Nature Communications (Apr 2017)

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

  • Akane Kawamura,
  • Martin Münzel,
  • Tatsuya Kojima,
  • Clarence Yapp,
  • Bhaskar Bhushan,
  • Yuki Goto,
  • Anthony Tumber,
  • Takayuki Katoh,
  • Oliver N. F. King,
  • Toby Passioura,
  • Louise J. Walport,
  • Stephanie B. Hatch,
  • Sarah Madden,
  • Susanne Müller,
  • Paul E. Brennan,
  • Rasheduzzaman Chowdhury,
  • Richard J. Hopkinson,
  • Hiroaki Suga,
  • Christopher J. Schofield

Journal volume & issue
Vol. 8, no. 1
pp. 1 – 10


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JmjC histone demethylases (KDMs) are cancer targets due to their links to cell proliferation, but selective inhibition remains a challenge. Here the authors identify potent inhibitors of KDM4A-C—viain vitroselection from a vast library of cyclic peptides—that show selectivity over other KDMs.