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The clinically used iron chelator deferasirox is an inhibitor of epigenetic jumonjiC domain-containing histone demethylases

Abstract:

Fe(II)- and 2-oxoglutarate (2OG)-dependent JumonjiC domain-containing histone demethylases (JmjC KDMs) are epigenetic eraser enzymes involved in the regulation of gene expression and are emerging drug targets in oncology. We screened a set of clinically used iron chelators and report that they potently inhibit JMJD2A (KDM4A) in vitro. Mode of action investigations revealed that one compound, deferasirox, is a bona fide active site-binding inhibitor as shown by kinetic and spectroscopic studie...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acschembio.9b00289

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Institution:
University of Oxford
Department:
Chemistry
Role:
Author
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Institution:
University of Oxford
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Department:
Chemistry
Role:
Author
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Publisher:
ACS Publications Publisher's website
Journal:
ACS Chemical Biology Journal website
Volume:
14
Issue:
8
Pages:
1737-1750
Publication date:
2019-07-09
Acceptance date:
2019-07-09
DOI:
EISSN:
1554-8937
ISSN:
1554-8929
Source identifiers:
1030804
Language:
English
Keywords:
Pubs id:
pubs:1030804
UUID:
uuid:386a1113-c5b2-4c3c-b133-0f003e0ef528
Local pid:
pubs:1030804
Deposit date:
2019-07-10

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