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高等学校化学研究 ›› 2021, Vol. 37 ›› Issue (3): 795-800.doi: 10.1007/s40242-021-1022-9

• Article • 上一篇    下一篇

NDI-induced Topological Conversion of Human Telomeric G-Quadruplexes from Hybrid-2 to Parallel Form

HAO Xueyu1,2, LI Chunjie1, WANG Yu1,2, ZHANG Feng1, HOU Jingwei1, KANG Chunqing1,2, GAO Lianxun1   

  1. 1. Laboratory of Polymer Composite and Engineering, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P. R. China;
    2. University of Science and Technology of China, Hefei 230026, P. R. China
  • 收稿日期:2021-01-15 修回日期:2021-02-09 出版日期:2021-06-01 发布日期:2021-03-10
  • 通讯作者: KANG Chuanqing E-mail:kangcq@ciac.ac.cn
  • 基金资助:
    The authors appreciate the technical help of Mr. LI Haoyu(Changchun Institute of Applied Chemistry, Chinese Academy of Sciences) for insightful comments and suggestions.

NDI-induced Topological Conversion of Human Telomeric G-Quadruplexes from Hybrid-2 to Parallel Form

HAO Xueyu1,2, LI Chunjie1, WANG Yu1,2, ZHANG Feng1, HOU Jingwei1, KANG Chunqing1,2, GAO Lianxun1   

  1. 1. Laboratory of Polymer Composite and Engineering, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P. R. China;
    2. University of Science and Technology of China, Hefei 230026, P. R. China
  • Received:2021-01-15 Revised:2021-02-09 Online:2021-06-01 Published:2021-03-10
  • Contact: KANG Chuanqing E-mail:kangcq@ciac.ac.cn
  • Supported by:
    The authors appreciate the technical help of Mr. LI Haoyu(Changchun Institute of Applied Chemistry, Chinese Academy of Sciences) for insightful comments and suggestions.

摘要: G-Quadruplexes(GQs), which are formed by G-rich DNA sequences in human telomeres, have become an attractive target for cancer treatment. The ligands to stabilize the conformation of human telomeric GQs in vivo are particularly important for structure-based ligand design and drug development targeting the noncanonical DNA structure. Here we report the conformational conversion of Tel26 induced by a naphthalene diimide(NDI) ligand in K+ buffer, even at cellular physiological temperature(37℃) and under mimetic cellular crowding conditions created by Ficoll 70. We provide an insight into the dynamic conversion from initial hybrid-2 GQ topology to final parallel GQ topology. These results are helpful for the design of ligands with GQ conformation regulation.

关键词: G-Quadruplex, Naphthalene diimide, Topological conversion, Telomeric DNA

Abstract: G-Quadruplexes(GQs), which are formed by G-rich DNA sequences in human telomeres, have become an attractive target for cancer treatment. The ligands to stabilize the conformation of human telomeric GQs in vivo are particularly important for structure-based ligand design and drug development targeting the noncanonical DNA structure. Here we report the conformational conversion of Tel26 induced by a naphthalene diimide(NDI) ligand in K+ buffer, even at cellular physiological temperature(37℃) and under mimetic cellular crowding conditions created by Ficoll 70. We provide an insight into the dynamic conversion from initial hybrid-2 GQ topology to final parallel GQ topology. These results are helpful for the design of ligands with GQ conformation regulation.

Key words: G-Quadruplex, Naphthalene diimide, Topological conversion, Telomeric DNA