G-四链体DNA稳定剂的研究进展

The study of G-quadruplex stabilizers

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.

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.