Raymond E, Sun D, Chen S F, Windle B, Von Hoff D D
Human Telomerase Research Group, Institute for Drug Development - Cancer Therapy and Research Center, 14960 Omicron Drive, San Antonio, TX 78245-3217, USA.
Curr Opin Biotechnol. 1996 Dec;7(6):583-91. doi: 10.1016/s0958-1669(96)80068-1.
Telomeres are guanine-rich regions that are located at the ends of chromosomes and are essential for preventing aberrant recombination and protecting against exonucleolytic DNA degradation. Telomeres are maintained by telomerase, an RNA-dependent DNA polymerase. Because telomerase is known to be expressed in tumor cells, which concurrently have short telomeres, and not in most somatic cells, which usually have long telomeres, telomerase and telomere structures have been recently proposed as attractive targets for the discovery of new anticancer agents. The most exciting current strategies are aimed at specifically designing new drugs that target telomerase or telomeres and new models have been formulated to study the biological effects of inhibitors of telomerase and telomeres both in vitro and in vivo.
端粒是位于染色体末端富含鸟嘌呤的区域，对于防止异常重组和保护免受核酸外切酶介导的DNA降解至关重要。端粒由端粒酶维持，端粒酶是一种依赖RNA的DNA聚合酶。由于已知端粒酶在具有短端粒的肿瘤细胞中表达，而在通常具有长端粒的大多数体细胞中不表达，因此端粒酶和端粒结构最近被提议作为发现新型抗癌药物的有吸引力的靶点。当前最令人兴奋的策略旨在专门设计靶向端粒酶或端粒的新药，并且已经制定了新的模型来研究端粒酶和端粒抑制剂在体外和体内的生物学效应。
