小分子端粒酶抑制剂的研究进展

Advances on small-molecule telomerase inhibitors

端粒酶是真核生物中一种逆转录酶,它能将端粒区的G重复序列加到染色体末端以维持端粒长度的稳定。端粒酶在绝大多数恶性肿瘤中特异性表达,因而它是肿瘤靶向治疗的靶点之一,研究和开发小分子端粒酶抑制剂将为癌症的诊断和治疗带来新的希望。该文重点介绍近年来报道的不同结构类型的小分子端粒酶抑制剂,并对其活性及构效关系进行综述。

Telomerase is a ribonucleoprotein enzyme maintaining the length of the telomeres by adding G-rich repeats to the end of the eukaryotic chromosomes.Telomerase is specifically expressed in most tumor cells and may be proposed as an attractive targets for cancer therapy.Research and development of new small molecule telomerase inhibitors brings hope for the diagnosis and treatment of tumor.This review had highlighted recent developments in different chemical types of telomerase inhibitors.The biological activity and the structure-activity relationship aspects were also described.