The ubiquitin-proteasome pathway responsible for the turnover of many cellular proteins represents an attractive target in the development of new drug therapies: In particular, modulation of the proteasome activity by specific inhibitors may represent a useful tool for the treatment of tumours. Here, we report synthesis and activity of a new series of oligopseudopeptide analogues bearing a vinyl ketone pharmacophoric unit at the C-terminal position. Some derivatives showed inhibition in the mu M range of the trypsin-like (T-L) active site of the proteasome.

Synthesis and biological properties of C-terminal vinyl ketone pseudotripeptides

TRAPELLA, Claudio;GAVIOLI, Riccardo;MARASTONI, Mauro
2013

Abstract

The ubiquitin-proteasome pathway responsible for the turnover of many cellular proteins represents an attractive target in the development of new drug therapies: In particular, modulation of the proteasome activity by specific inhibitors may represent a useful tool for the treatment of tumours. Here, we report synthesis and activity of a new series of oligopseudopeptide analogues bearing a vinyl ketone pharmacophoric unit at the C-terminal position. Some derivatives showed inhibition in the mu M range of the trypsin-like (T-L) active site of the proteasome.
2013
Franceschini, C; Trapella, Claudio; Sforza, F; Gavioli, Riccardo; Marastoni, Mauro
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2338630
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