NMR 揭示秋水仙碱与致癌基因 RET G-四链体的选择性相互作用。
Colchicine selective interaction with oncogene RET G-quadruplex revealed by NMR.
机构信息
State Key Laboratory of Bioorganic and Natural Product Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.
Institute of Drug Discovery Technology, Ningbo University, No. 818 Fenghua Road, Ningbo, Zhejiang 315211, China.
出版信息
Chem Commun (Camb). 2020 Feb 18;56(14):2099-2102. doi: 10.1039/d0cc00221f. Epub 2020 Feb 6.
G-quadruplexes (G4s) are frequently formed in the promoter regions of oncogenes, considered as promising drug targets for anticancer therapy. Due to high structure similarity of G4s, discovering ligands selectively interacting with only one G4 is extremely difficult. Here, mainly by NMR, we report that colchicine selectively binds to oncogene RET G4-DNA.
G-四链体（G4s）经常在癌基因的启动子区域形成，被认为是癌症治疗有前途的药物靶点。由于 G4s 具有高度的结构相似性，因此很难发现仅与一种 G4 选择性相互作用的配体。在这里，主要通过 NMR，我们报告秋水仙碱选择性地结合癌基因 RET G4-DNA。
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