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


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.

SUBMITTER: Cascella B 

PROVIDER: S-EPMC5511625 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature

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The small molecule JIB-04 disrupts O<sub>2</sub> binding in the Fe-dependent histone demethylase KDM4A/JMJD2A.

Cascella Barbara B   Lee Soon Goo SG   Singh Sukrit S   Jez Joseph M JM   Mirica Liviu M LM  

Chemical communications (Cambridge, England) 20170201 13


JIB-04, a specific inhibitor of the O<sub>2</sub>-activating, Fe-dependent histone lysine demethylases, is revealed to disrupt the binding of O<sub>2</sub> in KDM4A/JMJD2A through a continuous O<sub>2</sub>-consumption assay, X-ray crystal structure data, and molecular docking. ...[more]

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