Development of G-quadruplex ligands for selective induction of a parallel-type topology,Organic & Biomolecular Chemistry

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Development of G-quadruplex ligands for selective induction of a parallel-type topology
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2018-08-29 , DOI: 10.1039/c8ob01702f
Yue Ma _{1,

2,

3,

4,

5} , Yamato Tsushima _{1,

2,

3,

4,

5} , Mai Sakuma _{1,

2,

3,

4,

5} , Shogo Sasaki _{1,

2,

3,

4,

5} , Keisuke Iida _{5,

6,

7,

8,

9} , Sachiko Okabe _{10,

11,

12,

13,

14} , Hiroyuki Seimiya _{10,

11,

12,

13,

14} , Takatsugu Hirokawa _{5,

15,

16,

17,

18} , Kazuo Nagasawa _{1,

2,

3,

4,

5}

Affiliation

Department of Life Science and Biotechnology
Faculty of Technology
Tokyo University of Agriculture and Technology
Koganei
Japan
Department of Chemistry
Faculty of Science
Chiba University
Chiba 263-8522
Division of Molecular Biotherapy
Cancer Chemotherapy Center
Japanese Foundation for Cancer Research
Koto-ward
Tokyo 135-8550
Transborder Medical Research Center
University of Tsukuba
Tsukuba, 305-8575
Division of Biomedical Science

G-Quadruplex structures (G4s) in guanine-rich regions of DNA play critical roles in various biological phenomena, including replication, translation, and gene expression. The G4-forming DNAs can form three kinds of topologies, i.e., parallel, anti-parallel, and hybrid. In this paper, we present G4 ligands L2H2-2M2EA-6OTD (3) and L2G2-2M2EG-6OTD (4) bearing tetra-aminoalkyl and -guanidinylalkyl side chains, respectively, in a macrocyclic hexaoxazole structure. These ligands efficiently induce the parallel-type topology of telomeric G4 regardless of the effects of cations. Titration with 4 results in a drastic topology switch to the parallel topology from the anti-parallel structure induced by the structurally related ligand L2H2-6OTD (1).

中文翻译：

用于选择性诱导平行型拓扑的G-四链体配体的开发

DNA富含鸟嘌呤的区域中的G四联体结构（G4）在各种生物学现象（包括复制，翻译和基因表达）中起关键作用。形成G4的DNA可以形成三种拓扑，即并行，反并行和混合。在本文中，我们提出了在大环六恶唑结构中分别带有四氨基烷基和-胍基烷基侧链的G4配体L2H2-2M2EA-6OTD（3）和L2G2-2M2EG-6OTD（4）。这些配体可有效诱导端粒G4的平行型拓扑结构，而不受阳离子的影响。用4滴定结果导致急剧的拓扑结构从结构相关的配体L2H2-6OTD（1）诱导的反平行结构转换为平行拓扑。

更新日期：2018-10-18

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