2011年8月3日 · By screening a custom library of small hairpin RNAs (shRNAs) targeting known chromatin regulators in a genetically defined AML mouse model, we identify the protein bromodomain-containing 4 (Brd4)...

2021年1月11日 · Here, we report enhanced toxicity of combined MDM2i and BETi towards AML cell lines, primary human blasts and mouse models, resulting from BETi’s ability to evict an unexpected repressive form of...

Targeting BRD4/Brd4 using the inhibitor JQ1 has an effect on MLL-partial tandem duplication (MLL-PTD)/Mll-PTD acute myeloid leukemia cells. (A) WST-1 assay on EOL-1 and K562 cells treated with the indicated concentrations of JQ1 for 48 hours (h). (B) EOL-1 cells were treated for 24 h with the indicated concentration of JQ1.

2016年6月13日 · Using quantitative proteomics, chemoproteomics and biochemical fractionation, we found that native BRD4 and DOT1L exist in separate protein complexes. Genetic disruption or small-molecule...

2016年6月16日 · Using quantitative proteomics, chemoproteomics and biochemical fractionation, we found that native BRD4 and DOT1L exist in separate protein complexes. Genetic disruption or small-molecule inhibition of BRD4 and DOT1L showed marked synergistic activity against MLL leukemia cell lines, primary human leukemia cells and mouse leukemia models.

The bromodomain and extra terminal (BET) family protein bromodomain containing protein 4 (BRD4) is an epigenetic regulator recently identified as a therapeutic target for several hematological cancers, notably mixed lineage leukemia-fusion acute myeloid leukemia (MLL-AML). Here, we show that the BRD4 bromodomain inhibitor JQ1 is highly active ...

We show that MLL-AF9 cells critically depend on FLT3-ligand induced pathways as well as on BRD3/4 for their survival. We evaluated the in vitro and in vivo efficacy of the BRD3/4 inhibitor I-BET151 in various human MLL-AF9 (primary) models and patient samples and analyzed the transcriptome changes following treatment.

2021年9月1日 · Targeting BRD4 in acute myeloid leukemia with partial tandem duplication of the MLL gene Haematologica . 2021 Sep 1;106(9):2527-2532. doi: 10.3324/haematol.2020.271627.

Targeting BRD4/Brd4 using the inhibitor JQ1 has an effect on MLL-partial tandem duplication (MLL-PTD)/Mll-PTD acute myeloid leukemia cells. (A) WST-1 assay on EOL-1 and K562 cells treated with the indicated concentrations of JQ1 for 48 hours (h). (B) EOL-1 cells were treated for 24 h with the indicated concentration of JQ1.

探讨4型含Bromo结构域蛋白（BRD4）拮抗剂对普通型急性B淋巴细胞白血病（B-ALL）患者原代白血病细胞的作用及可能机制。 采用流式细胞术分选14例普通型B-ALL患者（Ph + B-ALL 4例，Ph − B-ALL 10例）白血病细胞，在模拟骨髓微环境条件下进行短期培养；给予BRD4拮抗剂GSK525762A处理后，采用CCK-8法检测细胞增殖抑制率，用AnnexinⅤ/7-AAD法检测细胞凋亡率，荧光定量PCR法检测c-MYC、CDK6、Bcl-2 mRNA表达水平，Western blot法检测c-MYC …