Title |
Design and synthesis of irreversible inhibitors of foot-and-mouth disease virus 3C protease
|
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Published in |
Bioorganic & Medicinal Chemistry Letters, December 2013
|
DOI | 10.1016/j.bmcl.2013.12.045 |
Pubmed ID | |
Authors |
Núria R. Roqué Rosell, Ladan Mokhlesi, Nicholas E. Milton, Trevor R. Sweeney, Patricia A. Zunszain, Stephen Curry, Robin J. Leatherbarrow |
Abstract |
Foot-and-mouth disease virus (FMDV) causes a highly infectious and economically devastating disease of livestock. The FMDV genome is translated as a single polypeptide precursor that is cleaved into functional proteins predominantly by the highly conserved viral 3C protease, making this enzyme an attractive target for antiviral drugs. A peptide corresponding to an optimal substrate has been modified at the C-terminus, by the addition of a warhead, to produce irreversible inhibitors that react as Michael acceptors with the enzyme active site. Further investigation highlighted key structural determinants for inhibition, with a positively charged P2 being particularly important for potency. |
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Mendeley readers
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