Journal article
Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases
- Abstract:
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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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(Version of record, pdf, 2.1MB)
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- Publisher copy:
- 10.1016/j.bmc.2018.03.030
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Authors
Funding
Bibliographic Details
- 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
Item Description
- Keywords:
- Pubs id:
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pubs:830265
- UUID:
-
uuid:452b211f-cae0-4f1a-b730-ef2f123fbe83
- Local pid:
- pubs:830265
- Deposit date:
- 2018-03-19
Terms of use
- Copyright holder:
- Bhushan et al
- Copyright date:
- 2018
- Notes:
- Copyright © 2018 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
- Licence:
- CC Attribution (CC BY)
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