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Inhibition of SARS-CoV 3CL protease by flavonoids

Open access
Jo, Seri, Kim, Suwon, Shin, Dong Hae, Kim, Mi-Sun·2020·Journal of Enzyme Inhibition and Medicinal Chemistry

Abstract

There were severe panics caused by Severe Acute Respiratory Syndrome (SARS) and Middle-East Respiratory Syndrome-Coronavirus. Therefore, researches targeting these viruses have been required. Coronaviruses (CoVs) have been rising targets of some flavonoids. The antiviral activity of some flavonoids against CoVs is presumed directly caused by inhibiting 3C-like protease (3CLpro). Here, we applied a flavonoid library to systematically probe inhibitory compounds against SARS-CoV 3CLpro. Herbacetin, rhoifolin and pectolinarin were found to efficiently block the enzymatic activity of SARS-CoV 3CLpro. The interaction of the three flavonoids was confirmed using a tryptophan-based fluorescence method, too. An induced-fit docking analysis indicated that S1, S2 and S3' sites are involved in binding with flavonoids. The comparison with previous studies showed that Triton X-100 played a critical role in objecting false positive or overestimated inhibitory activity of flavonoids. With the systematic analysis, the three flavonoids are suggested to be templates to design functionally improved inhibitors.

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Metadata

Authors
Jo, S., Kim, S., Shin, D. H., & Kim, M.-S.
Venue
Journal of Enzyme Inhibition and Medicinal Chemistry
Published
2019-11-14
Volume
35
Issue
1
Pages
145-151
ISSN
  • 1475-6366 (ISSN-L)
  • 1475-6374
OpenAlex
W2985346127
Cited by
685
References
3
FWCI
88.72
Type
journal article
Language
en
Open access
gold

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CoChat. (2026). Citation check: Inhibition of SARS-CoV 3CL protease by flavonoids. https://app.cochat.ai/papers/10.1080/14756366.2019.1690480
The paper
Jo, S., Kim, S., Shin, D. H., & Kim, M.-S. (2020). Inhibition of SARS-CoV 3CL protease by flavonoids. Journal of Enzyme Inhibition and Medicinal Chemistry. https://doi.org/10.1080/14756366.2019.1690480

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.