Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease

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dc.creatorFu, Lifeng
dc.creatorYe, Fei
dc.creatorFeng, Yong
dc.creatorYu, Feng
dc.creatorWang, Qisheng
dc.creatorWu, Yan
dc.creatorZhao, Cheng
dc.creatorSun, Huan
dc.creatorHuang, Baoying
dc.creatorNiu, Peihua
dc.creatorSong, Hao
dc.creatorShi, Yi
dc.creatorLi, Xuebing
dc.creatorTan, Wenjie
dc.creatorQi, Jianxun
dc.creatorGao, George Fu
dc.date.accessioned2020-09-18T03:39:17Z
dc.date.available2020-09-18T03:39:17Z
dc.date.created2020-09-04
dc.description.abstractenglishCOVID-19 was declared a pandemic on March 11 by WHO, due to its great threat to global public health. The coronavirus main protease (Mpro, also called 3CLpro) is essential for processing and maturation of the viral polyprotein, therefore recognized as an attractive drug target. Here we show that a clinically approved anti-HCV drug, Boceprevir, and a pre-clinical inhibitor against feline infectious peritonitis (corona) virus (FIPV), GC376, both efficaciously inhibit SARS-CoV-2 in Vero cells by targeting Mpro. Moreover, combined application of GC376 with Remdesivir, a nucleotide analogue that inhibits viral RNA dependent RNA polymerase (RdRp), results in sterilizing additive effect. Further structural analysis reveals binding of both inhibitors to the catalytically active side of SARS-CoV-2 protease Mpro as main mechanism of inhibition. Our findings may provide critical information for the optimization and design of more potent inhibitors against the emerging SARS-CoV-2 virus.spa
dc.format.extent8 páginasspa
dc.format.mimetypeapplication/pdfspa
dc.identifier.doihttps://doi.org/10.1038/s41467-020-18233-xspa
dc.identifier.issn2041-1723spa
dc.identifier.otherhttps://www.nature.com/articles/s41467-020-18233-x#article-infospa
dc.identifier.urihttps://hdl.handle.net/20.500.12010/13444
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.lembSíndrome respiratorio agudo gravespa
dc.subject.lembCOVID-19spa
dc.subject.lembSARS-CoV-2spa
dc.subject.lembCoronavirusspa
dc.titleBoth Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main proteasespa
dc.type.coarhttp://purl.org/coar/resource_type/c_6501spa
dc.type.hasversioninfo:eu-repo/semantics/acceptedVersionspa
dc.type.localArtículospa

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