| abstract |
Peptide-based compounds comprising three-membered rings containing heteroatoms efficiently and selectively inhibit specific N-terminal end-associated (Ntn) nucleophilic hydrolases associated with the proteasome. Peptide-based compounds include an epoxide or aziridine, and functionalization at the N. terminus. Among other therapeutic uses, peptide-based compounds are expected to exhibit anti-inflammatory properties and inhibit cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible because of their bioavailability profiles. |