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Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation

Abstract:

Histone acetyltransferases of the MYST family are recruited to chromatin by BRPF scaffolding proteins. We explored functional consequences and the therapeutic potential of inhibitors targeting acetyl-lysine dependent protein interaction domains (bromodomains) present in BRPF1-3 in bone maintenance. We report three potent and selective inhibitors: one (PFI-4) with high selectivity for the BRPF1B isoform and two pan-BRPF bromodomain inhibitors (OF-1, NI-57). The developed inhibitors displaced B...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/acschembio.7b00481

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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Target Discovery Institute
Role:
Author
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Funding agency for:
Oppermann, UCT
Grant:
20522
More from this funder
Funding agency for:
Oppermann, UCT
Grant:
20522
Publisher:
American Chemical Society Publisher's website
Journal:
ACS Chemical Biology Journal website
Volume:
12
Issue:
10
Pages:
2619–2630
Publication date:
2017-08-29
Acceptance date:
2017-08-29
DOI:
EISSN:
1554-8937
ISSN:
1554-8929
Pmid:
28849908
Language:
English
Pubs id:
pubs:725804
UUID:
uuid:35cc401b-268d-43a3-b526-a233fa86196b
Local pid:
pubs:725804
Deposit date:
2017-09-21

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