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Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

Abstract:

The posttranslational modification of chromatin through acetylation at selected histone lysine residues is governed by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The significance of this subset of the epigenetic code is interrogated and interpreted by an acetyllysine-specific protein-protein interaction with bromodomain reader modules. Selective inhibition of the bromo and extra C-terminal domain (BET) family of bromodomains with a small molecule is feasible, and this...

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Publication status:
Published

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Publisher copy:
10.1021/jm3010515

Authors


More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
Journal:
Journal of medicinal chemistry
Volume:
55
Issue:
22
Pages:
9831-9837
Publication date:
2012-11-01
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Source identifiers:
356261
Language:
English
Keywords:
Pubs id:
pubs:356261
UUID:
uuid:53a7e2eb-5d99-4173-be5b-019af9b32bd5
Local pid:
pubs:356261
Deposit date:
2013-11-16

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