Compounds for enzyme inhibition

Details Compounds for enzyme inhibition Compounds for enzyme inhibition

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) A61K 38/55 (2006.01)

Patent

CA 2629084

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N- terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti¬ inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.

L'invention concerne des composés à base de peptides comprenant des cycles à trois chaînons contenant un hétéroatome, lesquels inhibent efficacement et sélectivement les activités spécifiques d'hydrolases nucléophiles en extrémité N (Ntn) associées au protéasome. Les composés à base de peptides comprennent un époxyde ou une aziridine et une fonctionnalisation à l'extrémité N. Entre autres utilités thérapeutiques, on s'attend à ce que les composés à base de peptides présentent des propriétés anti-inflammatoires et une inhibition de la prolifération des cellules. L'administration orale de ces inhibiteurs de protéasome à base de peptides est possible à cause de leurs profils de biodisponibilité.

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