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Promiscuous targeting of bromodomains by Bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia

Abstract:

Bromodomains (BRDs) have emerged as compelling targets for cancer therapy. The development of selective and potent BET inhibitors and their significant activity in diverse tumor models has rapidly translated into clinical studies and has motivated drug development efforts targeting non-BET BRDs. However, the complex multidomain/subunit architecture of bromodomain protein complexes complicates predictions of consequences of their pharmacological targeting. To address this issue we developed a ...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher version

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Publisher copy:
10.1126/sciadv.1600760

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Department:
Oxford, MSD, NDM, Structural Genomics Consortium
Role:
Author
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Funding agency for:
Picaud, S
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Funding agency for:
Wang, CY
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Funding agency for:
Filippakopoulos, P
Publisher:
American Association for the Advancement of Science Publisher's website
Journal:
Science Advances Journal website
Volume:
2
Issue:
10
Pages:
Article: e1600760
Publication date:
2016-10-12
Acceptance date:
2016-08-22
DOI:
ISSN:
2375-2548
Pubs id:
pubs:644396
URN:
uri:ecfd7ba0-1dfa-4135-b073-c73a61413ee6
UUID:
uuid:ecfd7ba0-1dfa-4135-b073-c73a61413ee6
Local pid:
pubs:644396
Paper number:
10

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