US Patent:
20070105786, May 10, 2007
Inventors:
Han-Jie Zhou - Foster City CA, US
Congcong Sun - Cupertino CA, US
Kevin Shenk - Palo Alto CA, US
Guy Laidig - Menlo Park CA, US
Assignee:
Proteolix, Inc. - South San Francisco CA
International Classification:
A61K 38/04
C07K 5/06
US Classification:
514019000, 548954000, 549090000, 549551000
Abstract:
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