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Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases

Abstract:

Plant homeodomain (PHD) containing proteins are important epigenetic regulators and are of interest as potential drug targets. Inspired by the amiodarone derivatives reported to inhibit the PHD3-finger of KDM5A (KDM5A(PHD3)), a set of compounds were synthesised. Amiodarone and its derivatives were observed to weakly disrupt the interactions of a histone H3K4me3 peptide with KDM5A(PHD3). Selected amiodarone derivatives inhibited catalysis of KDM5A, but in a PHD-finger independent manner. Amiod...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bmc.2018.03.030

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Institution:
University of Oxford
Division:
MSD
Department:
RDM
Sub department:
RDM Cardiovascular Medicine
Role:
Author
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Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry; Organic Chemistry
Role:
Author
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Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry; Organic Chemistry
Role:
Author
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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDORMS
Role:
Author
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Grant:
Programme Grant [C8717/A18245, AK, CJS
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Publisher:
Elsevier Publisher's website
Journal:
Bioorganic and Medicinal Chemistry Journal website
Volume:
26
Issue:
11
Pages:
2984-2991
Publication date:
2018-03-19
Acceptance date:
2018-03-18
DOI:
ISSN:
0968-0896
Keywords:
Pubs id:
pubs:830265
UUID:
uuid:452b211f-cae0-4f1a-b730-ef2f123fbe83
Local pid:
pubs:830265
Deposit date:
2018-03-19

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