BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor

BRD4 分析可识别关键的慢性淋巴细胞白血病致癌回路并揭示对 PLX51107(一种新型结构独特的 BET 抑制剂)的敏感性

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作者:Hatice Gulcin Ozer #, Dalia El-Gamal #, Ben Powell #, Zachary A Hing, James S Blachly, Bonnie Harrington, Shaneice Mitchell, Nicole R Grieselhuber, Katie Williams, Tzung-Huei Lai, Lapo Alinari, Robert A Baiocchi, Lindsey Brinton, Elizabeth Baskin, Matthew Cannon, Larry Beaver, Virginia M Goettl, Dav

Significance

To date, functional studies of BRD4 in CLL are lacking. Through integrated genomic, functional, and pharmacologic analyses, we uncover the existence of BRD4-regulated core CLL transcriptional programs and present preclinical proof-of-concept studies validating BET inhibition as an epigenetic approach to target BCR signaling in CLL. Cancer Discov; 8(4); 458-77. ©2018 AACR.This article is highlighted in the In This Issue feature, p. 371.

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