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药物靶向 BET 溴结构域后相互作用组的重排。

Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.

机构信息

Lunenfeld-Tanenbaum Research Institute at Mount Sinai Hospital, Toronto, ON M5G 1X5, Canada.

Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford OX3 7DQ, UK.

出版信息

Mol Cell. 2019 Feb 7;73(3):621-638.e17. doi: 10.1016/j.molcel.2018.11.006. Epub 2018 Dec 13.

Abstract

Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the interactomes of BRD2, BRD3, BRD4, and BRDT following treatment with the pan-BET BRD inhibitor JQ1, revealing broad rewiring of the interaction landscape, with three distinct classes of behavior for the 603 unique interactors identified. A group of proteins associate in a JQ1-sensitive manner with BET BRDs through canonical and new binding modes, while two classes of extra-terminal (ET)-domain binding motifs mediate acetylation-independent interactions. Last, we identify an unexpected increase in several interactions following JQ1 treatment that define negative functions for BRD3 in the regulation of rRNA synthesis and potentially RNAPII-dependent gene expression that result in decreased cell proliferation. Together, our data highlight the contributions of BET protein modules to their interactomes allowing for a better understanding of pharmacological rewiring in response to JQ1.

摘要

靶向溴结构域(BRD)的溴和额外末端(BET)家族为癌症和其他疾病的治疗干预提供了机会。在这里,我们对 BRD2、BRD3、BRD4 和 BRDT 在使用泛 BET BRD 抑制剂 JQ1 治疗后的互作组进行了分析,揭示了广泛的互作景观重排,603 个独特互作蛋白可分为 3 个不同类别。一组蛋白通过规范和新的结合模式以 JQ1 敏感的方式与 BET BRD 结合,而两个额外末端(ET)结构域结合基序类介导乙酰化非依赖性相互作用。最后,我们在 JQ1 处理后发现了几个相互作用的意外增加,这些相互作用定义了 BRD3 在 rRNA 合成和潜在的 RNAPII 依赖性基因表达调节中的负功能,导致细胞增殖减少。总之,我们的数据突出了 BET 蛋白模块对其互作组的贡献,从而更好地理解了 JQ1 作用下的药理学重排。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14a1/6375729/381a71312198/fx1.jpg

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