES,2015,20(11):19735-19747. |
| APA | 祖勉.,Zu, M.,Li, C.,Fang, JS.,Lian, WW.,...&Du, GH.(2015).Drug Discovery of Host CLK1 Inhibitors for Influenza Treatment.MOLECULES,20(11),19735-19747. |
| MLA | 祖勉,et al."Drug Discovery of Host CLK1 Inhibitors for Influenza Treatment".MOLECULES 20.11(2015):19735-19747. |
入库方式： OAI收割
来源：高能物理研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。