Enzyme inhibition
US6831099B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | May 11, 2000 |
| Grant date | Dec 14, 2004 |
| Priority date | — |
| Expiry date | May 11, 2020 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K7/06
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
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 an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.