新型冠状病毒2型蛋白酶抑制剂的快速耐药性分析
Rapid resistance profiling of SARS-CoV-2 protease inhibitors.
作者信息
Moghadasi Seyed Arad, Biswas Rayhan G, Harki Daniel A, Harris Reuben S
机构信息
University of Minnesota, Minneapolis, 55455, MN, USA.
Department of Biochemistry and Structural Biology, University of Texas Health San Antonio, San Antonio, 78229, TX, USA.
出版信息
NPJ Antimicrob Resist. 2023 Aug 20;1(1):9. doi: 10.1038/s44259-023-00009-0.
Resistance to nirmatrelvir (Paxlovid) has been shown by multiple groups and may already exist in clinical SARS-CoV-2 isolates. Here a robust cell-based assay is used to determine the relative potencies of nirmatrelvir, ensitrelvir, and FB2001 against a panel of SARS-CoV-2 main protease (M) variants. The results reveal that these three drugs have at least partly distinct resistance mutation profiles and raise the possibility that the latter compounds may be effective in some instances of Paxlovid resistance and vice versa.
多个研究团队已证实存在对奈玛特韦（帕罗韦德）的耐药性，并且这种耐药性可能已存在于临床严重急性呼吸综合征冠状病毒2（SARS-CoV-2）分离株中。在此，我们使用一种强大的基于细胞的检测方法来确定奈玛特韦、恩赛特韦和FB2001对一组SARS-CoV-2主要蛋白酶（M）变体的相对效力。结果表明，这三种药物具有至少部分不同的耐药突变谱，并增加了后两种化合物在某些帕罗韦德耐药情况下可能有效的可能性，反之亦然。
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