Glutamine vinyl ester proteasome inhibitors selective for trypsin-like (beta2) 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 beta2 subunit and good enzymatic stability.
Baldisserotto
Anna
A
Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, Via Fossato di Mortara 17-19, Ferrara, Italy.
Marastoni
Mauro
M
Trapella
Claudio
C
Gavioli
Riccardo
R
Ferretti
Valeria
V
Pretto
Loretta
L
Tomatis
Roberto
R
D015853:Cysteine Proteinase Inhibitors / Q000494:pharmacology*; D004952:Esters; D005973:Glutamine / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D061988:Proteasome Inhibitors; D014357:Trypsin / Q000737:chemistry / Q000187:drug effects*
D015853:Cysteine Proteinase Inhibitors; D004952:Esters; D061988:Proteasome Inhibitors; D005973:Glutamine; D014357:Trypsin