NMR Studies on the Interaction between Oncogene RET G-Quadruplex and Berberine†
NMR Studies on the Interaction between Oncogene RET G-Quadruplex and Berberine†
复制标题
Oncogene RET G-Quadruplex 与小檗碱相互作用的 NMR 研究
DOI：
10.1002/cjoc.202000301
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发表时间：
2020
影响因子：
5.4
通讯作者：
Cao C.
中科院分区：
文献类型：
--
作者：
Wang F.;Wang C.;Liu Y.;Lan W.;Wang R.;Huang S.;Cao C.
主要观察和结论摘要RET蛋白启动子区形成RETG-四链体DNA（G4-DNA），参与人类肿瘤的发生和发展。小檗碱通过与RETG 4-DNA的相互作用抑制癌细胞生长，但它如何与RETG 4-DNA结合仍然未知。以前，我们报道了秋水仙素选择性结合RETG 4-DNA，但其结合选择性的结构基础尚不清楚。在这里，主要通过NMR，我们证明了小檗碱如何以不同于秋水仙碱的方式与RETG 4-DNA结合，并暗示了小分子特异性结合一个G4-DNA的几个关键决定因素。
Summary of main observation and conclusionRETG‐quadruplex DNA (G4‐DNA) is formed in the promoter region of RET protein, which is involved in the initiation and progression of human cancers. Berberine inhibits cancer cell growth through interactions withRETG4‐DNA, but how it binds toRETG4‐DNA remains unknown. Previously, we reported that colchicine selectively bound toRETG4‐DNA, but the structural basis of its binding selectivity is still unclear. Here, mainly by NMR, we demonstrated how berberine bound toRETG4‐DNA in a means different from colchicine, and implied several key determinants for small molecules specifically binding to one G4‐DNA.