BET bromodomain inhibition as a therapeutic strategy to target c-Myc ...
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 …
靶向BET蛋白的药物发现——研究进展及新技术 - 知乎
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。
Targeting MYC dependence in cancer by inhibiting BET …
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 …
溴结构域蛋白4的结构和功能及其抑制剂在肿瘤研究中的应用
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 …
Achieving clinical success with BET inhibitors as anti-cancer agents
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 …
Bromodomain and extraterminal (BET) proteins: biological …
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 …
BET inhibitors in the treatment of hematologic malignancies: …
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 …
征服“难以成药”的MYC：生物制药行业的攻坚之旅-MedSci.cn
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 …
Targeting MYC dependence in cancer by inhibiting BET bromodomains
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 …
BET 溴结构域抑制作为靶向 c-Myc 的治疗策略。,Cell - X-MOL
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 …