| abstract |
Peptide-based compounds, including three-membered rings containing heteroatoms, efficiently and selectively inhibit the specific activities of N-terminal nucleophilic hydrolases (Ntn) associated with the proteosome. Peptide-based compounds include an epoxide or aziridine and N-terminus functionalization. Among other therapeutic utilities, 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 thanks to their bioavailability profiles. |