Here we report the study of a new series of peptide-based proteasome inhibitors with a vinyl ester moiety at C-terminal. The presence of Tic, a rigid analogue of phenylalanine, in the central portion of some derivatives is not favourable for the activity. The best analogue of the series shows a potent and selective inhibition for the beta2 subunit and good enzymatic stability.
Glutamine vinyl ester proteasome inhibitors selective for trypsin-like (beta2) subunit
BALDISSEROTTO, Anna;MARASTONI, Mauro;TRAPELLA, Claudio;GAVIOLI, Riccardo;FERRETTI, Valeria;PRETTO, Loretta;TOMATIS, Roberto
2007
Abstract
Here we report the study of a new series of peptide-based proteasome inhibitors with a vinyl ester moiety at C-terminal. The presence of Tic, a rigid analogue of phenylalanine, in the central portion of some derivatives is not favourable for the activity. The best analogue of the series shows a potent and selective inhibition for the beta2 subunit and good enzymatic stability.File in questo prodotto:
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