端粒酶抑制剂研究进展

Advances in research of telomerase inhibitors

目的综述端粒酶抑制剂的研究进展。方法查阅近几年来国内外相关文献33篇,对其进行归纳、总结和分析。结果端粒酶是一种DNA逆转录酶,具有催化端粒DNA合成的功能,在85%~90%的肿瘤细胞中特异性表达。近几年来,人们发现的端粒酶抑制剂包括杨梅酮衍生物、南蛇藤醇衍生物、小檗碱类化合物、波尔定碱、虫草素等天然小分子及其类似物,以及伊美司他、噁二唑类化合物、吡唑类化合物、芳基乙烯类化合物、苯亚甲基-腙类化合物、咔唑类化合物和蒽醌类化合物等合成小分子类化合物。个别化合物已经进入了临床研究阶段。结论端粒酶抑制剂作为一类潜在的高选择性抗癌药物,为恶性肿瘤的诊断和治疗提供新的希望。

Objective To reviewthe advances in research of telomerase inhibitors.Methods Thirty-three relevant literatures on telomerase inhibitors were summarized and analyzed.Results As a DNA reverse transcriptase,telomerase can catalyze the synthesis of telomere DNA and it is selectively overexpressed in up to 85%-90% of tumor cells.In recent years,some telomerase inhibitors including natural small molecules such as myricelin derivatives,celastrol derivatives,berberine derivatives,boldine,cordycepin,and some synthetic small molecules such as imetelstat,oxadiazoles,pyrazoles,styrene derivatives,benzylene-hydrazone compounds,carbazoles,anthraquinones were found and studied.Among them,a fewcompounds have already been in clinical trials.Conclusions As a potential highly selective anticancer drug,telomerase inhibitor might bring newhopes for the diagnosis and treatment of malignant tumors.