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Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B

Abstract:

Bromodomains are acetyl-lysine specific protein interaction domains that have recently emerged as a new target class for the development of inhibitors that modulate gene transcription. The two closely related bromodomain containing proteins BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. However, BAZ2 bromodomains have low predicted druggability and so far no selective inhibitors have bee...

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

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Publisher copy:
10.1021/acs.jmedchem.5b00209

Authors


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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Structural Genomics Consortium
Bamborough, P More by this author
Bantscheff, M More by this author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Subgroup:
Structural Genomics Consortium; Vice-chancellor & Registrar
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
59
Issue:
4
Pages:
1410-1424
Publication date:
2015-03-23
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pubs id:
pubs:516914
URN:
uri:af1ee820-6fe3-4a45-9b9e-b5197e29d8b3
UUID:
uuid:af1ee820-6fe3-4a45-9b9e-b5197e29d8b3
Local pid:
pubs:516914

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