Identification of a novel inhibitor against middle east respiratory syndrome coronavirus
文献类型:期刊论文
作者 | Sun, Yaping1,2; Zhang, Huaidong1; Shi, Jian1; Zhang, Zhe1; Gong, Rui1 |
刊名 | Viruses-basel
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出版日期 | 2017-09-01 |
卷号 | 9期号:9页码:12 |
关键词 | Mers-cov Fusion inhibitor Six-helix bundle Heptad repeat Five-helix bundle |
ISSN号 | 1999-4915 |
DOI | 10.3390/v9090255 |
通讯作者 | Gong, rui(gongr@wh.iov.cn) |
英文摘要 | The middle east respiratory syndrome coronavirus (mers-cov) was first isolated in 2012, and circulated worldwide with high mortality. the continual outbreaks of mers-cov highlight the importance of developing antiviral therapeutics. here, we rationally designed a novel fusion inhibitor named mers-five-helix bundle (mers-5hb) derived from the six-helix bundle (mers-6hb) which was formed by the process of membrane fusion. mers-5hb consists of three copies of heptad repeat 1 (hr1) and two copies of heptad repeat 2 (hr2) while mers-6hb includes three copies each of hr1 and hr2. as it lacks one hr2, mers-5hb was expected to interact with viral hr2 to interrupt the fusion step. what we found was that mers-5hb could bind to hr2p, a peptide derived from hr2, with a strong affinity value (k-d) of up to 0.24 nm. subsequent assays indicated that mers-5hb could inhibit pseudotyped mers-cov entry effectively with 50% inhibitory concentration (ic50) of about 1 mu m. in addition, mers-5hb significantly inhibited spike (s) glycoprotein-mediated syncytial formation in a dose-dependent manner. further biophysical characterization showed that mers-5hb was a thermo-stable alpha-helical secondary structure. the inhibitory potency of mers-5hb may provide an attractive basis for identification of a novel inhibitor against mers-cov, as a potential antiviral agent. |
WOS关键词 | RECEPTOR-BINDING DOMAIN ; MERS-COV ; SPIKE PROTEIN ; NEUTRALIZING ANTIBODIES ; SAUDI-ARABIA ; SUBUNIT VACCINES ; S PROTEIN ; FUSION ; PEPTIDE ; ENTRY |
WOS研究方向 | Virology |
WOS类目 | Virology |
语种 | 英语 |
WOS记录号 | WOS:000411491600011 |
出版者 | MDPI AG |
URI标识 | http://www.irgrid.ac.cn/handle/1471x/2373387 |
专题 | 武汉病毒研究所 |
通讯作者 | Gong, Rui |
作者单位 | 1.Chinese Acad Sci, Ctr Emerging Infect Dis, CAS Key Lab Special Pathogens & Biosafety, Wuhan Inst Virol, 44 Xiao Hong Shan, Wuhan 430071, Hubei, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
推荐引用方式 GB/T 7714 | Sun, Yaping,Zhang, Huaidong,Shi, Jian,et al. Identification of a novel inhibitor against middle east respiratory syndrome coronavirus[J]. Viruses-basel,2017,9(9):12. |
APA | Sun, Yaping,Zhang, Huaidong,Shi, Jian,Zhang, Zhe,&Gong, Rui.(2017).Identification of a novel inhibitor against middle east respiratory syndrome coronavirus.Viruses-basel,9(9),12. |
MLA | Sun, Yaping,et al."Identification of a novel inhibitor against middle east respiratory syndrome coronavirus".Viruses-basel 9.9(2017):12. |
入库方式: iSwitch采集
来源:武汉病毒研究所
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