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• W2077148809 abstract "The 20S proteasome is a multicatalytic protease complex responsible for the degradation of many proteins in mammalian cells. Specific inhibition of proteasome enzymatic subunits represents a topic of great interest for the development of new drug therapies. Following our previous development of a new class of peptide-based inhibitors bearing a C-terminal vinyl ester residue as a pharmacophoric unit that are able to interact with the catalytic threonine, we report here the synthesis and biological properties of a new series of vinyl ester cyclopeptide analogues. Some of these derivatives were shown to inhibit the chymotrypsin-like activity of the proteasome at nanomolar concentration and their potency was found to depend on the size of the tetrapeptidic cyclic portion." @default.
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• W2077148809 date "2008-03-01" @default.
• W2077148809 modified "2023-09-24" @default.
• W2077148809 title "Vinyl ester-based cyclic peptide proteasome inhibitors" @default.
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• W2077148809 doi "https://doi.org/10.1016/j.bmcl.2008.02.016" @default.
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