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Structure-based design of highly selective inhibitors of the CREB binding protein bromodomain

Abstract:

Chemical probes are required for preclinical target validation to interrogate novel biological targets and pathways. Selective inhibitors of the CREB binding protein (CREBBP)/EP300 bromodomains are required to facilitate the elucidation of biology associated with these important epigenetic targets. Medicinal chemistry optimization that paid particular attention to physiochemical properties delivered chemical probes with desirable potency, selectivity, and permeability attributes. An important...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted Manuscript

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Publisher copy:
10.1021/acs.jmedchem.6b01839

Authors


Langille, J More by this author
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
60
Issue:
13
Pages:
5349–5363
Publication date:
2017-04-04
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pubs id:
pubs:697052
URN:
uri:409201b6-b901-4c7f-8a90-fc7475ffc7c1
UUID:
uuid:409201b6-b901-4c7f-8a90-fc7475ffc7c1
Local pid:
pubs:697052
Language:
English

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