Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

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.

Bibliographic Details
Main Authors:	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
Format:	Article
Language:	English
Published:	Nature Publishing Group 2017-04-01
Series:	Nature Communications
Online Access:	https://doi.org/10.1038/ncomms14773

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spelling	doaj-ef8ec2f09725496691198a2fa7af4d882021-05-11T07:33:15ZengNature Publishing GroupNature Communications2041-17232017-04-018111010.1038/ncomms14773Highly selective inhibition of histone demethylases by de novo macrocyclic peptidesAkane Kawamura0Martin Münzel1Tatsuya Kojima2Clarence Yapp3Bhaskar Bhushan4Yuki Goto5Anthony Tumber6Takayuki Katoh7Oliver N. F. King8Toby Passioura9Louise J. Walport10Stephanie B. Hatch11Sarah Madden12Susanne Müller13Paul E. Brennan14Rasheduzzaman Chowdhury15Richard J. Hopkinson16Hiroaki Suga17Christopher J. Schofield18Department of Chemistry, Chemistry Research Laboratory, University of OxfordDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordDepartment of Chemistry, Graduate School of Science, The University of TokyoStructural Genomics Consortium, University of OxfordDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordDepartment of Chemistry, Graduate School of Science, The University of TokyoStructural Genomics Consortium, University of OxfordDepartment of Chemistry, Graduate School of Science, The University of TokyoDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordDepartment of Chemistry, Graduate School of Science, The University of TokyoDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordStructural Genomics Consortium, University of OxfordDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordStructural Genomics Consortium, University of OxfordStructural Genomics Consortium, University of OxfordDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordDepartment of Chemistry, Graduate School of Science, The University of TokyoDepartment of Chemistry, Chemistry Research Laboratory, University of OxfordJmjC 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.https://doi.org/10.1038/ncomms14773
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	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
spellingShingle	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 Highly selective inhibition of histone demethylases by de novo macrocyclic peptides Nature Communications
author_facet	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
author_sort	Akane Kawamura
title	Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
title_short	Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
title_full	Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
title_fullStr	Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
title_full_unstemmed	Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
title_sort	highly selective inhibition of histone demethylases by de novo macrocyclic peptides
publisher	Nature Publishing Group
series	Nature Communications
issn	2041-1723
publishDate	2017-04-01
description	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.
url	https://doi.org/10.1038/ncomms14773
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Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

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