摘要 |
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.
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申请人 |
PROTEOLIX, INC.;BENNETT, MARK, K.;BUCHHOLZ, TONIA, J.;DEMO, SUSAN;LAIDIG, GUY, J.;LEWIS, EVAN, R.;SMYTH, MARK, S. |
发明人 |
BENNETT, MARK, K.;BUCHHOLZ, TONIA, J.;DEMO, SUSAN;LAIDIG, GUY, J.;LEWIS, EVAN, R.;SMYTH, MARK, S. |