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An activity-based probe targeting non-catalytic, highly conserved amino acid residues within bromodomains

Abstract:

Bromodomain‐containing proteins are epigenetic modulators involved in a wide range of cellular processes, from recruitment of transcription factors to pathological disruption of gene regulation and cancer development. Since the druggability of these acetyl‐lysine reader domains was established, efforts were made to develop potent and selective inhibitors across the entire family. Here we report the development of a small molecule‐based approach to covalently modify recombinant and endogenous ...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/anie.201807825

Authors


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Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
ORCID:
0000-0003-2449-6461
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
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John Fell Fund More from this funder
Medical Research Council More from this funder
Publisher:
Wiley Publisher's website
Journal:
Angewandte Chemie International Edition Journal website
Volume:
58
Issue:
4
Pages:
1007-1012
Publication date:
2018-12-27
Acceptance date:
2018-12-27
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
Language:
English
Keywords:
Pubs id:
pubs:954996
UUID:
uuid:39db9ad9-8705-4423-8ca6-f035504f2873
Local pid:
pubs:954996
Deposit date:
2018-12-31

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