BRD4
溴尿嘧啶
增强子
RNA聚合酶Ⅱ
染色质
转录因子
生物
癌症研究
发起人
辅活化剂
抄写(语言学)
基因
细胞生物学
基因表达
遗传学
组蛋白
哲学
语言学
作者
Francesca Zanconato,Giusy Battilana,Mattia Forcato,Letizia Filippi,Luca Azzolin,Andrea Manfrin,Erika Quaranta,Daniele Di Biagio,Gianluca Sigismondo,Vincenza Guzzardo,Pascale Lejeune,Bernard Haendler,Jeroen Krijgsveld,Matteo Fassan,Silvio Bicciato,Michelangelo Cordenonsi,Stefano Piccolo
出处
期刊:Nature Medicine
[Nature Portfolio]
日期:2018-09-06
卷期号:24 (10): 1599-1610
被引量:277
标识
DOI:10.1038/s41591-018-0158-8
摘要
Cancer cells rely on dysregulated gene expression. This establishes specific transcriptional addictions that may be therapeutically exploited. Yet, the mechanisms that are ultimately responsible for these addictions are poorly understood. Here, we investigated the transcriptional dependencies of transformed cells to the transcription factors YAP and TAZ. YAP/TAZ physically engage the general coactivator bromodomain-containing protein 4 (BRD4), dictating the genome-wide association of BRD4 to chromatin. YAP/TAZ flag a large set of enhancers with super-enhancer-like functional properties. YAP/TAZ-bound enhancers mediate the recruitment of BRD4 and RNA polymerase II at YAP/TAZ-regulated promoters, boosting the expression of a host of growth-regulating genes. Treatment with small-molecule inhibitors of BRD4 blunts YAP/TAZ pro-tumorigenic activity in several cell or tissue contexts, causes the regression of pre-established, YAP/TAZ-addicted neoplastic lesions and reverts drug resistance. This work sheds light on essential mediators, mechanisms and genome-wide regulatory elements that are responsible for transcriptional addiction in cancer and lays the groundwork for a rational use of BET inhibitors according to YAP/TAZ biology.
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