Department of Surgical Pathology, Changhua Christian Hospital, Changhua, Taiwan.
Department of Medical Technology, Jen-Teh Junior College of Medicine, Nursing and Management, Miaoli, Taiwan.
Sci Rep. 2016 Aug 16;6:31690. doi: 10.1038/srep31690.
While aberrant JAK/STAT signaling is crucial to the development of gastric cancer (GC), its effects on epigenetic alterations of its transcriptional targets remains unclear. In this study, by expression microarrays coupled with bioinformatic analyses, we identified a putative STAT3 target gene, NR4A3 that was downregulated in MKN28 GC daughter cells overexpressing a constitutively activated STAT3 mutant (S16), as compared to an empty vector control (C9). Bisulphite pyrosequencing and demethylation treatment showed that NR4A3 was epigenetically silenced by promoter DNA methylation in S16 and other GC cell lines including AGS cells, showing constitutive activation of STAT3. Subsequent experiments revealed that NR4A3 promoter binding by STAT3 might repress its transcription. Long-term depletion of STAT3 derepressed NR4A3 expression, by promoter demethylation, in AGS GC cells. NR4A3 re-expression in GC cell lines sensitized the cells to cisplatin, and inhibited tumor growth in vitro and in vivo, in an animal model. Clinically, GC patients with high NR4A3 methylation, or lower NR4A3 protein expression, had significantly shorter overall survival. Intriguingly, STAT3 activation significantly associated only with NR4A3 methylation in low-stage patient samples. Taken together, aberrant JAK/STAT3 signaling epigenetically silences a potential tumor suppressor, NR4A3, in gastric cancer, plausibly representing a reliable biomarker for gastric cancer prognosis.
虽然异常的 JAK/STAT 信号对胃癌(GC)的发展至关重要,但它对其转录靶标表观遗传改变的影响尚不清楚。在这项研究中,通过表达微阵列结合生物信息学分析,我们鉴定了一个假定的 STAT3 靶基因 NR4A3,与空载体对照(C9)相比,过度表达组成型激活 STAT3 突变体(S16)的 MKN28 GC 子细胞中 NR4A3 下调。亚硫酸氢盐焦磷酸测序和去甲基化处理表明,NR4A3 被 S16 和包括 AGS 细胞在内的其他 GC 细胞系中的启动子 DNA 甲基化表观沉默,显示 STAT3 的组成性激活。随后的实验表明,STAT3 对 NR4A3 启动子的结合可能抑制其转录。AGS GC 细胞中 STAT3 的长期耗竭通过启动子去甲基化使 NR4A3 表达去抑制。NR4A3 在 GC 细胞系中的重新表达使细胞对顺铂敏感,并在体外和体内动物模型中抑制肿瘤生长。临床上,NR4A3 甲基化水平高或 NR4A3 蛋白表达水平低的 GC 患者总生存期明显缩短。有趣的是,STAT3 激活仅与低分期患者样本中的 NR4A3 甲基化显著相关。总之,异常的 JAK/STAT3 信号通过表观遗传沉默胃癌中的潜在肿瘤抑制因子 NR4A3,可能代表一种可靠的胃癌预后生物标志物。
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