abstract |
Peptide-based compounds, which comprise three-membered rings containing heteroatoms, efficiently and selectively inhibit the specific activities of N-terminal nucleophilic (Ntn) hydrolases. The activities of those Ntn having multiple activities can be inhibited differently from the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited by the compounds of the invention. The peptide-based compounds include an epoxide or aziridine and treatment with a characteristic compound at the N-terminus. Among other therapeutic uses, peptide-based compounds are expected to exhibit anti-inflammatory properties and inhibit cell proliferation. |