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Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

Abstract:

Benzodiazepines are psychoactive drugs with anxiolytic, sedative, skeletal muscle relaxant and amnestic properties. Recently triazolo-benzodiazepines have been also described as potent and highly selective protein interaction inhibitors of bromodomain and extra-terminal (BET) proteins, a family of transcriptional co-regulators that play a key role in cancer cell survival and proliferation, but the requirements for high affinity interaction of this compound class with bromodomains has not been...

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Publisher copy:
10.1016/j.bmc.2011.10.080

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Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Fedorov, O More by this author
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Journal:
Bioorganic and Medicinal Chemistry
Volume:
20
Issue:
6
Pages:
1878-1886
Publication date:
2012-03-15
DOI:
EISSN:
1464-3391
ISSN:
0968-0896
URN:
uuid:d7625b8a-3bd0-4f30-987c-886783b54b0c
Source identifiers:
321046
Local pid:
pubs:321046

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