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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.

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


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.

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