- Abstract:
-
Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell-permeable inhibitors or suitable tool compounds for these enzymes. Here we describe the discovery of a new class of inhibitor that is highly selective towards the histone lysine demethylases KDM2A/7A. A modular synthetic approach was used to explore chemical space and accelerate investigation of key structure-activity relationships, leading to the de...
Expand abstract - Publication status:
- Published
- Peer review status:
- Peer reviewed
- Version:
- Publisher's version
- Files:
-
-
(pdf, 3.4MB)
-
- Publisher copy:
- 10.1002/ange.201706788
-
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- Publisher:
- Wiley Publisher's website
- Journal:
- Angewandte Chemie Journal website
- Volume:
- 129
- Issue:
- 49
- Pages:
- 15761-15765
- Publication date:
- 2017-11-07
- Acceptance date:
- 2017-10-02
- DOI:
- EISSN:
-
1521-3757
- ISSN:
-
0044-8249
- Pubs id:
-
pubs:732814
- URN:
-
uri:9ffa1eaa-d43f-45ac-8cc8-2100a981fde3
- UUID:
-
uuid:9ffa1eaa-d43f-45ac-8cc8-2100a981fde3
- Local pid:
- pubs:732814
- Paper number:
- 49
- Copyright holder:
- © 2017 Gerken, et al
- Copyright date:
- 2017
- Notes:
- 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
Discovery of a highly selective cell‐active inhibitor of the histone lysine demethylases KDM2/7
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