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A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.

Abstract:
The benzoxazinone and dihydroquinoxalinone fragments were employed as novel acetyl lysine mimics in the development of CREBBP bromodomain ligands. While the benzoxazinone series showed low affinity for the CREBBP bromodomain, expansion of the dihy...Expand abstract...
Publication status:
Published

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Publisher copy:
10.1002/anie.201402750

Authors


Rooney, TP More by this author
More by this author
Institution:
University of Oxford
Department:
Oxford, MSD, NDM, Structural Genomics Consortium
More by this author
Institution:
University of Oxford
Department:
Oxford, MSD, NDM, Target Discovery Institute
Cortopassi, WA More by this author
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Journal:
Angewandte Chemie (International ed. in English) More in this journal
Volume:
53
Issue:
24
Pages:
6126-6130
Publication date:
2014-06-19
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
URN:
uuid:6fa6267a-c739-4acc-be90-a1b602e746e9
Source identifiers:
464925
Local pid:
pubs:464925

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