
Severe acute respiratory syndrome coronavirus (SARS-CoV) emerged in southern China in late 2002 and caused a global outbreak with a fatality rate around 10% in 2003. Ten years later, a second highly pathogenic human CoV, MERS-CoV, emerged in the Middle East and has spread to other countries in Europe, North Africa, North America and Asia. As of November 2017, MERS-CoV had infected at least 2102 people with a fatality rate of about 35% globally, and hence there is an urgent need to identify antiviral drugs that are active against MERS-CoV. Here we show that a clinically available alcohol-aversive drug, disulfiram, can inhibit the papain-like proteases (PLpros) of MERS-CoV and SARS-CoV. Our findings suggest that disulfiram acts as an allosteric inhibitor of MERS-CoV PLpro but as a competitive (or mixed) inhibitor of SARS-CoV PLpro. The phenomenon of slow-binding inhibition and the irrecoverability of enzyme activity after removing unbound disulfiram indicate covalent inactivation of SARS-CoV PLpro by disulfiram, while synergistic inhibition of MERS-CoV PLpro by disulfiram and 6-thioguanine or mycophenolic acid implies the potential for combination treatments using these three clinically available drugs.
Models, Molecular, Dose-Response Relationship, Drug, Molecular Conformation, Microbial Sensitivity Tests, Antiviral Agents, Article, Enzyme Activation, Inhibitory Concentration 50, Severe acute respiratory syndrome-related coronavirus, Disulfiram, Middle East Respiratory Syndrome Coronavirus, Humans, Peptide Hydrolases, Protein Binding
Models, Molecular, Dose-Response Relationship, Drug, Molecular Conformation, Microbial Sensitivity Tests, Antiviral Agents, Article, Enzyme Activation, Inhibitory Concentration 50, Severe acute respiratory syndrome-related coronavirus, Disulfiram, Middle East Respiratory Syndrome Coronavirus, Humans, Peptide Hydrolases, Protein Binding
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