- 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...
Expand abstract - Publication status:
- Published
- Peer review status:
- Peer reviewed
- Version:
- Publisher's Version
- Files:
-
-
(pdf, 1.9mb)
-
- Publisher copy:
- 10.1002/anie.201810179
-
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- Funding agency for:
- Wright, M
- Grant:
- Oxford Biomedical Research Centre
- 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
- Language:
- English
- Keywords:
- Copyright holder:
- Vazquez-Rodriguez et al.
- Copyright date:
- 2018
- Notes:
-
© 2018 The Authors. Published by Wiley-VCH Verlag GmbH and Co. KGaA.
This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
Journal article
Design, synthesis and characterization of covalent KDM5 inhibitors
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+ Engineering and Physical Sciences Research Council
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+ National Institute for Health Research
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