具抑制端粒酶活性的G-四链体小分子配体研究进展

Progress in the study of G-quadruplex telomerase inhibitors

端粒酶能阻止端粒的缩短使细胞无限增殖形成肿瘤。端粒3′端富G序列在一定生理条件下可形成具有抑制端粒酶活性的G-四链体结构,从而达到促进肿瘤细胞凋亡的作用。能够诱导DNA特别是致癌基因富G区域形成并稳定G-四链体结构的配体具有重要的抗肿瘤意义。以G-四链体为抗癌药物作用靶点对化合物进行筛选和结构设计是目前化学家和生物学家的关注点。该文对近年来以G-四链体为靶点的小分子端粒酶抑制剂的研究进行了综述。

Telomerase can inhibit the shortening of telomere and stimulate continuous cell proliferation to form tumor. The activity of telomerase can be prohibited by G-quadruplex formed by the single chain in G-rich field of telomere 3＇ end,resulting in tumor cell apoptosis. Ligands which can induce the formation or stabilize the structure of G-quadruplex in G-rich field of oncogene exhibit antitumor function. Nowadays it becomes the coreconcern of chemists and biologists to screen and structurally design the compounds targeting G-quadruplex. This paper summarized the discoveries in the G-quadruplex-targeted telomerase inhibitors in recent years.