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季铵锌酞菁:通过稳定G-四链体以及诱导G-四链体结构转变和形成来抑制端粒酶

Quaternary ammonium zinc phthalocyanine: inhibiting telomerase by stabilizing G quadruplexes and inducing G-quadruplex structure transition and formation.

作者信息

Ren Lige, Zhang Anming, Huang Jing, Wang Ping, Weng Xiaocheng, Zhang Lixia, Liang Feng, Tan Zheng, Zhou Xiang

机构信息

College of Chemistry and Molecular Sciences, Wuhan University, Hongshan, Luo Jia Shan, Hubei, Wuhan 430072, P.R. China.

出版信息

Chembiochem. 2007 May 7;8(7):775-80. doi: 10.1002/cbic.200600554.

Abstract

Water-soluble, octacationic zinc phthalocyanine (ZnPc) was found to be a very good G-quadruplex DNA stabilizer by using UV-melting studies and DNA polymerase stop assays, and a potent telomerase inhibitor by using the telomeric repeat amplification protocol (TRAP) assay. The compound's DNA-binding properties were also studied by surface plasmon resonance (SPR). Furthermore, CD experiments demonstrated that ZnPc could induce intramolecular G-quadruplex structure transition from the antiparallel to parallel form. More importantly, ZnPc was found to induce parallel structure formation in cation-deficient conditions. The stability of the induced structure was determined with CD melting assays.

摘要

通过紫外熔解研究和DNA聚合酶终止试验发现,水溶性八阳离子锌酞菁(ZnPc)是一种非常好的G-四链体DNA稳定剂,并且通过端粒重复扩增协议(TRAP)试验发现它是一种有效的端粒酶抑制剂。还通过表面等离子体共振(SPR)研究了该化合物的DNA结合特性。此外,圆二色性实验表明,ZnPc可以诱导分子内G-四链体结构从反平行形式转变为平行形式。更重要的是,发现ZnPc在阳离子缺乏的条件下能诱导平行结构的形成。通过圆二色性熔解试验确定了诱导结构的稳定性。

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