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A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1.

Abstract:

The 2-oxoglutarate (2OG)-dependent Jumonji C domain (JmjC) family is the largest family of histone lysine demethylases. There is interest in developing small-molecule probes that modulate JmjC activity to investigate their biological roles. 5-Carboxy-8-hydroxyquinoline (IOX1) is the most potent broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases, reported to date; however, it suffers from low cell permeability. Here, we describe structure-activity relationship studies ...

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Publication status:
Published

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Publisher copy:
10.1002/cmdc.201300428

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Journal:
ChemMedChem More from this journal
Volume:
9
Issue:
3
Pages:
566-571
Publication date:
2014-03-01
DOI:
EISSN:
1860-7187
ISSN:
1860-7179
Language:
English
Keywords:
Pubs id:
pubs:447792
UUID:
uuid:cc2a3734-4a5d-4aa5-b621-f371f424091f
Local pid:
pubs:447792
Source identifiers:
447792
Deposit date:
2014-02-13

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