國家衛生研究院 NHRI:Item 3990099045/12808
English  |  正體中文  |  简体中文  |  全文筆數/總筆數 : 12145/12927 (94%)
造訪人次 : 855579      線上人數 : 1230
RC Version 6.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
搜尋範圍 查詢小技巧：
  • 您可在西文檢索詞彙前後加上"雙引號"，以獲取較精準的檢索結果
  • 若欲以作者姓名搜尋，建議至進階搜尋限定作者欄位，可獲得較完整資料
    •  進階搜尋
    主頁 ‧ 登入 ‧ 上傳 ‧ 說明 ‧ 關於NHRI ‧ 管理 到手機版


    請使用永久網址來引用或連結此文件: http://ir.nhri.org.tw/handle/3990099045/12808


    題名: Discovery of M protease inhibitors encoded by SARS-CoV-2
    作者: Hung, HC;Ke, YY;Huang, SY;Huang, PN;Kung, YA;Chang, TY;Yen, KJ;Peng, TT;Chang, SE;Huang, CT;Tsai, YR;Wu, SH;Lee, SJ;Lin, JH;Liu, BS;Sung, WC;Shih, SR;Chen, CT;Hsu, JT
    貢獻者: Institute of Biotechnology and Pharmaceutical Research;National Institute of Infectious Diseases and Vaccinology
    摘要: The COVID-19 pandemic caused by SARS-CoV-2 is a health threat worldwide. Viral main protease (M(pro), also called 3C-like protease, 3CL(pro)) is a therapeutic target for drug discovery. Herein, we report that GC376, a broad-spectrum inhibitor targeting M(pro) in the picornavirus-like supercluster, is potent inhibitor for the M(pro) encoded by SARS-CoV-2 with half-maximum inhibitory concentration (IC(50)) of 26.4±1.1 nM. In this study, we also show that GC376 inhibits SARS-CoV-2 replication with a half-maximum effective concentration (EC(50)) of 0.91±0.03 μM. Only a small portion of SARS-CoV-2-M(pro) was covalently modified in the excess of GC376 as evaluated by mass spectrometry analysis; indicating that improved inhibitors are needed. Subsequently, molecular docking analysis revealing the recognition and binding groups of GC376 within the active site of SARS-CoV-2 M(pro) provides important new information for the optimization of GC376. Given that sufficient safety and efficacy data are available for GC376 as an investigational veterinary drug, expedited development of GC376, or its optimized analogues, for treatment of SARS-CoV-2 infection in human is recommended.
    日期: 2020-08-20
    關聯: Antimicrobial Agents and Chemotherapy. 2020 Aug 20;64(9):e00872-20.
    Link to: http://dx.doi.org/10.1128/aac.00872-20
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0066-4804&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000566461500005
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85089786845
    顯示於類別:[徐祖安] 期刊論文
    [陳炯東] 期刊論文
    [李秀珠] 期刊論文
    [宋旺洲] 期刊論文

    文件中的檔案:

    檔案 描述 大小格式瀏覽次數
    PUB32669265.pdf1174KbAdobe PDF351檢視/開啟


    在NHRI中所有的資料項目都受到原著作權保護.

    TAIR相關文章

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - 回饋