dc.contributor.author | Kankanamalage, Anushka C. Galasiti | |
dc.contributor.author | Kim, Yunjeong | |
dc.contributor.author | Weerawarna, Pathum M. | |
dc.contributor.author | Uz, Roxanne Adeline Z. | |
dc.contributor.author | Damalanka, Vishnu C. | |
dc.contributor.author | Mandadapu, Sivakoteswara Rao | |
dc.contributor.author | Alliston, Kevin R. | |
dc.contributor.author | Mehzabeen, Nurjahan | |
dc.contributor.author | Battaile, Kevin P. | |
dc.contributor.author | Lovell, Scott | |
dc.contributor.author | Chang, Kyeong-Ok | |
dc.contributor.author | Groutas, William C. | |
dc.date.accessioned | 2017-04-12T15:21:39Z | |
dc.date.available | 2017-04-12T15:21:39Z | |
dc.date.issued | 2015-04-09 | |
dc.identifier.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 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/23628 | |
dc.description.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. | en_US |
dc.publisher | American Chemical Society | en_US |
dc.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. | en_US |
dc.title | 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 | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Mehzabeen, Nurjahan | |
kusw.kuauthor | Lovell, Scott | |
kusw.kudepartment | Medicinal Chemistry | en_US |
dc.identifier.doi | 10.1021/jm5019934 | en_US |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.rights.accessrights | openAccess | |