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Roqué Rosell, NR, Mokhlesi, L, Milton, NE, Sweeney, TR, Zunszain, PA, Curry, S and Leatherbarrow, RJ (2013) Design and synthesis of irreversible inhibitors of foot-and-mouth disease virus 3C protease. Bioorganic and Medicinal Chemistry Letters, 24 (2). pp. 490-494. ISSN 0960-894X
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Design and synthesis of irreversible inhibitors of Foot-and-mouth disease virus 3C protease.pdf - Accepted Version Available under License Creative Commons Attribution Non-commercial No Derivatives. Download (1MB) | Preview |
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. © 2013 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
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| Uncontrolled Keywords: | 0304 Medicinal And Biomolecular Chemistry, 1115 Pharmacology And Pharmaceutical Sciences, 0305 Organic Chemistry |
| Subjects: | Q Science > QD Chemistry Q Science > QL Zoology R Medicine > RM Therapeutics. Pharmacology |
| Divisions: | Vice-Chancellor's Office |
| Publisher: | Elsevier |
| Date Deposited: | 19 Jun 2018 11:46 |
| Last Modified: | 04 Sep 2021 10:23 |
| DOI or ID number: | 10.1016/j.bmcl.2013.12.045 |
| URI: | https://researchonline.ljmu.ac.uk/id/eprint/8857 |
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