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An important functional group, benzo[1,3]dioxole, of alkaloids induces the formation of the human telomeric dna G-quadruplex

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Science Bulletin 2011年第7期 611-617页

作者： YANG Shu1,2, XIANG JunFeng1, YANG QianFan1,2, ZHOU QiuJu1,2, ZHANG XiuFeng1, Li Qian1,2, TANG YaLin1 & XU GuangZhi1 1 Beijing National Laboratory for Molecular Sciences, Centre for Molecular Sciences, State Key Laboratory for Structural Chemistry for Unstable and Stable Species Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China 2 Graduate University of Chinese Academy of Sciences, Beijing 100049, China

Over the past few decades, numerous molecules have been discovered or designed to interact efficiently and selectively with a peculiar dna structure named G-quadruplex. Some of these molecules have been developed as anticancer agents. To aid the design of anticancer agents, the ability of alkaloids possessing Protoberberine and Benzophenanthridine groups to induce the formation of G-quadruplexes were studied using CD spectroscopy. By careful examination of their structures, we found that a benzo[1,3]dioxole group plays an important role in influencing their inductive properties. The more functional groups the alkaloids have, the stronger their G-quadruplex inductive ability.

关键词： benzo[1 3]dioxole group telomeric dna G-quadruplex alkaloids Protoberberine Benzophenanthridine

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

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Chemical Research in Chinese Universities 2021年第3期37卷 795-800页

作者： HAO Xueyu LI Chunjie WANG Yu ZHANG Feng HOU Jingwei KANG Chunqing GAO Lianxun Laboratory of Polymer Composite and Engineering Changchun Institute of Applied ChemistryChinese Academy of SciencesChangchun130022P.R.China University of Science and Technology of China Hefei230026P.R.China

G-Quadruplexes(GQs),which are formed by G-rich dna sequences in human telomeres,have become an attractive target for cancer *** 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 *** 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 *** provide an insight into the dynamic conversion from initial hybrid-2 GQ topology to final parallel GQ *** results are helpful for the design of ligands with GQ conformation regulation.

关键词： G-Quadruplex Naphthalene diimide Topological conversion telomeric dna

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