
pmid: 32105468
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.
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
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
| 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). | 104 | |
| 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. | Top 1% | |
| influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | Top 10% | |
| impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network. | Top 1% |
