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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. 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...

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

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Publisher copy:
10.1002/ange.201706788

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Department:
Oxford, MSD, NDM, Target Discovery Institute
Role:
Author
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Department:
Oxford, MPLS, Chemistry, Organic Chemistry
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Author
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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

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