G-四链体(G-quadruplex,G4)是由富含串联重复的鸟嘌呤碱基(G)的DNA或RNA链折叠形成的一种特殊的核酸二级结构.可形成G4结构的核酸序列在基因组和人端粒中广泛存在,对生理和病理过程起重要的调节作用.近年来研究发现,一些化学合成的G4核酸具有选择性的抗肿瘤增殖活性;其中AS1411是一个26个碱基的G4序列核酸,目前已作为抗癌药物进入二期临床研究.对G4核酸的结构和功能,抗癌活性及分子机理研究进行综合评述,并简要介绍G4核酸在相关领域的应用研究.%G-quadruplexes(G4s) are four-stranded nucleic acid structures adopted by some repetitive guanine-rich sequences.G4 sequences are highly prevalent in human genome and telomere.Recently,some synthetic G4s have been reported to have cancer-selective antiproliferative activity.AS1411,a 26-mer G4 DNA,is currently in phase II clinical trials as an anticancer agent.The structures,functions,antiproliferative activities and mechanisms,and the applications of G4s are reviewed.
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