title: Functions of bromodomain-containing proteins and their roles in homeostasis and cancer.
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.
authors.affiliation: Ludwig Institute for Cancer Research, Old Road Campus Research Building, Roosevelt Drive, Oxford.
authors.forename: Takao
authors.initials: T
authors.lastname: Fujisawa
authors.affiliation: 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.
authors.forename: Panagis
authors.initials: P
authors.lastname: Filippakopoulos
mesh_terms: D000215:Acylation; D000818:Animals; D042002:Chromatin Assembly and Disassembly; D005786:Gene Expression Regulation; D006657:Histones / Q000378:metabolism; D006706:Homeostasis; D006801:Humans; D008239:Lysine / Q000378:metabolism; D009154:Mutation; D009369:Neoplasms / Q000235:genetics / Q000378:metabolism*; D015514:Oncogene Proteins, Fusion / Q000737:chemistry / Q000378:metabolism; D000072417:Protein Domains; D011499:Protein Processing, Post-Translational; D011506:Proteins / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism*; D025521:Tumor Suppressor Proteins / Q000235:genetics / Q000378:metabolism
chemical_list: D006657:Histones; D015514:Oncogene Proteins, Fusion; D011506:Proteins; D025521:Tumor Suppressor Proteins; D008239:Lysine