TY - JOUR
T1 - Bromodomain biology and drug discovery
AU - Zaware, Nilesh
AU - Zhou, Ming Ming
N1 - Funding Information:
We thank members of the Zhou group for helpful discussion and C. Kim for preparing Supplementary Tables 1 and 2. This work was supported in part by the research grants from the National Institutes of Health (to M.-M.Z. and N.Z.).
Publisher Copyright:
© 2019, Springer Nature America, Inc.
PY - 2019/10/1
Y1 - 2019/10/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85072926380&partnerID=8YFLogxK
U2 - 10.1038/s41594-019-0309-8
DO - 10.1038/s41594-019-0309-8
M3 - Review article
C2 - 31582847
AN - SCOPUS:85072926380
SN - 1545-9993
VL - 26
SP - 870
EP - 879
JO - Nature Structural and Molecular Biology
JF - Nature Structural and Molecular Biology
IS - 10
ER -