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Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease

Authors: Xiaobo Cen; Bing Zhang; Haitao Yang; Yechun Xu; Jiang Wang; Xiong Xie; Zhenming Jin; +22 Authors

Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease

Abstract

Promising antiviral protease inhibitors With no vaccine or proven effective drug against the virus that causes coronavirus disease 2019 (COVID-19), scientists are racing to find clinical antiviral treatments. A promising drug target is the viral main protease M pro , which plays a key role in viral replication and transcription. Dai et al. designed two inhibitors, 11a and 11b, based on analyzing the structure of the M pro active site. Both strongly inhibited the activity of M pro and showed good antiviral activity in cell culture. Compound 11a had better pharmacokinetic properties and low toxicity when tested in mice and dogs, suggesting that this compound is a promising drug candidate. Science , this issue p. 1331

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Keywords

Male, Pneumonia, Viral, Drug Evaluation, Preclinical, Antiviral Agents, Betacoronavirus, Mice, Dogs, Catalytic Domain, Chlorocebus aethiops, Animals, Humans, Pandemics, Research Articles, Coronavirus 3C Proteases, Multidisciplinary, Molecular Structure, COVID-19, Protein Structure, Tertiary, Cysteine Endopeptidases, Drug Design, Female, Coronavirus Infections

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    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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    influence
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    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
1K
Top 0.01%
Top 1%
Top 0.01%
Green
hybrid