Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors

…, A Kazi, F Marsilio, B Fang, WC Guida…

文献索引：Ge, Yiyu; Kazi, Aslamuzzaman; Marsilio, Frank; Luo, Yunting; Jain, Sanjula; Brooks, Wesley; Daniel, Kenyon G.; Guida, Wayne C.; Sebti, Said M.; Lawrence, Harshani R. Journal of Medicinal Chemistry, 2012 , vol. 55, # 5 p. 1978 - 1998

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被引用次数: 10

摘要

Screening of the 50 000 ChemBridge compound library led to the identification of the oxadiazole-isopropylamide 1 (PI-1833) which inhibited chymotrypsin-like (CT-L) activity (IC50= 0.60 μM) with little effects on the other two major proteasome proteolytic activities, trypsin-like (TL) and postglutamyl-peptide-hydrolysis-like (PGPH-L). LC–MS/MS and dialysis show that 1 is a noncovalent and rapidly reversible CT-L inhibitor. Focused library ...