Nature Communications (Oct 2016)

Targeted inhibition of the COP9 signalosome for treatment of cancer

  • Anita Schlierf,
  • Eva Altmann,
  • Jean Quancard,
  • Anne B. Jefferson,
  • René Assenberg,
  • Martin Renatus,
  • Matthew Jones,
  • Ulrich Hassiepen,
  • Michael Schaefer,
  • Michael Kiffe,
  • Andreas Weiss,
  • Christian Wiesmann,
  • Richard Sedrani,
  • Jörg Eder,
  • Bruno Martoglio

DOI
https://doi.org/10.1038/ncomms13166
Journal volume & issue
Vol. 7, no. 1
pp. 1 – 10

Abstract

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Dysregulation of protein degradation by the ubiquitin-proteasome system is a feature commonly associated with cancer. Here, the authors develop an orally available small molecule that inhibits CSN5, the proteolytic subunit of the COP9 signalosome, and blocks tumour growth in a xenograft model.