2011年9月16日 · Using a selective small-molecule bromodomain inhibitor, JQ1, we identify BET bromodomain proteins as regulatory factors for c-Myc. BET inhibition by JQ1 downregulates MYC transcription, followed by genome-wide downregulation of Myc-dependent target genes.

bet抑制能够下调myc转录和后续的全基因组myc依赖性的靶基因。 鉴于MYC在癌症中的广泛致病作用，通过BET溴结构域对MYC的药理抑制作用为癌症治疗提供了广阔前景。

Here, we demonstrate the rapid and potent abrogation of MYC gene transcription by representative small molecule inhibitors of the BET family of chromatin adaptors. MYC transcriptional suppression was observed in the context of the natural, chromosomally translocated, and amplified gene locus.

c-myc蛋白是一种核内DNA结合蛋白, 可调节碱性螺旋-环-螺旋转录因子(basic helix-loop-helix, bHLH)的转录，从而调控细胞生长、分化与凋亡，与肿瘤的发生与转归密切相关。因此，c-myc基因一个重要的肿瘤相关基因。

2021年3月15日 · BET-family members influence cell cycle progression by activating oncogenes such as MYC, JUNB, CCND1 and CCNA1. 15, 16, 17 Consistent with a role in regulating the expression of cell cycle...

2023年11月6日 · BET proteins, which influence gene expression and contribute to the development of cancer, are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic anticancer...

BET inhibitors have been demonstrated to repress c-Myc expression, and were initially shown to have efficacy in a number of c-Myc-dependent hematologic malignancies. Recent studies have now revealed a broader role for BET inhibitors in hematologic malignancies.

2025年2月23日 · 二、间接抑制MYC的策略. BET溴结构域抑制剂（JQ1、OTX015等）：抑制BET蛋白与MYC启动子结合，减少其转录。 CDK9抑制剂（KB-0742）：阻断RNA聚合酶Ⅱ延长复合物，抑制MYC转录。 eIF4F翻译复合体抑制剂（如silvestrol）：干扰MYC mRNA的翻译。

2011年10月4日 · Treatment with a BET inhibitor resulted in significant antitumor activity in xenograft models of Burkitt's lymphoma and acute myeloid leukemia. These findings demonstrate that pharmacologic inhibition of MYC is achievable through targeting BET bromodomains.

Using a selective small-molecule bromodomain inhibitor, JQ1, we identify BET bromodomain proteins as regulatory factors for c-Myc. BET inhibition by JQ1 downregulates MYC transcription, followed by genome-wide downregulation of Myc-dependent target genes.