Selective recognition of c-myc promoter G-quadruplex and down-regulation of oncogene c-myc transcription in human cancer cells by 3,8a-disubstituted indolizinone
Selective recognition of c-myc promoter G-quadruplex and down-regulation of oncogene c-myc transcription in human cancer cells by 3,8a-disubstituted indolizinone
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3,8a-二取代吲哚嗪酮选择性识别 c-myc 启动子 G-四链体并下调人癌细胞中癌基因 c-myc 转录
DOI：
10.1039/c7ra09870g
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发表时间：
2017
期刊：
影响因子：
3.9
通讯作者：
Tang Yalin
中科院分区：
文献类型：
--
作者：
Yang Fengmin;Sun Xin;Wang Lixia;Li Qian;Guan Aijiao;Shen Gang;Tang Yalin
C-myc promoter G-quadruplex is a very important target for developing anti-cancer drugs. However, highly selective recognition of DNA c-myc G-quadruplex with parallel configuration is also a very challenging problem. Here, we showed a new type of N-containing alkaloid, 3,8a-disubstituted indolizinone, which adopted a distorted configuration. 6-Methyl-3-(naphthalen-2-yl)-8a-(4-methylpyridin-2-yl)-indolizinone could selectively recognize DNA c-myc G-quadruplex leading to an obvious fluorescence enhancement by 11-fold, and meanwhile the G-quadruplex can be stabilized up to 90 °C. Further, it could down-regulate the transcription of oncogene c-myc in both human non-small cell line (A549) and human laryngeal epithelial cell line (Hep-2).
