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Design, synthesis and characterization of covalent KDM5 inhibitors

Abstract:

Histone lysine demethylases (KDMs) are involved in the dynamic regulation of gene expression and they play a critical role in several biological processes. Achieving selectivity over the different KDMs has been a major challenge for KDM inhibitor development. Here we report potent and selective KDM5 covalent inhibitors designed to target cysteine residues only present in the KDM5 sub‐family. The covalent binding to the targeted proteins was confirmed by MS and time‐dependent inhibition. Addit...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's Version

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Publisher copy:
10.1002/anie.201810179

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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM: Target Discovery Institute
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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM: Target Discovery Institute
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDORMS
Velupillai, S More by this author
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Funding agency for:
Vazquez-Rodriguez, S
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Grant:
Oxford Biomedical Research Centre
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Grant:
Seventh Framework Programme: 609305
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Publisher:
John Wiley and Sons, Ltd. Publisher's website
Journal:
Angewandte Chemie: International Edition Journal website
Volume:
58
Issue:
2
Pages:
515-519
Publication date:
2018-11-15
Acceptance date:
2018-11-12
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
Pubs id:
pubs:943531
URN:
uri:c3803e34-51e8-44ea-a415-1481a7898278
UUID:
uuid:c3803e34-51e8-44ea-a415-1481a7898278
Local pid:
pubs:943531

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