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.

Graphical abstractNew glutamine vinyl ester pseudopeptides were prepared and tested as selective β2 subunit proteasome inhibitorsFigure optionsDownload full-size imageDownload as PowerPoint slide