- Synthesis and biological evaluation of 9-oxo-9hindeno[1,2-b]pyrazine-2,3- dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes
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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.
- Colombo, Matteo,Vallese, Stefania,Peretto, Ilaria,Jacq, Xavier,Rain, Jean-Christophe,Colland, Frederic,Guedat, Philippe
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experimental part
p. 552 - 558
(2010/12/25)
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- Novel cysteine protease inhibitors and their therapeutic applications
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The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
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Page/Page column 24
(2008/06/13)
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