Division of Medical Oncology, Department of Internal Medicine, Norris Comprehensive Cancer Center, Keck School of Medicine, University of Southern California, Los Angeles, California 90033, USA.
Mol Cancer Ther. 2010 Feb;9(2):438-49. doi: 10.1158/1535-7163.MCT-09-0682. Epub 2010 Feb 2.
Telomerase plays a critical role in cancer, prompting the pursuit of various telomerase-based therapeutic strategies. One such strategy, telomerase interference, exploits the high telomerase activity in cancer cells and reprograms telomerase to encode "toxic" telomeres. To date, telomerase interference has been tested in human cancer cells xenografted into mice, an approach that does not recapitulate spontaneous malignancy and offers few insights about host toxicities, because human telomerase is targeted in a mouse host. To address these limitations, we designed and validated two new gene constructs specifically targeting mouse telomerase: mutant template mouse telomerase RNA (MT-mTer) and small interfering RNA against wild-type mouse telomerase RNA (α-mTer-siRNA). Using lentiviral delivery in mouse prostate cancer cells, we achieved α-mTer-siRNA-mediated knockdown of wild-type mTer (80% depletion) and concurrent overexpression of MT-mTer (50-fold). We showed that the two constructs effectively synergize to reprogram murine telomerase to add mutant instead of wild-type telomeric repeats, resulting in rapid telomeric uncapping (5-fold increase in DNA damage foci). This, in turn, led to rapid and significant apoptosis (>90% of cells) and growth inhibition in vitro (90% reduction in viable cell mass) and in vivo (75% reduction in tumor allograft wet weight). In summary, we have shown that mouse cancer cells are vulnerable to direct telomerase interference using novel murine telomerase-targeting constructs; this approach can now be used to study the true therapeutic potential of telomerase interference in mouse spontaneous cancer models.
端粒酶在癌症中起着关键作用,促使人们寻求各种基于端粒酶的治疗策略。其中一种策略是端粒酶干扰,利用癌细胞中端粒酶的高活性,重新编程端粒酶以编码“毒性”端粒。迄今为止,端粒酶干扰已在移植入小鼠的人类癌细胞中进行了测试,这种方法不能再现自发性恶性肿瘤,并且由于在小鼠宿主中靶向人类端粒酶,因此很少能提供关于宿主毒性的见解。为了解决这些局限性,我们设计并验证了两种专门针对小鼠端粒酶的新基因构建体:突变模板小鼠端粒酶 RNA(MT-mTer)和针对野生型小鼠端粒酶 RNA 的小干扰 RNA(α-mTer-siRNA)。我们使用慢病毒在小鼠前列腺癌细胞中进行递送,实现了α-mTer-siRNA 介导的野生型 mTer 的敲低(80%耗竭)和 MT-mTer 的过表达(50 倍)。我们表明,这两种构建体有效地协同作用,将小鼠端粒酶重新编程为添加突变而非野生型端粒重复序列,导致端粒快速去帽(DNA 损伤焦点增加 5 倍)。这反过来又导致体外(细胞活力减少 90%)和体内(肿瘤异种移植物湿重减少 75%)快速而显著的细胞凋亡(超过 90%的细胞)和生长抑制。总之,我们已经表明,使用新型的靶向小鼠端粒酶的构建体,小鼠癌细胞容易受到直接的端粒酶干扰;现在可以使用这种方法来研究端粒酶干扰在小鼠自发性癌症模型中的真正治疗潜力。