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Development of selective CBP/P300 benzoxazepine bromodomain inhibitors

Abstract:

CBP (CREB (cAMP responsive element binding protein) binding protein (CREBBP)) and P300 (adenovirus E1A-associated 300 kDa protein) are two closely related histone acetyltransferases (HATs) that play a key role in the regulation of gene transcription. Both proteins contain a bromodomain flanking the HAT catalytic domain that is important for the targeting of CBP/P300 to chromatin and which offeres an opportunity for the development of protein-protein interaction inhibitors. Here we present the...

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Publication status:
Published
Peer review status:
Peer reviewed

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Department:
Oxford, MSD, NDM, Structural Genomics Consortium
Role:
Author
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Department:
Oxford, MSD, NDM, Target Discovery Institute
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Author
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Department:
Oxford, MSD, NDM, Target Discovery Institute
Role:
Author
More by this author
Department:
Oxford, MSD, NDM, Target Discovery Institute
Role:
Author
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
59
Issue:
19
Pages:
8889–8912
Publication date:
2016-09-27
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pubs id:
pubs:648035
URN:
uri:44a065f6-7c68-4647-a989-220a9780b8b0
UUID:
uuid:44a065f6-7c68-4647-a989-220a9780b8b0
Local pid:
pubs:648035
Paper number:
19
Language:
English
Keywords:

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