非基因组β雌激素受体增强尼古丁衍生致癌物4-(甲基亚硝胺基)-1-(3-吡啶基)-1-丁酮在人小气道上皮细胞中诱导的β1肾上腺素能信号传导。
Nongenomic beta estrogen receptors enhance beta1 adrenergic signaling induced by the nicotine-derived carcinogen 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone in human small airway epithelial cells.
作者信息
Majidi Mourad, Al-Wadei Hussein A, Takahashi Takashi, Schuller Hildegard M
机构信息
Experimental Oncology Laboratory, Department of Pathobiology, College of Veterinary Medicine, University of Tennessee, 2407 River Drive, Knoxville, TN 37996, USA.
出版信息
Cancer Res. 2007 Jul 15;67(14):6863-71. doi: 10.1158/0008-5472.CAN-07-0483.
Women are at higher risk for the development of lung adenocarcinoma than men; however, the mechanisms responsible for this are poorly understood. In lung adenocarcinoma cells, the estrogen receptor beta (ERbeta) is the predominating form. We found that 17beta-estradiol enhanced proliferation of the putative cells of origin of lung adenocarcinoma, small airway epithelial cells (HPLD1), in response to the nicotine-derived nitrosamine 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK). Reverse-phase protein microarrays combined with Western blotting revealed that NNK induced phosphorylation of ERbeta, an effect that involved stimulation of the adrenergic receptors beta1 (beta1AR). In transiently transfected cells, beta1AR coprecipitated with ERbeta, which increased with NNK treatment. ERbeta enhanced NNK-induced cyclic AMP accumulation as well as Galphai-mediated mitogen-activated protein kinase/extracellular signal-regulated kinase (ERK) 1/2 activation. Coexpression of beta1AR and ERbeta activated NNK-mediated ERK1/2 cooperatively. ERbeta gene knockdown, as well as coexpression of the dominant negative Ras and Raf, reduced stimulation of ERK1/2 by NNK. Whereas NNK phosphorylated Akt at Thr(308) and Ser(473), ERbeta had no effect on this activity. Luciferase reporter assays showed that, in response to NNK, ERbeta stimulated transcription of serum responsive element (SRE) but had a very small effect on the activity of estrogen responsive element (ERE). Together, the phosphorylation of ERbeta, the dependence on Galphai proteins, the activation of ERK1/2, and the preferential targeting of SRE over the classic ERE pathway support a role for nongenomic ERbeta in the development of smoking-associated lung cancer. This novel cooperation between beta1AR and ERbeta signaling may contribute to the prominence of lung adenocarcinoma in women.
女性患肺腺癌的风险高于男性;然而,其背后的机制却知之甚少。在肺腺癌细胞中,雌激素受体β(ERβ)是主要形式。我们发现,17β-雌二醇可增强肺腺癌假定起源细胞——小气道上皮细胞(HPLD1)对尼古丁衍生的亚硝胺4-(甲基亚硝胺基)-1-(3-吡啶基)-1-丁酮(NNK)的增殖反应。反相蛋白质微阵列结合蛋白质免疫印迹法显示,NNK可诱导ERβ磷酸化,这一效应涉及对肾上腺素能受体β1(β1AR)的刺激。在瞬时转染细胞中,β1AR与ERβ共沉淀,且随着NNK处理而增加。ERβ增强了NNK诱导的环磷酸腺苷积累以及Gαi介导的丝裂原活化蛋白激酶/细胞外信号调节激酶(ERK)1/2激活。β1AR和ERβ的共表达协同激活了NNK介导的ERK1/2。ERβ基因敲低以及显性负性Ras和Raf的共表达降低了NNK对ERK1/2的刺激。虽然NNK使Akt在苏氨酸(Thr)308和丝氨酸(Ser)473位点磷酸化,但ERβ对此活性没有影响。荧光素酶报告基因检测表明,在NNK作用下,ERβ刺激血清反应元件(SRE)的转录,但对雌激素反应元件(ERE)的活性影响很小。总之,ERβ的磷酸化、对Gαi蛋白的依赖性、ERK1/2的激活以及SRE相对于经典ERE途径的优先靶向作用支持了非基因组ERβ在吸烟相关肺癌发生中的作用。β1AR和ERβ信号之间这种新的协同作用可能导致了女性肺腺癌的高发。