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Nat Rev Mol Cell Biol. 2017 Apr;18(4):246-262. doi: 10.1038/nrm.2016.143. Epub 2017 Jan 5.

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer.

Author information

1
Ludwig Institute for Cancer Research, Old Road Campus Research Building, Roosevelt Drive, Oxford.
2
Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.

Abstract

Bromodomains (BRDs) are evolutionarily conserved protein-protein interaction modules that are found in a wide range of proteins with diverse catalytic and scaffolding functions and are present in most tissues. BRDs selectively recognize and bind to acetylated Lys residues - particularly in histones - and thereby have important roles in the regulation of gene expression. BRD-containing proteins are frequently dysregulated in cancer, they participate in gene fusions that generate diverse, frequently oncogenic proteins, and many cancer-causing mutations have been mapped to the BRDs themselves. Importantly, BRDs can be targeted by small-molecule inhibitors, which has stimulated many translational research projects that seek to attenuate the aberrant functions of BRD-containing proteins in disease.

PMID:
28053347
DOI:
10.1038/nrm.2016.143
[Indexed for MEDLINE]

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