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

doi:10.1007/s40242-021-1022-9

Chemical Research in Chinese Universities ›› 2021, Vol. 37 ›› Issue (3): 795-800.doi: 10.1007/s40242-021-1022-9

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

HAO Xueyu^1,2, LI Chunjie¹, WANG Yu^1,2, ZHANG Feng¹, HOU Jingwei¹, KANG Chunqing^1,2, GAO Lianxun¹

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.

Abstract

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

HAO Xueyu, LI Chunjie, WANG Yu, ZHANG Feng, HOU Jingwei, KANG Chunqing, GAO Lianxun. NDI-induced Topological Conversion of Human Telomeric G-Quadruplexes from Hybrid-2 to Parallel Form[J]. Chemical Research in Chinese Universities, 2021, 37(3): 795-800.

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

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