PropertyValue
?:abstract
  • In December 2019, the first cases of infection with a novel coronavirus, SARS-CoV-2, were diagnosed. Currently, there is no effective antiviral treatment for COVID-19. To address this emerging problem, we focused on the SARS-CoV-2 main protease that constitutes one of the most attractive antiviral drug targets. We have synthesized a combinatorial library of fluorogenic substrates with glutamine in the P1 position. We used it to determine the substrate preferences of the SARS-CoV and SARS-CoV-2 main proteases. On the basis of these findings, we designed and synthesized a potent SARS-CoV-2 inhibitor (Ac-Abu-DTyr-Leu-Gln-VS, half-maximal effective concentration of 3.7 µM) and two activity-based probes, for one of which we determined the crystal structure of its complex with the SARS-CoV-2 Mpro. We visualized active SARS-CoV-2 Mpro in nasopharyngeal epithelial cells of patients suffering from COVID-19 infection. The results of our work provide a structural framework for the design of inhibitors as antiviral agents and/or diagnostic tests.
is ?:annotates of
?:creator
?:doi
  • 10.1038/s41589-020-00689-z
?:doi
?:journal
  • Nature_chemical_biology
?:license
  • unk
?:pmid
?:pmid
  • 33093684.0
?:publication_isRelatedTo_Disease
is ?:relation_isRelatedTo_publication of
?:source
  • Medline
?:title
  • SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging.
?:type
?:year
  • 2020-10-22

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