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RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

Abstract:

Bromodomains have emerged as attractive candidates for the development of inhibitors targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently showed promising activity in diverse disease models. However, the pleiotropic nature of BET proteins regulating tissue-specific transcription has raised safety concerns and suggested that attempts should be made for domain-specific targeting. Here, we report that RVX-208, a compound currently in phase II clinical tri...

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Authors


Felletar, I More by this author
Brotherton, D More by this author
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Journal:
Proceedings of the National Academy of Sciences of the United States of America
Volume:
110
Issue:
49
Pages:
19754-19759
Publication date:
2013-12-03
DOI:
EISSN:
1091-6490
ISSN:
0027-8424
URN:
uuid:574ba64f-ddf8-4e83-910d-6664b5b586da
Source identifiers:
444291
Local pid:
pubs:444291

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