Madson Justin G, Lynch David T, Svoboda Jessica, Ophardt Rebecca, Yanagida Jodi, Putta Sumanth K, Bowles Andrew, Trempus Carol S, Tennant Raymond W, Hansen Laura A
Department of Biomedical Sciences, School of Medicine, Creighton University, 2500 California Plaza, Omaha, NE 68178, USA.
Am J Pathol. 2009 Jun;174(6):2357-66. doi: 10.2353/ajpath.2009.080638. Epub 2009 Apr 30.
The Erbb2 receptor is activated by UV irradiation, the primary cause of non-melanoma skin cancer. We hypothesized that Erbb2 activation contributes to UV-induced skin tumorigenesis by suppressing cell cycle arrest. Consistent with this hypothesis, inhibition of Erbb2 in v-ras(Ha) transgenic mice before UV exposure resulted in both 56% fewer skin tumors and tumors that were 70% smaller. Inhibition of the UV-induced activation of Erbb2 also resulted in milder epidermal hyperplasia, S-phase accumulation, and decreased levels of the cell cycle regulator Cdc25a, suggesting altered cell cycle regulation on inhibition of Erbb2. Further investigation using inhibition or genetic deletion of Erbb2 in vitro revealed reduced Cdc25a levels and increased S-phase arrest in UV-irradiated cells lacking Erbb2 activity. Ectopic expression of Cdc25a prevented UV-induced S-phase arrest in keratinocytes lacking Erbb2 activity, demonstrating that maintenance of Cdc25a by Erbb2 suppresses cell cycle arrest. Examination of checkpoint pathway activation upstream of Cdc25a revealed Erbb2 activation did not alter Ataxia Telangiectasia and Rad3-related/Ataxia Telangiectasia Mutated activity but increased inhibitory phosphorylation of Chk1-Ser(280). Since Akt phosphorylates Chk1-Ser(280), the effect of Erbb2 on phosphatidyl inositol-3-kinase (PI3K)/Akt signaling during UV-induced cell cycle arrest was determined. Erbb2 ablation reduced the UV-induced activation of PI3K while inhibition of PI3K/Akt increased UV-induced S-phase arrest. Thus, UV-induced Erbb2 activation increases skin tumorigenesis through inhibitory phosphorylation of Chk1, Cdc25a maintenance, and suppression of S-phase arrest via a PI3K/Akt-dependent mechanism.
Erbb2受体可被紫外线照射激活,而紫外线照射是非黑色素瘤皮肤癌的主要病因。我们推测,Erbb2激活通过抑制细胞周期停滞促进紫外线诱导的皮肤肿瘤发生。与这一假设相符的是,在紫外线暴露前抑制v-ras(Ha)转基因小鼠中的Erbb2,可使皮肤肿瘤数量减少56%,且肿瘤大小缩小70%。抑制紫外线诱导的Erbb2激活还会导致较轻的表皮增生、S期积累以及细胞周期调节因子Cdc25a水平降低,这表明抑制Erbb2会改变细胞周期调节。进一步在体外使用Erbb2抑制剂或基因敲除进行研究发现,在缺乏Erbb2活性的紫外线照射细胞中,Cdc25a水平降低,S期停滞增加。在缺乏Erbb2活性的角质形成细胞中异位表达Cdc25a可阻止紫外线诱导的S期停滞,这表明Erbb2维持Cdc25a可抑制细胞周期停滞。对Cdc25a上游检查点通路激活的检测显示,Erbb2激活并未改变共济失调毛细血管扩张症和Rad3相关蛋白/共济失调毛细血管扩张症突变蛋白的活性,但增加了Chk1-Ser(280)的抑制性磷酸化。由于Akt可磷酸化Chk1-Ser(280),因此确定了Erbb2在紫外线诱导的细胞周期停滞过程中对磷脂酰肌醇-3-激酶(PI3K)/Akt信号传导的影响。敲除Erbb2可降低紫外线诱导的PI3K激活,而抑制PI3K/Akt则会增加紫外线诱导的S期停滞。因此,紫外线诱导的Erbb2激活通过Chk1的抑制性磷酸化、Cdc25a的维持以及通过PI3K/Akt依赖性机制抑制S期停滞来增加皮肤肿瘤发生。