Improved fluorescence-based assay for rapid screening and evaluation of SARS-CoV-2 main protease inhibitors

文献类型： 外文期刊

第一作者： Zhang, Rui

作者： Zhang, Rui;Yan, Haohao;Zhou, Jiahao;Yan, Gangan;Liu, Xiaoping;Chen, Yunyu;Shang, Chao

作者机构：

关键词： echinatin; high-throughput screening; main protease inhibitor; MG-101; red fluorescent protein; SARS-CoV-2

期刊名称：JOURNAL OF MEDICAL VIROLOGY （ 影响因子：6.8； 五年影响因子：6.6 ）

ISSN： 0146-6615

年卷期： 2024 年 96 卷 3 期

页码：

收录情况： SCI

摘要： The outbreak of coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a global threat to human health. In parallel with vaccines, efficacious antivirals are urgently needed. SARS-CoV-2 main protease (Mpro) is an attractive drug target for antiviral development owing to its key roles in virus replication and host immune evasion. Due to the limitations of currently available methods, the development of novel high-throughput screening assays is of the highest importance for the discovery of Mpro inhibitors. In this study, we first developed an improved fluorescence-based assay for rapid screening of Mpro inhibitors from an anti-infection compound library using a versatile dimerization-dependent red fluorescent protein (ddRFP) biosensor. Utilizing this assay, we identified MG-101 as a competitive Mpro inhibitor in vitro. Moreover, our results revealed that ensitrelvir is a potent Mpro inhibitor, but baicalein, chloroquine, ebselen, echinatin, and silibinin are not. Therefore, this robust ddRFP assay provides a faithful avenue for rapid screening and evaluation of Mpro inhibitors to fight against COVID-19.

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