Inhibition of norovirus 3CL protease by bisulfite adducts of transition state inhibitors

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dc.contributor.author Mandadapu, Sivakoteswara Rao
dc.contributor.author Gunnam, Mallikarjuna Reddy
dc.contributor.author Tiew, Kok-Chuan
dc.contributor.author Uy, Roxanne Adeline Z.
dc.contributor.author Prior, Allan M.
dc.contributor.author Alliston, Kevin R.
dc.contributor.author Hua, Duy H.
dc.contributor.author Kim, Yunjeong
dc.contributor.author Chang, Kyeong-Ok
dc.contributor.author Groutas, William C.
dc.date.accessioned 2012-12-18T17:25:32Z
dc.date.available 2012-12-18T17:25:32Z
dc.date.issued 2013-01-01
dc.identifier.uri http://hdl.handle.net/2097/15183
dc.description.abstract Noroviruses are the most common cause of acute viral gastroenteritis, accounting for >21 million cases annually in the U.S. alone. Norovirus infections constitute an important health problem for which there are no specific antiviral therapeutics or vaccines. In this study, a series of bisulfite adducts derived from representative transition state inhibitors (dipeptidyl aldehydes and α-ketoamides) was synthesized and shown to exhibit anti-norovirus activity in a cell-based replicon system. The ED[subscript 50] of the most effective inhibitor was 60 nM. This study demonstrates for the first time the utilization of bisulfite adducts of transition state inhibitors in the inhibition of norovirus 3CL protease in vitro and in a cell-based replicon system. The approach described herein can be extended to the synthesis of the bisulfite adducts of other classes of transition state inhibitors of serine and cysteine proteases, such as α-ketoheterocycles, α-ketoesters, and others. en_US
dc.language.iso en_US en_US
dc.relation.uri http://doi.org/10.1016/j.bmcl.2012.11.026 en_US
dc.rights This Item is protected by copyright and/or related rights. You are free to use this Item in any way that is permitted by the copyright and related rights legislation that applies to your use. For other uses you need to obtain permission from the rights-holder(s).
dc.rights.uri http://rightsstatements.org/vocab/InC/1.0/
dc.subject Norovirus 3CL protease en_US
dc.subject Bisulfite salt adducts en_US
dc.subject Transition state inhibitors en_US
dc.title Inhibition of norovirus 3CL protease by bisulfite adducts of transition state inhibitors en_US
dc.type Article (author version) en_US
dc.date.published 2013 en_US
dc.citation.doi 10.1016/j.bmcl.2012.11.026 en_US
dc.citation.epage 65 en_US
dc.citation.issue 1 en_US
dc.citation.jtitle Bioorganic & Medicinal Chemistry Letters en_US
dc.citation.spage 62 en_US
dc.citation.volume 23 en_US
dc.contributor.authoreid duy en_US
dc.contributor.authoreid ykim en_US
dc.contributor.authoreid kchang en_US


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This Item is protected by copyright and/or related rights. You are free to use this Item in any way that is permitted by the copyright and related rights legislation that applies to your use. For other uses you need to obtain permission from the rights-holder(s). Except where otherwise noted, the use of this item is bound by the following: This Item is protected by copyright and/or related rights. You are free to use this Item in any way that is permitted by the copyright and related rights legislation that applies to your use. For other uses you need to obtain permission from the rights-holder(s).

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