Feline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replication

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dc.creatorVuong, Wayne
dc.creatorKhan, Muhammad Bashir
dc.creatorFischer, Conrad
dc.creatorArutyunova, Elena
dc.creatorLamer, Tess
dc.creatorShields, Justin
dc.creatorSaffran, Holly A
dc.creatorMcKay, Ryan T
dc.creatorvan Belkum, Marco J
dc.creatorJoyce, Michael A
dc.creatorYoung, Howard S
dc.creatorTyrrell, D Lorne
dc.creatorVederas, John C
dc.creatorLemieux, M Joanne
dc.date.accessioned2020-09-18T02:53:43Z
dc.date.available2020-09-18T02:53:43Z
dc.date.created2020-08-27
dc.description.abstractenglishThe main protease, Mpro (or 3CLpro) in SARS-CoV-2 is a viable drug target because of its essential role in the cleavage of the virus polypeptide. Feline infectious peritonitis, a fatal coronavirus infection in cats, was successfully treated previously with a prodrug GC376, a dipeptide-based protease inhibitor. Here, we show the prodrug and its parent GC373, are effective inhibitors of the Mpro from both SARS-CoV and SARS-CoV-2 with IC50 values in the nanomolar range. Crystal structures of SARS-CoV-2 Mpro with these inhibitors have a covalent modification of the nucleophilic Cys145. NMR analysis reveals that inhibition proceeds via reversible formation of a hemithioacetal. GC373 and GC376 are potent inhibitors of SARS-CoV-2 replication in cell culture. They are strong drug candidates for the treatment of human coronavirus infections because they have already been successful in animals. The work here lays the framework for their use in human trials for the treatment of COVID-19.spa
dc.format.extent8 páginasspa
dc.format.mimetypeapplication/pdfspa
dc.identifier.doihttps://doi.org/10.1038/s41467-020-18096-2spa
dc.identifier.issn2041-1723spa
dc.identifier.otherhttps://www.nature.com/articles/s41467-020-18096-2#article-infospa
dc.identifier.urihttps://hdl.handle.net/20.500.12010/13433
dc.language.isoengspa
dc.publisherNature Communicationsspa
dc.rights.accessrightsinfo:eu-repo/semantics/openAccessspa
dc.rights.localAbierto (Texto Completo)spa
dc.sourcereponame:Expeditio Repositorio Institucional UJTLspa
dc.sourceinstname:Universidad de Bogotá Jorge Tadeo Lozanospa
dc.subjectSARS-CoV-2spa
dc.subject.keywordSARS-CoV-2spa
dc.subject.keywordFeline coronavirusspa
dc.subject.lembSíndrome respiratorio agudo gravespa
dc.subject.lembCOVID-19spa
dc.subject.lembSARS-CoV-2spa
dc.subject.lembCoronavirusspa
dc.titleFeline coronavirus drug inhibits the main protease of SARS-CoV-2 and blocks virus replicationspa
dc.type.coarhttp://purl.org/coar/resource_type/c_6501spa
dc.type.hasversioninfo:eu-repo/semantics/acceptedVersionspa
dc.type.localArtículospa

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