期刊
CHEMMEDCHEM
卷 5, 期 4, 页码 552-558出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.200900409
关键词
drug discovery; heterocycles; inhibitors; proteases; ubiquitin
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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