TY - JOUR
T1 - BET inhibition disrupts transcription but retains enhancer-promoter contact
AU - Crump, Nicholas T
AU - Ballabio, Erica
AU - Godfrey, Laura
AU - Thorne, Ross
AU - Repapi, Emmanouela
AU - Kerry, Jon
AU - Tapia, Marta
AU - Hua, Peng
AU - Lagerholm, Christoffer
AU - Filippakopoulos, Panagis
AU - Davies, James O J
AU - Milne, Thomas A
PY - 2021/1/11
Y1 - 2021/1/11
N2 - Enhancers are DNA sequences that enable complex temporal and tissue-specific regulation of genes in higher eukaryotes. Although it is not entirely clear how enhancer-promoter interactions can increase gene expression, this proximity has been observed in multiple systems at multiple loci and is thought to be essential for the maintenance of gene expression. Bromodomain and Extra-Terminal domain (BET) and Mediator proteins have been shown capable of forming phase condensates and are thought to be essential for super-enhancer function. Here, we show that targeting of cells with inhibitors of BET proteins or pharmacological degradation of BET protein Bromodomain-containing protein 4 (BRD4) has a strong impact on transcription but very little impact on enhancer-promoter interactions. Dissolving phase condensates reduces BRD4 and Mediator binding at enhancers and can also strongly affect gene transcription, without disrupting enhancer-promoter interactions. These results suggest that activation of transcription and maintenance of enhancer-promoter interactions are separable events. Our findings further indicate that enhancer-promoter interactions are not dependent on high levels of BRD4 and Mediator, and are likely maintained by a complex set of factors including additional activator complexes and, at some sites, CTCF and cohesin.
AB - Enhancers are DNA sequences that enable complex temporal and tissue-specific regulation of genes in higher eukaryotes. Although it is not entirely clear how enhancer-promoter interactions can increase gene expression, this proximity has been observed in multiple systems at multiple loci and is thought to be essential for the maintenance of gene expression. Bromodomain and Extra-Terminal domain (BET) and Mediator proteins have been shown capable of forming phase condensates and are thought to be essential for super-enhancer function. Here, we show that targeting of cells with inhibitors of BET proteins or pharmacological degradation of BET protein Bromodomain-containing protein 4 (BRD4) has a strong impact on transcription but very little impact on enhancer-promoter interactions. Dissolving phase condensates reduces BRD4 and Mediator binding at enhancers and can also strongly affect gene transcription, without disrupting enhancer-promoter interactions. These results suggest that activation of transcription and maintenance of enhancer-promoter interactions are separable events. Our findings further indicate that enhancer-promoter interactions are not dependent on high levels of BRD4 and Mediator, and are likely maintained by a complex set of factors including additional activator complexes and, at some sites, CTCF and cohesin.
KW - CCCTC-Binding Factor/metabolism
KW - Carcinogenesis/drug effects
KW - Cell Cycle Proteins/metabolism
KW - Cell Line, Tumor
KW - Chromatin/metabolism
KW - Chromosomal Proteins, Non-Histone/metabolism
KW - DNA-Binding Proteins/metabolism
KW - Enhancer Elements, Genetic
KW - Glycols/pharmacology
KW - Histones/metabolism
KW - Humans
KW - Leukemia/genetics
KW - Models, Genetic
KW - Promoter Regions, Genetic
KW - Protein Binding/drug effects
KW - Proto-Oncogene Proteins c-myc/genetics
KW - Transcription, Genetic/drug effects
UR - http://www.scopus.com/inward/record.url?scp=85099211231&partnerID=8YFLogxK
U2 - 10.1038/s41467-020-20400-z
DO - 10.1038/s41467-020-20400-z
M3 - Journal article
C2 - 33431820
SN - 2041-1722
VL - 12
SP - 223
JO - Nature Communications
JF - Nature Communications
IS - 1
M1 - 223
ER -