abstract |
Peptide-based compounds containing a heteroatom-bearing, 3-membered ring efficiently and selectively inhibit the specific activity of the N-terminal nucleophile (Ntn) hydrolase linked to a proteasome. These peptide-based compounds include functionalization at the epoxide or aziridine and the N-terminus. In other therapeutic applications, these peptide-based compounds are expected to exhibit anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profile. [Index] Proteasome inhibiting substance |