α,β-Unsaturated <i>N</i>-Acylpyrrole Peptidyl Derivatives: New Proteasome Inhibitors
Anna Baldisserotto
Valeria Ferretti
Federica Destro
Christian Franceschini
Mauro Marastoni
Riccardo Gavioli
Roberto Tomatis
10.1021/jm100122e.s001
https://acs.figshare.com/articles/journal_contribution/_Unsaturated_i_N_i_Acylpyrrole_Peptidyl_Derivatives_New_Proteasome_Inhibitors/2732047
Because of the encouraging results obtained using vinyl ester derivatives, we synthesized and tested a novel series of peptide-based proteasome inhibitors bearing a new pharmacophore unit at the C-terminal. <i>N</i>-Acylpyrrole moiety is a potential substrate for Michael addition by catalytic threonine. Several analogues have demonstrated a selective inhibition of the multicatalytic complex β1 subunits, the capacity to permeate cellular membrane, and good pharmacokinetics properties.
2010-09-09 00:00:00
vinyl ester derivatives
Derivative
moiety
capacity
Michael addition
multicatalytic
pharmacophore unit
pharmacokinetics properties
membrane
Several analogues
proteasome
Peptidyl
β1 subunits
inhibition
threonine
substrate
New Proteasome InhibitorsBecause
novel series
inhibitor
Unsaturated