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Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.

Abstract:

Concomitant inhibition of multiple cancer-driving kinases is an established strategy to improve the durability of clinical responses to targeted therapies. The difficulty of discovering kinase inhibitors with an appropriate multitarget profile has, however, necessitated the application of combination therapies, which can pose major clinical development challenges. Epigenetic reader domains of the bromodomain family have recently emerged as new targets for cancer therapy. Here we report that s...

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

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Publisher copy:
10.1038/nchembio.1471

Authors


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Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Role:
Author
More by this author
Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Role:
Author
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Publisher:
Nature Research Publisher's website
Journal:
Nature Chemical Biology Journal website
Volume:
10
Issue:
4
Pages:
305-312
Publication date:
2014-03-02
DOI:
EISSN:
1552-4469
ISSN:
1552-4450
URN:
uuid:1b14729e-56d8-4cf4-876a-9b465341762c
Source identifiers:
450967
Local pid:
pubs:450967

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