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

被引：437

作者：

Fujisawa, Takao ^{[1
,2
]}

Filippakopoulos, Panagis ^{[1
,2
]}

机构：

[1] Ludwig Inst Canc Res, Old Rd Campus Res Bldg,Roosevelt Dr, Oxford OX3 7DQ, England

[2] Struct Genom Consortium, Old Rd Campus Res Bldg,Roosevelt Dr, Oxford OX3 7DQ, England

来源：

NATURE REVIEWS MOLECULAR CELL BIOLOGY | 2017年 / 18卷 / 04期

基金：

英国惠康基金; 巴西圣保罗研究基金会; 加拿大创新基金会;

关键词：

CHROMATIN-REMODELING COMPLEX; ACETYL-LYSINE RECOGNITION; PHD FINGER-BROMODOMAIN; NF-KAPPA-B; SOMATIC MUTATIONS; STRUCTURAL BASIS; DNA-DAMAGE; TRANSCRIPTIONAL ELONGATION; EMBRYONIC-DEVELOPMENT; HISTONE DEACETYLASES;

D O I：

10.1038/nrm.2016.143

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

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.

引用

页码：246 / 262

页数：17

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