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Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands.

Abstract:

Bromodomains are protein modules that bind to acetylated lysine residues and hence facilitate protein-protein interactions. These bromodomain-mediated interactions often play key roles in transcriptional regulation and their dysfunction is implicated in a large number of diseases. The discovery of potent and selective small-molecule bromodomain and extra C-terminal domain bromodomain ligands, which show promising results for the treatment of cancers and atherosclerosis, has promoted intense i...

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Publication status:
Published

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Publisher copy:
10.4155/fmc.13.197

Authors


Jennings, LE More by this author
Measures, AR More by this author
Wilson, BG More by this author
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Journal:
Future medicinal chemistry
Volume:
6
Issue:
2
Pages:
179-204
Publication date:
2014-02-05
DOI:
EISSN:
1756-8927
ISSN:
1756-8919
URN:
uuid:cd42a9db-60ec-4a8f-a0dd-650e497a26bf
Source identifiers:
447854
Local pid:
pubs:447854

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