一种芘衍生物对人 c-myc 癌基因启动子中 G-四链体和双链 DNA 平衡的调控。
Regulation of the equilibrium between G-quadruplex and duplex DNA in promoter of human c-myc oncogene by a pyrene derivative.
机构信息
Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
出版信息
Int J Biol Macromol. 2011 Dec 1;49(5):1173-6. doi: 10.1016/j.ijbiomac.2011.05.024. Epub 2011 Jun 12.
It has been established that the equilibrium between duplex and G-quadruplex of the nuclease hypersensitivity element III1 (NHE III1) in human c-myc promoter is linked with this gene's transcription. Using NMR and ESI-MS, we have found a pyrene derivative, DMAPP, is able to modulate this equilibrium and, thus, might have the potential to regulate this oncogene's transcription. DMAPP has shown as a G-quadruplex binding agent and could induce c-myc G-quadruplex formation out of duplex. These results provide new clue for rational drug design to target transcription control of c-myc.
已经证实，人类 c-myc 启动子中核酸酶敏感性元件 III1（NHE III1）的双链体和 G-四链体之间的平衡与该基因的转录有关。我们使用 NMR 和 ESI-MS 发现，一种名为 DMAPP 的芘衍生物能够调节这种平衡，因此可能具有调节这种致癌基因转录的潜力。DMAPP 已被证明是一种 G-四链体结合剂，能够诱导 c-myc G-四链体从双链体中形成。这些结果为靶向 c-myc 转录控制的合理药物设计提供了新的线索。
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