脱氮酶
蛋白酵素
化学
吡嗪
泛素
酶
体外
立体化学
高通量筛选
生物化学
组合化学
基因
作者
Matteo Colombo,Stefania Vallese,Ilaria Peretto,Xavier Jacq,Jean‐Christophe Rain,Frédéric Colland,Philippe Guédat
出处
期刊:ChemMedChem
[Wiley]
日期:2010-02-23
卷期号:5 (4): 552-558
被引量:114
标识
DOI:10.1002/cmdc.200900409
摘要
High-throughput screening highlighted 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile (1) as an active inhibitor of ubiquitin-specific proteases (USPs), a family of hydrolytic enzymes involved in the removal of ubiquitin from protein substrates. The chemical behavior of compound 1 was examined. Moreover, the synthesis and in vitro evaluation of new compounds, analogues of 1, led to the identification of potent and selective inhibitors of the deubiquitinating enzyme USP8.
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