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富含鸟嘌呤的单链DNA序列可以缠绕折叠形成G- 四链体结构。人类基因组中有36,000 个以上的DNA 序列有潜力生成 G-四链体，如端粒末端重复序列，以及c-myc、c-kit、bcl-2 等原癌基因启动子区域。G-四链体是由四个鸟嘌呤之间通过Hoogsteen 氢键形成G-四分体，相邻的G-四分体再通过π-π 堆积作用，由糖- 磷酸骨架相连而成。G- 四链体DNA 的形成有着重要的生物学意义，它和相关基因表达水平密切相关，诱导和稳定G- 四链体结构就有可能抑制癌基因的转录和表达，引起肿瘤细胞生物学功能的紊乱，从而抑制肿瘤细胞的增殖。G-四链体结构作为新的抗肿瘤药物靶点引起了科学家的广泛关注，能够稳定G- 四链体结构的配体包括二酰胺蒽醌类、苝类、阳离子卟啉类、金属配合物和天然产物等。本文对近年来以G-四链体为靶点的配体的研究进行了综述。

英文摘要:

Guanine-rich DNA sequences can flod G-quadruplex structure. More than 36,000 DNA sequences in the human genome has the potential to form G-quadruplex structure, such as telomeric chromosomal terminals and c-myc, c-kit, bcl-2 oncogene promoter region. G-quadruplex structure is composed of stacked guanine tetrads which is assembled via Hoogsteen hydrogen-bonding in a coplanar arrangement. The formation of DNA G-quadruplex have important biological significance and it is related to the level of gene expression. The induction and stabilization of G-quadruplex structure can lead to the biology disorder of tumor cell, thereby inhibiting the proliferation of tumor cell. G-quadruplex structure, as a new anticancer drug target, has caused much attention. The ligands which can stabilize the G-quadruplex structure include diamide anthraquinone, perylene, cationic porphyrins, metal complexes and natural products. This article briefly describes the formation and biological significance of G-quadruplex, also current developments in G-quadruplex targeted ligands were reviewed.

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