Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil.
Cell Death Dis. 2013 Aug 15;4(8):e767. doi: 10.1038/cddis.2013.283.
Glioblastomas (GBMs) are devastating tumors of the central nervous system, with a poor prognosis of 1-year survival. This results from a high resistance of GBM tumor cells to current therapeutic options, including etoposide (VP-16). Understanding resistance mechanisms may thus open new therapeutic avenues. VP-16 is a topoisomerase inhibitor that causes replication fork stalling and, ultimately, the formation of DNA double-strand breaks and apoptotic cell death. Autophagy has been identified as a VP-16 treatment resistance mechanism in tumor cells. Retinoblastoma protein (RB) is a classical tumor suppressor owing to its role in G1/S cell cycle checkpoint, but recent data have shown RB participation in many other cellular functions, including, counterintuitively, negative regulation of apoptosis. As GBMs usually display an amplification of the EGFR signaling involving the RB protein pathway, we questioned whether RB might be involved in mechanisms of resistance of GBM cells to VP-16. We observed that RB silencing increased VP-16-induced DNA double-strand breaks and p53 activation. Moreover, RB knockdown increased VP-16-induced apoptosis in GBM cell lines and cancer stem cells, the latter being now recognized essential to resistance to treatments and recurrence. We also showed that VP-16 treatment induced autophagy, and that RB silencing impaired this process by inhibiting the fusion of autophagosomes with lysosomes. Taken together, our data suggest that RB silencing causes a blockage on the VP-16-induced autophagic flux, which is followed by apoptosis in GBM cell lines and in cancer stem cells. Therefore, we show here, for the first time, that RB represents a molecular link between autophagy and apoptosis, and a resistance marker in GBM, a discovery with potential importance for anticancer treatment.
胶质母细胞瘤(GBM)是一种毁灭性的中枢神经系统肿瘤,其 1 年生存率较差。这是由于 GBM 肿瘤细胞对目前的治疗选择(包括依托泊苷(VP-16))具有很高的耐药性。因此,了解耐药机制可能会开辟新的治疗途径。VP-16 是一种拓扑异构酶抑制剂,可导致复制叉停滞,最终形成 DNA 双链断裂和凋亡细胞死亡。自噬已被确定为肿瘤细胞中 VP-16 治疗耐药的机制。视网膜母细胞瘤蛋白(RB)是一种经典的肿瘤抑制因子,因为它在 G1/S 细胞周期检查点中的作用,但最近的数据表明 RB 参与许多其他细胞功能,包括,与预期相反,负调控细胞凋亡。由于 GBM 通常显示 EGFR 信号的扩增,涉及 RB 蛋白途径,我们质疑 RB 是否参与 GBM 细胞对 VP-16 的耐药机制。我们观察到 RB 沉默增加了 VP-16 诱导的 DNA 双链断裂和 p53 激活。此外,RB 敲低增加了 GBM 细胞系和癌症干细胞中 VP-16 诱导的细胞凋亡,后者现在被认为对治疗和复发的耐药性至关重要。我们还表明,VP-16 处理诱导自噬,并且 RB 沉默通过抑制自噬体与溶酶体的融合来破坏该过程。总之,我们的数据表明,RB 沉默导致 VP-16 诱导的自噬通量受阻,随后在 GBM 细胞系和癌症干细胞中发生细胞凋亡。因此,我们在这里首次表明,RB 代表自噬和细胞凋亡之间的分子联系,并且是 GBM 的耐药标志物,这一发现对于癌症治疗具有潜在的重要意义。