Journal article
The clinically used iron chelator deferasirox is an inhibitor of epigenetic jumonjiC domain-containing histone demethylases
- Abstract:
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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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- Files:
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(Accepted manuscript, pdf, 1003.7KB)
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- Publisher copy:
- 10.1021/acschembio.9b00289
Authors
Funding
Bibliographic Details
- 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:
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1554-8937
- ISSN:
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1554-8929
Item Description
- Language:
- English
- Keywords:
- Pubs id:
-
pubs:1030804
- UUID:
-
uuid:386a1113-c5b2-4c3c-b133-0f003e0ef528
- Local pid:
- pubs:1030804
- Source identifiers:
-
1030804
- Deposit date:
- 2019-07-10
Terms of use
- Copyright holder:
- American Chemical Society
- Copyright date:
- 2019
- Rights statement:
- © 2019 American Chemical Society.
- Notes:
- This is the accepted manuscript version of the article. The final version is available from ASC at: https://doi.org/10.1021/acschembio.9b00289
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