Small-Molecule Antiviral β- <scp>d</scp> - <i>N</i> <sup>4</sup> -Hydroxycytidine Inhibits a Proofreading-Intact Coronavirus with a High Genetic Barrier to Resistance

  • Maria L. Agostini
    Department of Pathology, Microbiology, and Immunology, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
  • Andrea J. Pruijssers
    Department of Pediatrics, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
  • James D. Chappell
    Department of Pediatrics, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
  • Jennifer Gribble
    Department of Pathology, Microbiology, and Immunology, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
  • Xiaotao Lu
    Department of Pediatrics, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
  • Erica L. Andres
    Department of Pediatrics, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
  • Gregory R. Bluemling
    Emory Institute for Drug Development, Emory University, Atlanta, Georgia, USA
  • Mark A. Lockwood
    Emory Institute for Drug Development, Emory University, Atlanta, Georgia, USA
  • Timothy P. Sheahan
    Department of Epidemiology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
  • Amy C. Sims
    Department of Epidemiology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
  • Michael G. Natchus
    Emory Institute for Drug Development, Emory University, Atlanta, Georgia, USA
  • Manohar Saindane
    Emory Institute for Drug Development, Emory University, Atlanta, Georgia, USA
  • Alexander A. Kolykhalov
    Emory Institute for Drug Development, Emory University, Atlanta, Georgia, USA
  • George R. Painter
    Emory Institute for Drug Development, Emory University, Atlanta, Georgia, USA
  • Ralph S. Baric
    Department of Epidemiology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
  • Mark R. Denison
    Department of Pathology, Microbiology, and Immunology, Vanderbilt University School of Medicine, Nashville, Tennessee, USA

書誌事項

公開日
2019-12
権利情報
  • https://journals.asm.org/non-commercial-tdm-license
DOI
  • 10.1128/jvi.01348-19
公開者
American Society for Microbiology

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説明

<jats:p> The emergence of coronaviruses (CoVs) into human populations from animal reservoirs has demonstrated their epidemic capability, pandemic potential, and ability to cause severe disease. However, no antivirals have been approved to treat these infections. Here, we demonstrate the potent antiviral activity of a broad-spectrum ribonucleoside analogue, β- <jats:sc>d</jats:sc> - <jats:italic>N</jats:italic> <jats:sup>4</jats:sup> -hydroxycytidine (NHC), against two divergent CoVs. Viral proofreading activity does not markedly impact sensitivity to NHC inhibition, suggesting a novel interaction between a nucleoside analogue inhibitor and the CoV replicase. Further, passage in the presence of NHC generates only low-level resistance, likely due to the accumulation of multiple potentially deleterious transition mutations. Together, these data support a mutagenic mechanism of inhibition by NHC and further support the development of NHC for treatment of CoV infections. </jats:p>

収録刊行物

  • Journal of Virology

    Journal of Virology 93 (24), e01348-19-, 2019-12

    American Society for Microbiology

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