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- W2167129369 abstract "Peptide epoxyketones are potent and selective proteasome inhibitors. Selectivity is governed by the epoxyketone dual electrophilic warhead, which reacts with the N-terminal threonine 1,2-amino alcohol uniquely present in proteasome active sites. We studied a series of C-terminally modified oligopeptides featuring adjacent electrophiles based on the epoxyketone warhead. We found that the carbonyl moiety in the natural warhead is essential, but that the adjacent epoxide can be replaced by a carbonyl, though with considerable loss of activity." @default.
- W2167129369 created "2016-06-24" @default.
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- W2167129369 date "2014-01-01" @default.
- W2167129369 modified "2023-10-18" @default.
- W2167129369 title "Exploring dual electrophiles in peptide-based proteasome inhibitors: carbonyls and epoxides" @default.
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- W2167129369 doi "https://doi.org/10.1039/c4ob00893f" @default.
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