Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery.
Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery.
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BET 溴结构域的抑制作为癌症药物发现的治疗策略
DOI：
10.18632/oncotarget.3551
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发表时间：
2015-03-20
期刊：
影响因子：
--
通讯作者：
Liu B
中科院分区：
文献类型：
--
作者：
Fu LL;Tian M;Li X;Li JJ;Huang J;Ouyang L;Zhang Y;Liu B
溴结构域（bromodomain，BRD）作为一种保守的蛋白质相互作用模块，识别并结合乙酰化赖氨酸，含有一个深度的、疏水性很强的乙酰赖氨酸结合位点。具有两个BRD和一个末端外结构域的蛋白质属于BET家族，包括BRD 2、BRD 3、BRD 4和BRDT。BET家族蛋白在正常条件下执行转录调节功能，而在癌症中，它们调节几种癌基因如c-Myc和Bcl-2的转录。因此，靶向BET蛋白可能是一种有前途的策略，并且对BET蛋白的强烈兴趣推动了癌症中基于结构的溴结构域抑制剂的开发。本文就近年来发现的几种小分子BET抑制剂及其抗肿瘤作用机制进行综述，为开发新型靶向BET抑制剂提供参考。
As a conserved protein interaction module that recognizes and binds to acetylated lysine, bromodomain (BRD) contains a deep, largely hydrophobic acetyl lysine binding site. Proteins that share the feature of containing two BRDs and an extra-terminal domain belong to BET family, including BRD2, BRD3, BRD4 and BRDT. BET family proteins perform transcription regulatory function under normal conditions, while in cancer, they regulate transcription of several oncogenes, such as c-Myc and Bcl-2. Thus, targeting BET proteins may be a promising strategy, and intense interest of BET proteins has fueled the development of structure-based bromodomain inhibitors in cancer. In this review, we focus on summarizing several small-molecule BET inhibitors and their relevant anti-tumor mechanisms, which would provide a clue for exploiting new targeted BET inhibitors in the future cancer therapy.
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影响因子：
56.9
作者：
Choudhary, Chunaram;Kumar, Chanchal;Mann, Matthias
通讯作者：
Mann, Matthias
DOI：
10.1158/1078-0432.ccr-12-3066
发表时间：
2013-04-01
期刊：
Clinical cancer research : an official journal of the American Association for Cancer Research
影响因子：
--
作者：
Cheng Z;Gong Y;Ma Y;Lu K;Lu X;Pierce LA;Thompson RC;Muller S;Knapp S;Wang J
通讯作者：
Wang J
影响因子：
2.7
作者：
Berkovits BD;Wolgemuth DJ
通讯作者：
Wolgemuth DJ
影响因子：
64.8
作者：
通讯作者：
--
影响因子：
4
作者：
Barbieri, Isaia;Cannizzaro, Ester;Dawson, Mark A.
通讯作者：
Dawson, Mark A.