Cited by 113

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Synthesis and Biological Evaluation of 9‐Oxo‐9 H ‐indeno[1,2‐ b ]pyrazine‐2,3‐dicarbonitrile Analogues as Potential Inhibitors of Deubiquitinating Enzymes

Colombo, Matteo, Vallese, Stefania, Peretto, Ilaria, Jacq, Xavier, Rain, Jean‐Christophe, Colland, Frédéric, Guedat, Philippe·2010·ChemMedChem

Abstract

High‐throughput screening highlighted 9‐oxo‐9 H ‐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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Research works printed but not linked: 25

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  21. 10.1063/1.1677527 · DOI
  22. 10.1002/jcc.540141112 · DOI
  23. 10.1063/1.1732476 · DOI
  24. 10.1016/S0065-3276(08)60339-1 · DOI
  25. 10.1021/bi9723360 · DOI

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Metadata

Authors
Colombo, M., Vallese, S., Peretto, I., Jacq, X., Rain, J., Colland, F., & Guedat, P.
Venue
ChemMedChem
Publisher
Wiley
Published
2010-03-30
Volume
5
Issue
4
Pages
552-558
ISSN
  • 1860-7179
  • 1860-7187
Cited by
113
References
1
Language
en

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