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 associated with the proteasome. 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. Oral administration of these peptide-based proteasomeinhibitors is possible due to their bioavailability profiles.