COMPOUNDS FOR INHIBITION OF CHYMOTRYPSIN-LIKE ACTIVITY OF THE 20S PROTEASOME

摘要

Peptide-based compounds including heteroatom-containing, three-membered ringsefficiently and selectively inhibit specific activities of N-terminalnucleophile (Ntn) hydrolases. The activities of those Ntn having multipleactivities can be differentially inhibited by the compounds described. Forexample, the chymotrypsin-like activity of the 20S proteasome may beselectively inhibited with the inventive compounds. The peptide-basedcompounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds areexpected to display anti-inflammatory properties and inhibition of cellproliferation.