Journal article
Discovery of a highly selective cell-active inhibitor of the histone lysine demethylases KDM2/7
- 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. We describe the discovery of a new class of inhibitor that is highly potent towards the histone lysine demethylases KDM2A/7A.Amodular synthetic approach was used to explore the chemical space and accelerate the investigation of key structure–activity relationships, leading to the development of a small molecule with around 75- fold selectivity towards KDM2A/7A versus other KDMs, as well as cellular activity at low micromolar concentrations.
- Publication status:
- Published
- Peer review status:
- Peer reviewed
Actions
Access Document
- Files:
-
-
(Preview, Version of record, pdf, 3.4MB, Terms of use)
-
- Publisher copy:
- 10.1002/anie.201706788
Authors
- Publisher:
- Wiley
- Journal:
- Angewandte Chemie International Edition More from this journal
- Publication date:
- 2017-11-07
- Acceptance date:
- 2017-10-04
- DOI:
- EISSN:
-
1521-3773
- ISSN:
-
1433-7851
- Keywords:
- Pubs id:
-
pubs:809869
- UUID:
-
uuid:db0e3705-824b-4816-9939-b01811859716
- Local pid:
-
pubs:809869
- Source identifiers:
-
809869
- Deposit date:
-
2017-12-19
Terms of use
- Copyright holder:
- Brennan et al
- Copyright date:
- 2017
- Notes:
- © 2017 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.
- Licence:
- CC Attribution (CC BY)
If you are the owner of this record, you can report an update to it here: Report update to this record