Labeled compounds for proteasome inhibition

Details Labeled compounds for proteasome inhibition Labeled compounds for proteasome inhibition

C - Chemistry, Metallurgy

07

K

C07K 5/087 (2006.01) A61K 38/06 (2006.01) C07K 5/08 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2584515

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus, such as a detectable label. Along with therapeutic utilities, these peptide based compounds can be used in assays useful for screening, monitoring, diagnostic and/or dosing purposes.

L'invention concerne des composés à base de peptides comprenant des noyaux à trois éléments contenant un hétéroatome, lesdits composés inhibant efficacement et sélectivement des activités spécifiques d'hydrolases de nucléophile N-terminal (Ntn). Les activités de ces Ntn à activités multiples peuvent être inhibées de manière différentielle par les composés susmentionnés. Par exemple, les activités de type chymotrypsine et PGPH du protéasome 20S peuvent être inhibées sélectivement au moyen des composés de l'invention. Ces composés à base de peptides renferment au moins trois unités peptidiques, un époxyde ou une aziridine, et une fonctionnalisation en terminaison N, telle qu'un marqueur détectable. Outre leur utilité thérapeutique, ces composés à base de peptides peuvent être utilisés dans des méthodes de criblage, de surveillance, de diagnostic et/ou de dosage.

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