title: Glutamine vinyl ester proteasome inhibitors selective for trypsin-like (beta2) subunit.
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.
authors.affiliation: Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, Via Fossato di Mortara 17-19, Ferrara, Italy.
authors.forename: Anna
authors.initials: A
authors.lastname: Baldisserotto
authors.forename: Mauro
authors.initials: M
authors.lastname: Marastoni
authors.forename: Claudio
authors.initials: C
authors.lastname: Trapella
authors.forename: Riccardo
authors.initials: R
authors.lastname: Gavioli
authors.forename: Valeria
authors.initials: V
authors.lastname: Ferretti
authors.forename: Loretta
authors.initials: L
authors.lastname: Pretto
authors.forename: Roberto
authors.initials: R
authors.lastname: Tomatis
mesh_terms: 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*
chemical_list: D015853:Cysteine Proteinase Inhibitors; D004952:Esters; D061988:Proteasome Inhibitors; D005973:Glutamine; D014357:Trypsin