Bromodomain biology and drug discovery.
Nilesh ZawareMing-Ming ZhouPublished in: Nature structural & molecular biology (2019)
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.
Keyphrases
- transcription factor
- drug discovery
- small molecule
- dna damage
- gene expression
- genome wide
- endothelial cells
- dna methylation
- genome wide identification
- papillary thyroid
- oxidative stress
- dna repair
- single molecule
- circulating tumor
- cell free
- cancer therapy
- induced pluripotent stem cells
- squamous cell carcinoma
- squamous cell
- lymph node metastasis
- young adults
- pluripotent stem cells