Design and synthesis of irreversible inhibitors of foot-and-mouth disease virus 3C protease.
نویسندگان
چکیده
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.
منابع مشابه
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 24 2 شماره
صفحات -
تاریخ انتشار 2014