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Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

Abstract:

The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET (bromodomain and extra terminal domain) bromodomain family with good ligand efficiency. X-ray crystal structures of the most potent compounds reveal key interactions required for high affinity at BRD4(1). Cellular studies demonstrate that the phenol a...

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Publication status:
Published

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Publisher copy:
10.1021/jm301588r

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Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Role:
Author
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Journal:
Journal of medicinal chemistry
Volume:
56
Issue:
8
Pages:
3217-3227
Publication date:
2013-04-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:0e7f0389-b43f-425a-8884-39502b8e63dd
Source identifiers:
390906
Local pid:
pubs:390906

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