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G-四链体DNA稳定剂的研究进展
引用本文:郑小辉,穆舸,谭彩萍,曹乾,毛宗万.G-四链体DNA稳定剂的研究进展[J].中国科学:化学,2014(4):484-494.
作者姓名:郑小辉  穆舸  谭彩萍  曹乾  毛宗万
作者单位:生物无机与合成化学教育部重点实验室;中山大学化学与化学工程学院,广州510275
基金项目:国家自然科学基金(21172274,21121061,21231007);国家高技术研究发展计划(863计划,2012AA020305);教育部(20100171110013,313058);中央高校基本科研基金的资助
摘    要:人体端粒由富含鸟嘌呤(G)的DNA重复序列组成,该序列在一定的条件下可以形成G-四链体DNA的结构.小分子化合物诱导该结构的形成并使之稳定,不但可以抑制端粒酶的活性或降低癌基因的转录表达而达到抗肿瘤的目的,还可以作为G-四链体DNA的探针,辅助G-四链体DNA生物功能的研究及与之相关疾病的诊断.因此,G-四链体DNA稳定剂的设计是近年来化学生物学的重要前沿领域之一.到目前为止,G-四链体DNA稳定剂主要可分为有机小分子化合物和金属配合物.本文重点综述这两方面特别是后者的最新研究进展.

关 键 词:G-四链体DNA  端粒酶抑制剂  抗肿瘤药物  稳定剂  荧光探针

The study of G-quadruplex stabilizers
ZHENG XiaoHui,MU Ge,TAN CaiPing,CAO Qian,MAO ZongWan.The study of G-quadruplex stabilizers[J].Scientia Sinica Chimica,2014(4):484-494.
Authors:ZHENG XiaoHui  MU Ge  TAN CaiPing  CAO Qian  MAO ZongWan
Institution:MOE Key Laboratory of Bioinorganic and Synthetic Chemistry; School of Chemistry and Chemical Engineering Sun Yat-Sen University, Guangzhou 510275, China
Abstract:Human telomere consists of a series of DNA sequences rich in Guanine, which may form G-quadruplex structure. The formation and stabilization of the specific structure by small molecular compounds can not only inhibit the telomerase and disrupt the mechanism of the maintenance of telomere in cancer cells but also work as a probe for G-quedruplex on the research of the biological functions of G-quadruplex and diagnosis of relevant diseases. So the designing of stabilizers of G-quadruplex has been one of the focuses of chemical biology in recent years. The G-quadruplex stabilizers can be divided in two types up to now: small organic molecular compounds and metal complexes. This review focuses on the latest progress of the two parts, especially the latter one.
Keywords:G-quadruplex DNA  telomerase inhibitor  anti-tumor drugs  stabilize  fluorescent probe
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