Oxadiazole-isopropylamides as Potent and Non-covalent Proteasome Inhibitors

Screening of the 50,000 ChemBridge compound library led to the identification of the oxadiazole-isopropylamide 1 (PI-1833) which inhibited CT-L activity (IC(50) 0.60 μM) with little effects on the other 2 major proteasome proteolytic activities, T-L and PGPH-L. LC/MS-MS and dialysis show that 1 is a...

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Bibliografiske detaljer
Main Authors: Ozcan, Sevil, Kazi, Aslamuzzaman, Marsilio, Frank, Fang, Bin, Guida, Wayne C., Koomen, John, Lawrence, Harshani R., Sebti, Saïd M.
Format: Artigo
Sprog:Inglês
Udgivet: 2013
Fag:
Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3774303/
https://ncbi.nlm.nih.gov/pubmed/23547706
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm400221d
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