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
Affiliations
- Akane Kawamura
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Martin Münzel
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Tatsuya Kojima
- Department of Chemistry, Graduate School of Science, The University of Tokyo
- Clarence Yapp
- Structural Genomics Consortium, University of Oxford
- Bhaskar Bhushan
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Yuki Goto
- Department of Chemistry, Graduate School of Science, The University of Tokyo
- Anthony Tumber
- Structural Genomics Consortium, University of Oxford
- Takayuki Katoh
- Department of Chemistry, Graduate School of Science, The University of Tokyo
- Oliver N. F. King
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Toby Passioura
- Department of Chemistry, Graduate School of Science, The University of Tokyo
- Louise J. Walport
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Stephanie B. Hatch
- Structural Genomics Consortium, University of Oxford
- Sarah Madden
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Susanne Müller
- Structural Genomics Consortium, University of Oxford
- Paul E. Brennan
- Structural Genomics Consortium, University of Oxford
- Rasheduzzaman Chowdhury
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Richard J. Hopkinson
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- Hiroaki Suga
- Department of Chemistry, Graduate School of Science, The University of Tokyo
- Christopher J. Schofield
- Department of Chemistry, Chemistry Research Laboratory, University of Oxford
- DOI
- https://doi.org/10.1038/ncomms14773
- Journal volume & issue
-
Vol. 8,
no. 1
pp. 1 – 10
Abstract
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.
