Glutamine vinyl ester proteasome inhibitors selective for trypsin-like (β2) subunit

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 β2 subunit and good enzymatic stability.

New glutamine vinyl ester pseudopeptides were prepared and tested as selective β2 subunit proteasome inhibitorsFigure optionsDownload as PowerPoint slide