BET bromodomain inhibitors: a patent review
Publication Year 2014-02, Volume 24, Issue #2, Page 185-99
Journal Title
Expert opinion on therapeutic patents
Publication Type
Journal Article
INTRODUCTION: The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT). These "epigenetic readers" bind to acetyllysine (KAc) residues on the tails of histones H3 and H4, and regulate chromatin structure and gene expression. There is increasing evidence of their role in human disease, and recently a number of small-molecule inhibitors have been reported. There is increasing interest in the inhibition of BET proteins for a variety of therapeutic applications that have resulted in considerable patent activity from academia and biotechnology and pharmaceutical companies. AREAS COVERED: Data supporting the use of BET inhibitors in treating disease are outlined, and the current patent literature is discussed. The survey is focused on patents claiming compounds as BET inhibitors and additional patents covering compounds now reported as BET inhibitors have been included. EXPERT OPINION: There is now compelling preclinical data demonstrating BET inhibition as a strategy to target processes known to be involved in disease development and progression with clinical trials of two bona fide BET inhibitors now underway. Patent activity in this area is increasing with initial activity focused on variations to reported BET inhibitors and more recent patents disclosing novel chemotypes as BET inhibitors.
BET, BRD2, BRD3, BRD4, BRDT, bromodomain
WEHI Research Division(s)
Chemical Biology
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Creation Date: 2014-04-16 08:43:41
Last Modified: 0001-01-01 12:00:00
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