Bromodomain biology and drug discovery

Nat Struct Mol Biol. 2019 Oct;26(10):870-879. doi: 10.1038/s41594-019-0309-8. Epub 2019 Oct 3.


The bromodomain (BrD) is a conserved structural module found in chromatin- and transcription-associated proteins that acts as the primary reader for acetylated lysine residues. This basic activity endows BrD proteins with versatile functions in the regulation of protein-protein interactions mediating chromatin-templated gene transcription, DNA recombination, replication and repair. Consequently, BrD proteins are involved in the pathogenesis of numerous human diseases. In this Review, we highlight our current understanding of BrD biology, and discuss the latest development of small-molecule inhibitors targeting BrDs as emerging epigenetic therapies for cancer and inflammatory disorders.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Acetylation / drug effects
  • Animals
  • Drug Discovery / methods*
  • Epigenesis, Genetic / drug effects*
  • Histone Code / drug effects
  • Histones / chemistry
  • Histones / genetics
  • Humans
  • Inflammation / drug therapy
  • Inflammation / genetics
  • Models, Molecular
  • Neoplasms / drug therapy
  • Neoplasms / genetics
  • Protein Domains / drug effects*
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / pharmacology*
  • Transcription Factors / chemistry
  • Transcription Factors / genetics


  • Histones
  • Small Molecule Libraries
  • Transcription Factors