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Discovery of BET bromodomain inhibitors and their role in target validation

Abstract:

Bromodomains (BRDs) are protein interaction modules that selectively recognize ε-N-acetylated lysine residues. BRDs are present in diverse proteins that play key functions in chromatin organization and regulation of gene transcription. Aberrant transcription is a hallmark of many diseases in particular cancer and inflammation. The complexity of molecular processes regulating gene transcription identified transcriptional regulators as interesting targets for the development of specific chemica...

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Publication status:
Published

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Publisher copy:
10.1039/c3md00291h

Authors


Mueller, S More by this author
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Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Publisher:
Royal Society of Chemistry
Journal:
MEDCHEMCOMM
Volume:
5
Issue:
3
Pages:
288-296
Publication date:
2014-03-05
DOI:
EISSN:
2040-2511
ISSN:
2040-2503
URN:
uuid:bcaaa80b-6928-44b8-85b0-9a598f8e795e
Source identifiers:
457780
Local pid:
pubs:457780
Language:
English

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