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Journal of Medicinal Chemistry
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Journal of Medicinal Chemistry
Article . 2020 . Peer-reviewed
Data sources: Crossref
Journal of Medicinal Chemistry
Article . 2020 . Peer-reviewed
Data sources: Crossref
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Structure-Based Stabilization of Non-native Protein–Protein Interactions of Coronavirus Nucleocapsid Proteins in Antiviral Drug Design

Authors: Lin, Shan-Meng; Lin, Shih-Chao; Hsu, Jia-Ning; Chang, Chung-ke; Chien, Ching-Ming; Wang, Yong-Sheng; Wu, Hung-Yi; +3 Authors

Structure-Based Stabilization of Non-native Protein–Protein Interactions of Coronavirus Nucleocapsid Proteins in Antiviral Drug Design

Abstract

Structure-based stabilization of protein-protein interactions (PPIs) is a promising strategy for drug discovery. However, this approach has mainly focused on the stabilization of native PPIs, and non-native PPIs have received little consideration. Here, we identified a non-native interaction interface on the three-dimensional dimeric structure of the N-terminal domain of the MERS-CoV nucleocapsid protein (MERS-CoV N-NTD). The interface formed a conserved hydrophobic cavity suitable for targeted drug screening. By considering the hydrophobic complementarity during the virtual screening step, we identified 5-benzyloxygramine as a new N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities. X-ray crystallography and small-angle X-ray scattering showed that 5-benzyloxygramine stabilizes the N-NTD dimers through simultaneous hydrophobic interactions with both partners, resulting in abnormal N protein oligomerization that was further confirmed in the cell. This unique approach based on the identification and stabilization of non-native PPIs of N protein could be applied toward drug discovery against CoV diseases.

Keywords

Indoles, Nucleocapsid Proteins, Crystallography, X-Ray, Antiviral Agents, Molecular Docking Simulation, Alkaloids, Protein Domains, Drug Design, Chlorocebus aethiops, Drug Discovery, Middle East Respiratory Syndrome Coronavirus, Animals, Coronavirus Nucleocapsid Proteins, Molecular Medicine, Amino Acid Sequence, Protein Multimerization, Hydrophobic and Hydrophilic Interactions, Sequence Alignment, Vero Cells, Protein Binding

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    popularity
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    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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selected citations
These citations are derived from selected sources.
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!
104
Top 1%
Top 10%
Top 1%
hybrid