A robust high-throughput fluorescence polarization assay for rapid of SARS-CoV-2 inhibitors

被引：10

作者：

Yan, Haohao ^{[1
]}

Liu, Zhicheng ^{[1
]}

Yan, Gangan ^{[1
]}

Liu, Xiaoli ^{[1
]}

Liu, Xiaoping ^{[1
]}

Wang, Yanchang ^{[2
]}

Chen, Yunyu ^{[1
]}

机构：

[1] Wannan Med Coll, Inst Drug Screening & Evaluat, Wuhu, Peoples R China

[2] Florida State Univ, Coll Med, Dept Biomed Sci, Tallahassee, FL 32306 USA

来源：

VIROLOGY | 2022年 / 574卷

基金：

中国国家自然科学基金;

关键词：

SARS-CoV-2; Papain-like protease inhibitors; Fluorescence polarization; High -throughput screening; Anacardic acid;

D O I：

10.1016/j.virol.2022.07.006

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

The global scourge of COVID-19 is a serious threat to public health, but effective therapies remain very limited for this disease. Therefore, the discovery of novel antiviral agents is urgently needed to fight against COVID-19. In the lifecycle of SARS-CoV-2, the causing pathogen of COVID-19, papain-like protease (PLpro) is responsible for the cleavage of polyprotein into functional units as well as immune evasion of vaccines. Hence, PLpro has been regarded as an attractive target to develop antiviral agents. Herein, we first developed a robust and simple sandwich-like fluorescence polarization (FP) screening assay for the discovery of PLpro inhibitors, and identified anacardic acid as a novel competitive inhibitor against PLpro in vitro with an IC50 value of 24.26 & PLUSMN; 0.4 mu M. This reliable FP screening assay could provide a prospective avenue for rapid discovery of antiviral agents targeting PLpro in a large-scale screening.

引用

页码：18 / 24

页数：7

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