多骨髓瘤中纽兰诱导细胞凋亡的分子机制:p53 转录依赖性和非依赖性途径的证据。
Molecular mechanisms of nutlin-induced apoptosis in multiple myeloma: evidence for p53-transcription-dependent and -independent pathways.
机构信息
Division of Molecular and Cellular Biology, Toronto General Hospital Research Institute, Dept of Laboratory Medicine and Pathobiology, University of Toronto, Ontario, Canada.
出版信息
Cancer Biol Ther. 2010 Sep 15;10(6):567-78. doi: 10.4161/cbt.10.6.12535. Epub 2010 Oct 1.
Multiple myeloma (MM) is an incurable plasma cell malignancy in which p53 is rarely mutated. Thus, activation of the p53 pathway by a small molecule inhibitor of the p53-MDM2 interaction, nutlin, in MM cells retaining wild type p53 is an attractive therapeutic strategy. Recently we reported that nutlin plus velcade (a proteasome inhibitor) displayed a synergistic response in MM. However, the mechanism of the p53-mediated apoptosis in MM has not been fully understood. Our data show that nutlin-induced apoptosis correlated with reduction in cell viability, upregulation of p53, p21 and MDM2 protein levels with a simultaneous increase in pro-apoptotic targets PUMA, Bax and Bak and downregulation of anti-apoptotic targets Bcl2 and survivin and activation of caspase in MM cells harboring wild type p53. Nutlin-induced apoptosis was inhibited when activation of caspase was blocked by the caspase inhibitor. Nutlin caused mitochondrial translocation of p53 where it binds with Bcl2, leading to cytochrome C release. Moreover, blocking the transcriptional arm of p53 by the p53-specific transcriptional inhibitor, pifithrin-α, not only inhibited nutlin-induced upregulation of p53-transcriptional targets but also augmented apoptosis in MM cells, suggesting an association of transcription-independent pathway of apoptosis. However, inhibitor of mitochondrial translocation of p53, PFT-μ, did not prevent nutlin-induced apoptosis, suggesting that the p53 transcription-dependent pathway was also operational in nutlin-induced apoptosis in MM. Our study provides the evidence that nutlin-induced apoptosis in MM cells is mediated by transcription-dependent and -independent pathways and supports further clinical evaluation of nutlin as a novel therapeutic agent in MM.
多发性骨髓瘤(MM)是一种无法治愈的浆细胞恶性肿瘤,其中 p53 很少发生突变。因此,小分子抑制剂 nutlin 通过抑制 p53-MDM2 相互作用来激活 p53 通路,在保留野生型 p53 的 MM 细胞中是一种有吸引力的治疗策略。最近我们报道,在 MM 中,nutlin 加硼替佐米(蛋白酶体抑制剂)显示出协同反应。然而,p53 介导的 MM 细胞凋亡的机制尚未完全理解。我们的数据表明,nutlin 诱导的凋亡与细胞活力降低、p53、p21 和 MDM2 蛋白水平上调、促凋亡靶点 PUMA、Bax 和 Bak 同时增加以及抗凋亡靶点 Bcl2 和 survivin 下调以及 caspase 在携带野生型 p53 的 MM 细胞中的激活相关。当 caspase 激活被 caspase 抑制剂阻断时,nutlin 诱导的凋亡被抑制。nutlin 导致 p53 在线粒体易位,与 Bcl2 结合,导致细胞色素 C 释放。此外,p53 特异性转录抑制剂 pifithrin-α 阻断 p53 的转录激活臂,不仅抑制了 nutlin 诱导的 p53 转录靶基因的上调,而且增强了 MM 细胞的凋亡,表明凋亡存在不依赖转录的途径。然而,p53 线粒体易位抑制剂 PFT-μ 并没有阻止 nutlin 诱导的凋亡,表明 nutlin 诱导的 MM 细胞凋亡中也存在 p53 转录依赖性途径。我们的研究提供了证据,表明 nutlin 诱导的 MM 细胞凋亡是通过转录依赖和非依赖途径介导的,并支持进一步临床评估 nutlin 作为 MM 的新型治疗剂。