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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

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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
Role:
Author
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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM: Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDORMS
Role:
Author
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Funding agency for:
Vazquez-Rodriguez, S
Grant:
Marie Sklodowska-Curie: 744389
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Funding agency for:
Wright, M
Grant:
EP/L015838/1
National Institute for Health Research More from this funder
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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
Pmid:
30431220
Source identifiers:
943531
Language:
English
Keywords:
Pubs id:
pubs:943531
UUID:
uuid:c3803e34-51e8-44ea-a415-1481a7898278
Local pid:
pubs:943531
Deposit date:
2018-11-16

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