中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Porphyrin Bound to i-Motifs: Intercalation versus External Groove Binding

文献类型:期刊论文

作者Qin, Tingxiao1,3; Liu, Kunhui2; Song, Di1; Yang, Chunfan2; Su, Hongmei2
刊名CHEMISTRY-AN ASIAN JOURNAL
出版日期2017-07-04
卷号12期号:13页码:1578-1586
关键词Dna Structures I-motif Intercalations Laser Flash Photolysis Pi Interactions Porphyrinoids
英文摘要G-rich and C-rich DNA can fold into the tetrastranded helical structures G quadruplex or C quadruplex (imotif), which are considered to be specific drug targets for cancer therapy. A large number of small molecules (so-called ligands), which can bind and modulate the stability of G quadruplex structures, have been widely examined. Much less is known, however, about the ligand binding interactions with the C quadruplex (i-motif). By combining steadystate measurements (UV/Vis, fluorescence, and induced circular dichroism (ICD)) with time-resolved laser flash photolysis spectroscopy, we have studied the binding interactions of cationic porphyrin (5,10,15,20-tetrakis(N-methylpyridinium- 4-yl)-21H, 23H-porphyrin, abbreviated as TMPyP4) with imotifs (C(3)TA(2))(3)C3T and (C(4)A(4)C(4))(2). The intercalation binding mode through pi-pi stacking of the porphyrin macrocycle and the C: C+ hemiprotonated base pair has been identified for the first time. The coexistent binding modes of intercalation (approximate to 80%) versus external major-groove binding (approximate to 20%) have been determined quantitatively, thereby allowing a fuller understanding of the porphyrin-i-motif interactions. The ionic strength was found to play an important role in affecting affects the binding modes, with the progressive increase in the ionic strength resulting in the gradual decrease in the intercalation percentage and an increase in the groove-binding percentage. Furthermore, an extended study of the porphyrin derivative with four bulky side-arm substituents (T4) suggests a complete prohibition of the intercalation mode owing to large steric hindrance, thereby providing a novel groove-binding ligand with site selectivity. These results provide in-depth mechanistic insights to better understand the ligand interactions with i-motifs and guidance for related applications in anticancer drug design.
语种英语
源URL[http://ir.iccas.ac.cn/handle/121111/39212]  
专题化学研究所_绿色印刷实验室
作者单位1.Chinese Acad Sci, Inst Chem, Beijing Natl Lab Mol Sci BNLMS, Beijing 100190, Peoples R China
2.Beijing Normal Univ, Coll Chem, Beijing 100875, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714
Qin, Tingxiao,Liu, Kunhui,Song, Di,et al. Porphyrin Bound to i-Motifs: Intercalation versus External Groove Binding[J]. CHEMISTRY-AN ASIAN JOURNAL,2017,12(13):1578-1586.
APA Qin, Tingxiao,Liu, Kunhui,Song, Di,Yang, Chunfan,&Su, Hongmei.(2017).Porphyrin Bound to i-Motifs: Intercalation versus External Groove Binding.CHEMISTRY-AN ASIAN JOURNAL,12(13),1578-1586.
MLA Qin, Tingxiao,et al."Porphyrin Bound to i-Motifs: Intercalation versus External Groove Binding".CHEMISTRY-AN ASIAN JOURNAL 12.13(2017):1578-1586.

入库方式: OAI收割

来源:化学研究所

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