Lixia Guo, Fei Yin, Jiajia Jing, Jianhui Liu
Research Center of Pharmaceutical Chemistry & Chemobiology, Chongqing Technology and Business University, Chongqing 400067, China.
Biotechnol Lett. 2008 Jan;30(1):47-53. doi: 10.1007/s10529-007-9513-4. Epub 2007 Sep 6.
Interference with telomerase and telomere maintenance is emerging as an attractive target for antitumor therapies. Ligands stabilizing G-quadruplexes have the potential to interfere with telomere replication by blocking the elongation of telomeres in tumors. Here, we report that long-term treatment with triethylene tetramine (TETA), at 50 or 100 microM, induced marked cellular senescence phenotypes accompanied by increased time of population doubling of MCF-7 cells. Cyclin-dependent kinase inhibitors, including p53 and p21, were also upregulated in TETA-treated MCF-7 cells. TETA is therefore as novel ligand of G-quadruplex and can induce tumor senescence; it is a promising material for tumor treatment.
干扰端粒酶和端粒维持正成为一种有吸引力的抗肿瘤治疗靶点。稳定G-四链体的配体有可能通过阻断肿瘤中端粒的延长来干扰端粒复制。在此，我们报告，用50或100微摩尔的三亚乙基四胺（TETA）长期处理，可诱导明显的细胞衰老表型，同时伴有MCF-7细胞群体倍增时间增加。在TETA处理的MCF-7细胞中，包括p53和p21在内的细胞周期蛋白依赖性激酶抑制剂也上调。因此，TETA是一种新型的G-四链体配体，可诱导肿瘤衰老；它是一种有前途的肿瘤治疗材料。
