Han-Jie Zhou,Congcong M. Sun,Kevin D. Shenk,Guy J. Laidig
申请号:
US15606076
公开号:
US10150794B2
申请日:
2017.05.26
申请国别(地区):
US
年份:
2018
代理人:
摘要:
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.