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    Structure-Guided Design and Optimization of Dipeptidyl Inhibitors of Norovirus 3CL Protease. Structure-Activity Relationships and Biochemical, X-ray Crystallographic, Cell-Based, and In Vivo Studies

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    Mehzabeen_2015.pdf (2.889Mb)
    Issue Date
    2015-04-09
    Author
    Kankanamalage, Anushka C. Galasiti
    Kim, Yunjeong
    Weerawarna, Pathum M.
    Uz, Roxanne Adeline Z.
    Damalanka, Vishnu C.
    Mandadapu, Sivakoteswara Rao
    Alliston, Kevin R.
    Mehzabeen, Nurjahan
    Battaile, Kevin P.
    Lovell, Scott
    Chang, Kyeong-Ok
    Groutas, William C.
    Publisher
    American Chemical Society
    Type
    Article
    Article Version
    Scholarly/refereed, author accepted manuscript
    Rights
    This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/jm5019934.
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    Abstract
    Norovirus infection constitutes the primary cause of acute viral gastroenteritis. There are currently no vaccines or norovirus-specific antiviral therapeutics available for the management of norovirus infection. Norovirus 3C-like protease is essential for viral replication, consequently, inhibition of this enzyme is a fruitful avenue of investigation that may lead to the emergence of anti-norovirus therapeutics. We describe herein the optimization of dipeptidyl inhibitors of norovirus 3C-like protease using iterative SAR, X-ray crystallographic, and enzyme and cell-based studies. We also demonstrate herein in vivo efficacy of an inhibitor using the murine model of norovirus infection.
    URI
    http://hdl.handle.net/1808/23628
    DOI
    https://doi.org/10.1021/jm5019934
    Collections
    • Medicinal Chemistry Scholarly Works [225]
    Citation
    Kankanamalage, A. C. G., Kim, Y., Weerawarna, P. M., Uy, R. A. Z., Damalanka, V. C., Mandadapu, S. R., … Groutas, W. C. (2015). Structure-Guided Design and Optimization of Dipeptidyl Inhibitors of Norovirus 3CL Protease. Structure-Activity Relationships and Biochemical, X-ray Crystallographic, Cell-Based, and In Vivo Studies. Journal of Medicinal Chemistry, 58(7), 3144–3155. http://doi.org/10.1021/jm5019934

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    KU Libraries
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    785-864-8983

    KU Libraries
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    Lawrence, KS 66045
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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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