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端粒酶是一种核糖蛋白,包括人端粒酶RNA、端粒酶相关蛋白和端粒酶催化蛋白亚单位三个主要组成部分,可向染色体末端添加端粒DNA序列。端粒酶在85%~95%的恶性肿瘤组织中有阳性表达,而正常体细胞则一般阴性,是进行肿瘤基因治疗的理想靶点。目前以抑制端粒酶活性为划点的肿瘤治疗研究较多,其主要策略有:①阻断人端粒酶RNA的模板作用;②抑制端粒酶催化蛋白亚单位;③核苷类似物竞争性抑制反转录过程;④细胞分化诱导剂抑制端粒酶活性;⑤对细胞内调节机制进行调控;⑥其它抑制剂对端粒酶活性的调节。
Telomerase is a riboprotein that includes three main components of human telomerase RNA, telomerase-associated protein, and telomerase-catalyzed protein subunit, and can add telomere DNA sequences to the ends of chromosomes. Telomerase is positively expressed in 85% to 95% of malignant tumors, whereas normal somatic cells are generally negative. It is an ideal target for tumor gene therapy. At present, there are many researches on the treatment of tumors with the inhibition of telomerase activity. The main strategies are as follows: (1) blocking the template action of human telomerase RNA; (2) inhibiting the telomerase catalytic protein subunit; (3) competing with nucleoside analogs; Suppression of reverse transcription; 4 cell differentiation inducer inhibits telomerase activity; 5 regulates the regulation of intracellular regulation; 6 other inhibitors on the regulation of telomerase activity.