Department II of Internal Medicine and Center for Molecular Medicine Cologne, Cologne, Germany.
Cell Cycle. 2012 Nov 15;11(22):4122-8. doi: 10.4161/cc.21997. Epub 2012 Sep 14.
Following genotoxic stress, cells activate a complex, kinase-based signaling network to arrest the cell cycle and initiate DNA repair or apoptosis. The tumor suppressor p53 lies at the heart of this DNA damage response. p53 mediates the transactivation of both cell cycle-regulating and pro-apoptotic clusters of target genes. However, it remains incompletely understood which signaling molecules dictate the choice between these two opposing p53-dependent cellular outcomes. Over recent years, numerous regulatory mechanisms impacting on the cellular outcome of p53 signaling have been described. However, no single dominant mechanism has thus far been identified to regulate the cellular choice between p53-driven apoptosis or senescence. The transcriptional regulator AATF has recently emerged as a novel factor impacting on the cellular outcome of the p53 response. Upon genotoxic stress, cytoplasmic pools of MRLC-bound AATF are phosphorylated through the p38MAPK/MK2 checkpoint kinase complex. This AATF phosphorylation results in the disruption of cytoplasmic MRLC3:AATF complexes followed by rapid nuclear localization of AATF. Once in the nucleus, AATF binds to the PUMA, BAX and BAK promoters to repress the DNA damage-induced expression of these pro-apoptotic p53 target genes. Depletion of AATF in tumor cells results in a dramatically enhanced response to DNA-damaging chemotherapeutics, both in vitro and in vivo. Furthermore, focal copy number gains at the AATF locus in neuroblastoma correlate with adverse prognosis and reduced overall survival in this typically p53-proficient malignancy. These data identify the p38/MK2/AATF signaling pathway as a critical repressor of p53-driven apoptosis in tumor cells and implicate this signaling cascade as a novel target for chemotherapy-sensitizing therapeutic efforts.
在遗传毒性应激后,细胞激活一个复杂的、基于激酶的信号网络,以阻止细胞周期并启动 DNA 修复或细胞凋亡。肿瘤抑制因子 p53 处于这个 DNA 损伤反应的核心。p53 介导细胞周期调节和促凋亡靶基因簇的转录激活。然而,p53 依赖性细胞命运之间的选择取决于哪些信号分子,这一点仍不完全清楚。近年来,描述了许多影响 p53 信号细胞后果的调节机制。然而,迄今为止,尚未确定单一的主导机制来调节 p53 驱动的凋亡或衰老之间的细胞选择。转录调节因子 AATF 最近成为影响 p53 反应细胞后果的一个新因素。在遗传毒性应激下,细胞质中与 MRLC 结合的 AATF 池通过 p38MAPK/MK2 检查点激酶复合物磷酸化。这种 AATF 磷酸化导致细胞质中 MRLC3:AATF 复合物的破坏,随后 AATF 迅速核定位。一旦进入细胞核,AATF 就结合到 PUMA、BAX 和 BAK 启动子上,抑制这些促凋亡 p53 靶基因的 DNA 损伤诱导表达。在肿瘤细胞中耗尽 AATF 会导致对 DNA 损伤化学疗法的反应显著增强,无论是在体外还是体内。此外,神经母细胞瘤中 AATF 基因座的局部拷贝数增益与不良预后相关,并降低了这种典型的 p53 丰富恶性肿瘤的总生存率。这些数据表明 p38/MK2/AATF 信号通路是肿瘤细胞中 p53 驱动的细胞凋亡的关键抑制剂,并暗示该信号级联作为化疗增敏治疗努力的新靶点。