Department of Pediatrics, Children's Hospital Colorado and University of Colorado Denver, Anschutz Medical Campus, Aurora, CO, USA.
J Neurooncol. 2013 Jan;111(2):113-21. doi: 10.1007/s11060-012-1000-7. Epub 2012 Nov 9.
Medulloblastoma accounts for 20 % of all primary pediatric intracranial tumors. Current treatment cures 50-80 % of patients but is associated with significant long-term morbidity and thus new therapeutic targets are needed. One such target is cyclin-dependent kinase 6 (CDK6), a serine/threonine kinase that plays a vital role in cell cycle progression and differentiation. CDK6 is overexpressed in medulloblastoma patients and is associated with an adverse prognosis. To investigate the role of CDK6 in medulloblastoma, we assayed the effect of CDK6 inhibition on proliferation by depleting expression with RNA interference (RNAi) or by inhibiting kinase function with a small molecule inhibitor, PD0332991. Cell proliferation was assessed by colony focus assay or by the xCELLigence system. We then investigated the impact of CDK6 inhibition on differentiation of murine neural stem cells by immunofluorescence of relevant markers. Finally we evaluated the effects of PD0332991 treatment on medulloblastoma cell cycle and radiosensitivity using colony focus assays. Gene expression analysis revealed that CDK6 mRNA expression is higher than normal cerebellum in fifteen out of sixteen medulloblastoma patient samples. Inhibition of CDK6 by RNAi significantly decreased medulloblastoma cell proliferation and colony forming potential. Interestingly, CDK6 inhibition by RNAi increased differentiation in murine neural stem cells. PD0332991 treatment significantly decreased medulloblastoma cell proliferation and led to a G0/G1 cell cycle arrest. Furthermore, PD0332991 pretreatment sensitized medulloblastoma cells to ionizing radiation. Our findings suggest that targeting CDK6 with small molecule inhibitors may prove beneficial in the treatment of medulloblastoma, especially when combined with radiation.
成神经管细胞瘤占所有儿童颅内原发性肿瘤的 20%。目前的治疗方法可治愈 50-80%的患者,但会导致严重的长期发病率,因此需要新的治疗靶点。其中一个靶点是细胞周期蛋白依赖性激酶 6(CDK6),一种丝氨酸/苏氨酸激酶,在细胞周期进程和分化中起着至关重要的作用。CDK6 在成神经管细胞瘤患者中过度表达,与不良预后相关。为了研究 CDK6 在成神经管细胞瘤中的作用,我们通过 RNA 干扰(RNAi)耗尽表达或用小分子抑制剂 PD0332991 抑制激酶功能来检测 CDK6 抑制对增殖的影响。通过集落焦点测定或 xCELLigence 系统评估细胞增殖。然后,我们通过免疫荧光检测相关标志物,研究 CDK6 抑制对鼠神经干细胞分化的影响。最后,我们通过集落焦点测定评估 PD0332991 处理对成神经管细胞瘤细胞周期和放射敏感性的影响。基因表达分析显示,在 16 例成神经管细胞瘤患者样本中,有 15 例的 CDK6 mRNA 表达高于正常小脑。通过 RNAi 抑制 CDK6 显著降低成神经管细胞瘤细胞增殖和集落形成能力。有趣的是,CDK6 抑制通过 RNAi 增加了鼠神经干细胞的分化。PD0332991 处理显著降低了成神经管细胞瘤细胞的增殖,并导致 G0/G1 细胞周期停滞。此外,PD0332991 预处理使成神经管细胞瘤细胞对电离辐射敏感。我们的研究结果表明,用小分子抑制剂靶向 CDK6 可能对成神经管细胞瘤的治疗有益,尤其是与放射治疗联合使用时。