Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02115, USA.
Section of Computational Biomedicine, Boston University School of Medicine, Boston, MA 02118, USA.
Cancer Cell. 2013 Dec 9;24(6):777-90. doi: 10.1016/j.ccr.2013.11.003.
Diffuse large B cell lymphoma (DLBCL) is a biologically heterogeneous and clinically aggressive disease. Here, we explore the role of bromodomain and extra-terminal domain (BET) proteins in DLBCL, using integrative chemical genetics and functional epigenomics. We observe highly asymmetric loading of bromodomain 4 (BRD4) at enhancers, with approximately 33% of all BRD4 localizing to enhancers at 1.6% of occupied genes. These super-enhancers prove particularly sensitive to bromodomain inhibition, explaining the selective effect of BET inhibitors on oncogenic and lineage-specific transcriptional circuits. Functional study of genes marked by super-enhancers identifies DLBCLs dependent on OCA-B and suggests a strategy for discovering unrecognized cancer dependencies. Translational studies performed on a comprehensive panel of DLBCLs establish a therapeutic rationale for evaluating BET inhibitors in this disease.
弥漫性大 B 细胞淋巴瘤(DLBCL)是一种生物学上具有异质性和临床上侵袭性的疾病。在这里,我们通过整合化学遗传学和功能表观基因组学来探索溴结构域和末端结构域(BET)蛋白在 DLBCL 中的作用。我们观察到溴结构域 4(BRD4)在增强子上的高度不对称加载,大约 33%的 BRD4 定位在 1.6%的被占据基因的增强子上。这些超级增强子对溴结构域抑制特别敏感,这解释了 BET 抑制剂对致癌和谱系特异性转录回路的选择性作用。通过对超级增强子标记的基因进行功能研究,确定了依赖于 OCA-B 的 DLBCLs,并提出了一种发现未被识别的癌症依赖性的策略。对广泛的 DLBCL 进行的转化研究为在该疾病中评估 BET 抑制剂建立了治疗依据。
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