title: BET bromodomain inhibitors: a patent review.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: The Walter and Eliza Hall Institute of Medical Research , 1G Royal Pde, Parkville, VIC, 3052 , Australia +61 3 9345 2957 ; +61 3 9347 0852 ; burns@wehi.edu.au.
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Garnier
authors.forename: Phillip P
authors.initials: PP
authors.lastname: Sharp
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Burns
mesh_terms: D000818:Animals; D015195:Drug Design; D004335:Drug and Narcotic Control; D044127:Epigenesis, Genetic / Q000187:drug effects; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D010330:Patents as Topic; D017434:Protein Structure, Tertiary; D016601:RNA-Binding Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism
chemical_list: D009687:Nuclear Proteins; D016601:RNA-Binding Proteins; D014157:Transcription Factors