Place your BETs: the therapeutic potential of bromodomains

Trends Pharmacol Sci. 2012 Mar;33(3):146-53. doi: 10.1016/ Epub 2012 Jan 23.


Therapeutic targeting of the processes that regulate histone modification is a growing area of scientific exploration. Although most interest has concentrated on the various families of enzymes that contribute to these processes, this review focuses on emerging data demonstrating the chemical tractability and therapeutic potential of a hitherto underexplored family of proteins, namely the bromodomain (BRD) family of reader proteins. These proteins perform a crucial role in translating histone modifications with powerful transcriptional consequences. We review current knowledge of the biology of this emergent target class and highlight recent breakthroughs that now make the BRD family of reader proteins attractive for drug discovery.

Publication types

  • Review

MeSH terms

  • Acetylation
  • Animals
  • Drug Discovery / methods
  • Gene Expression
  • Histones / genetics
  • Histones / metabolism*
  • Humans
  • Nuclear Proteins / genetics
  • Nuclear Proteins / metabolism*


  • Histones
  • Nuclear Proteins