A robust high-throughput fluorescent polarization assay for the evaluation and screening of SARS-CoV-2 fusion inhibitors

doi:10.1016/j.bioorg.2021.105362

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	A robust high-throughput fluorescent polarization assay for the evaluation and screening of SARS-CoV-2 fusion inhibitors
	X. J. Yin; L. T. Chen; S. W. Yuan; L. Liu and Z. Z. Gao
	2021
发表期刊	Bioorganic Chemistry
ISSN	0045-2068
卷号	116 期号:7 页码:2341-2363
摘要	Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is a serious threat to global health. One attractive antiviral target is the membrane fusion mechanism employed by the virus to gain access to the host cell. Here we report a robust protein-based fluorescent polarization assay, that mimicking the formation of the sixhelix bundle (6-HB) process during the membrane fusion, for the evaluation and screening of SARS-CoV-2 fusion Inhibitors. The IC50 of known inhibitors, HR2P, EK1, and Salvianolic acid C (Sal-C) were measured to be 6.1 nM, 2.5 nM, and 8.9 mu M respectively. In addition, we found Sal-A has a slightly lower IC50 (3.9 mu M) than Sal-C. Interestingly, simple caffeic acid can also disrupt the formation of 6-HB with a sub-mM concentration. Pilot high throughput screening (HTS) of a small marine natural product library validates the assay with a Z' factor close to 0.8. We envision the current assay provides a convenient way to screen SARS-CoV-2 fusion inhibitors and assess their binding affinity.
DOI	10.1016/j.bioorg.2021.105362
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收录类别	SCI
引用统计
文献类型	期刊论文
条目标识符	http://ir.ciomp.ac.cn/handle/181722/65605
专题	中国科学院长春光学精密机械与物理研究所
推荐引用方式 GB/T 7714	X. J. Yin,L. T. Chen,S. W. Yuan,et al. A robust high-throughput fluorescent polarization assay for the evaluation and screening of SARS-CoV-2 fusion inhibitors[J]. Bioorganic Chemistry,2021,116(7):2341-2363.
APA	X. J. Yin,L. T. Chen,S. W. Yuan,&L. Liu and Z. Z. Gao.(2021).A robust high-throughput fluorescent polarization assay for the evaluation and screening of SARS-CoV-2 fusion inhibitors.Bioorganic Chemistry,116(7),2341-2363.
MLA	X. J. Yin,et al."A robust high-throughput fluorescent polarization assay for the evaluation and screening of SARS-CoV-2 fusion inhibitors".Bioorganic Chemistry 116.7(2021):2341-2363.

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