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Design of a biased potent small molecule inhibitor of the bromodomain and PHD finger-containing (BRPF) proteins suitable for cellular and in vivo studies.

Abstract:

The BRPF (bromodomain and PHD finger-containing) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family to chromatin. Evaluation of the BRPF family as a potential drug target is at an early stage although there is an emerging understanding of a role in acute myeloid leukemia (AML). We report the optimization of fragment hit 5b to 13-d as a biased, potent inhibitor of the BRD of the BRP...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted manuscript

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Publisher copy:
10.1021/acs.jmedchem.6b01583

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Department:
Oxford, MSD, NDM, Target Discovery Institute
More by this author
Department:
Oxford, MSD, NDM, Target Discovery Institute
Savitsky, P More by this author
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University College London More from this funder
Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
60
Issue:
2
Pages:
668–680
Publication date:
2017-01-05
Acceptance date:
2017-01-09
DOI:
ISSN:
1520-4804
Pubs id:
pubs:670809
URN:
uri:583ad7a8-d67e-4ccc-8416-ba3de717b200
UUID:
uuid:583ad7a8-d67e-4ccc-8416-ba3de717b200
Local pid:
pubs:670809

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