The small molecule JIB-04 disrupts O2 binding in the Fe-dependent histone demethylase KDM4A/JMJD2A

Barbara Cascella; Soon Goo Lee; Sukrit Singh; Joseph M. Jez; Liviu M. Mirica

doi:10.1039/C6CC09882G

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The small molecule JIB-04 disrupts O₂ binding in the Fe-dependent histone demethylase KDM4A/JMJD2A†

Barbara Cascella,

^ab Soon Goo Lee,^b Sukrit Singh,

^a Joseph M. Jez*^b and Liviu M. Mirica

*^a

Author affiliations

* Corresponding authors

^a Department of Chemistry, Washington University, St. Louis, Missouri 63130, USA
E-mail: mirica@wustl.edu

^b Department of Biology, Washington University, St. Louis, Missouri 63130, USA
E-mail: jjez@wustl.edu

Abstract

JIB-04, a specific inhibitor of the O₂-activating, Fe-dependent histone lysine demethylases, is revealed to disrupt the binding of O₂ in KDM4A/JMJD2A through a continuous O₂-consumption assay, X-ray crystal structure data, and molecular docking.

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Article information

DOI: https://doi.org/10.1039/C6CC09882G
Article type: Communication
Submitted: 12 Dec 2016
Accepted: 23 Jan 2017
First published: 23 Jan 2017

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Chem. Commun., 2017,53, 2174-2177

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The small molecule JIB-04 disrupts O₂ binding in the Fe-dependent histone demethylase KDM4A/JMJD2A

B. Cascella, S. G. Lee, S. Singh, J. M. Jez and L. M. Mirica, Chem. Commun., 2017, 53, 2174 DOI: 10.1039/C6CC09882G

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