Henriquet Corinne, Gougat Claire, Combes Audrey, Lazennec Gwendal, Mathieu Marc
Institut National de la Santé et de la Recherche Médicale U454-IFR3, 34295 Montpellier cedex 5, France.
Lung Cancer. 2007 May;56(2):167-74. doi: 10.1016/j.lungcan.2006.12.003. Epub 2007 Jan 17.
In lung adenocarcinoma, expression of Regulated upon Activation, Normal T cell Expressed and presumably Secreted (RANTES) is a predictor of survival while that of interleukin (IL)-8 is associated with a poor prognosis. In several models, tumorigenesis is abolished by RANTES, while it is facilitated by IL-8. We studied the regulation of RANTES and IL-8 expression in A549 lung adenocarcinoma cells. The effects of tumor necrosis factor (TNF)-alpha and regulators of protein kinases C (PKC)alpha/beta were tested because these have been shown to modulate cancer development and progression. TNF-alpha stimulated expression of both chemokines, while the PKCalpha/beta activator 12-O-tetradecanoyl-phorbol-13-acetate (TPA) induced only expression of IL-8 and inhibited TNF-alpha-induced RANTES expression. The PKCalpha/beta inhibitor Gö 6976 increased TNF-alpha-induced RANTES production and prevented its down-regulation by TPA. In contrast, it decreased TNF-alpha or TPA-induced IL-8 release. The differential regulation of RANTES and IL-8 expression was further analyzed. Site-directed mutagenesis indicated that regulation of RANTES promoter activity required two nuclear factor (NF)-kappaB response elements but not its activator protein (AP)-1 binding sites. An AP-1 and a NF-kappaB recognition sites were necessary for full induction of IL-8 promoter activity by TNF-alpha and TPA. Moreover, electrophoretic mobility shift assays demonstrated that NF-kappaB response elements from the RANTES promoter were of lower affinity than that from the IL-8 promoter. Immunoblotting experiments showed that TPA was more potent than TNF-alpha to induce in a PKCalpha/beta dependent manner the p44/p42 mitogen-activated protein kinases (MAPK) signaling cascade which controls AP-1 activity. Conversely, TPA inhibited TNF-alpha-induced NF-kappaB signaling and was a weak activator of this pathway. Thus, TPA did not sufficiently activate NF-kappaB to increase transcription through the low affinity NF-kappaB binding sites on RANTES promoter and its inhibitory effect on TNF-alpha-induced NF-kappaB signaling resulted in a reduced transcription rate. On IL-8 promoter, increased transcription through the high affinity NF-kappaB binding site occurred even with poorly activated NF-kappaB and the functional AP-1 response element compensated any loss of transcription rate. These data provide a mechanistic insight into the differential regulation of IL-8 and RANTES expression by PKCalpha/beta in lung adenocarcinoma cells.
在肺腺癌中,受激活调节的正常T细胞表达和可能分泌的因子(RANTES)的表达是生存的一个预测指标,而白细胞介素(IL)-8的表达则与预后不良相关。在几种模型中,RANTES可消除肿瘤发生,而IL-8则促进肿瘤发生。我们研究了A549肺腺癌细胞中RANTES和IL-8表达的调控。测试了肿瘤坏死因子(TNF)-α和蛋白激酶C(PKC)α/β调节剂的作用,因为这些已被证明可调节癌症的发展和进展。TNF-α刺激了两种趋化因子的表达,而PKCα/β激活剂12-O-十四烷酰佛波醇-13-乙酸酯(TPA)仅诱导IL-8的表达并抑制TNF-α诱导的RANTES表达。PKCα/β抑制剂Gö 6976增加了TNF-α诱导的RANTES产生,并阻止了TPA对其的下调。相反,它降低了TNF-α或TPA诱导的IL-8释放。进一步分析了RANTES和IL-8表达的差异调节。定点诱变表明,RANTES启动子活性的调节需要两个核因子(NF)-κB反应元件,而不需要其激活蛋白(AP)-1结合位点。一个AP-1和一个NF-κB识别位点对于TNF-α和TPA完全诱导IL-8启动子活性是必需的。此外,电泳迁移率变动分析表明,RANTES启动子的NF-κB反应元件的亲和力低于IL-8启动子的。免疫印迹实验表明,TPA比TNF-α更有效地以PKCα/β依赖性方式诱导控制AP-1活性的p44/p42丝裂原活化蛋白激酶(MAPK)信号级联反应。相反,TPA抑制TNF-α诱导的NF-κB信号传导,并且是该途径的弱激活剂。因此,TPA没有充分激活NF-κB以通过RANTES启动子上的低亲和力NF-κB结合位点增加转录,并且其对TNF-α诱导的NF-κB信号传导的抑制作用导致转录速率降低。在IL-8启动子上,即使NF-κB激活不良,通过高亲和力NF-κB结合位点的转录增加,并且功能性AP-1反应元件补偿了转录速率的任何损失。这些数据为PKCα/β在肺腺癌细胞中对IL-