Department of Pharmacology and Experimental Therapeutics, Thomas Jefferson University, Philadelphia, Pennsylvania, USA.
Clin Transl Sci. 2009 Aug;2(4):286-93. doi: 10.1111/j.1752-8062.2009.00131.x.
While bile acids are a risk factor for tumorigenesis induced by reflux disease, the mechanisms by which they contribute to neoplasia remain undefined. Here, we reveal that in gastroesophageal junction (GEJ) cells bile acids activate a tissue-specific developmental program defining the intestinal epithelial cell phenotype characterizing GEJ metaplasia. Deoxycholic acid (DCA) inhibited phosphorylation of EGF receptors (EGFRs) suppressing the proto-oncogene AKT. Suppression of EGFRs and AKT by DCA actuated an intestine-specific cascade in which NF-kappaB transactivated the tissue-specific transcription factor CDX2. In turn, CDX2 orchestrated a lineage-specific differentiation program encompassing genes characterizing intestinal epithelial cells. Conversely, progression from metaplasia to invasive carcinoma in patients, universally associated with autonomous activation of EGFRs and/or AKT, was coupled with loss of this intestinal program. Thus, bile acids induce intestinal metaplasia at the GEJ by activating the lineage-specific differentiation program involving suppression of EGFR and AKT, activating the NF-kappaB-CDX2 axis. Induction of this axis provides the context for lineage-addicted tumorigenesis, in which autonomous activation of AKT corrupts adaptive intestinal NF-kappaB signaling, amplifying tumorigenic programs.
虽然胆汁酸是反流性疾病引起肿瘤发生的一个风险因素,但它们促进肿瘤发生的机制尚不清楚。在这里,我们揭示了胆汁酸在胃食管交界处(GEJ)细胞中激活了一个组织特异性的发育程序,定义了具有特征性的 GEJ 化生的肠上皮细胞表型。脱氧胆酸(DCA)抑制表皮生长因子受体(EGFRs)的磷酸化,从而抑制原癌基因 AKT。DCA 对 EGFRs 和 AKT 的抑制作用引发了一个肠道特异性级联反应,其中 NF-κB 转激活组织特异性转录因子 CDX2。反过来,CDX2 协调了一个包含肠上皮细胞特征基因的谱系特异性分化程序。相反,在普遍与 EGFRs 和/或 AKT 的自主激活相关的患者中,从化生到侵袭性癌的进展伴随着这种肠程序的丧失。因此,胆汁酸通过激活涉及 EGFR 和 AKT 抑制、激活 NF-κB-CDX2 轴的谱系特异性分化程序,在 GEJ 诱导肠化生。该轴的诱导为谱系依赖的肿瘤发生提供了背景,其中 AKT 的自主激活使适应性的肠 NF-κB 信号发生腐败,放大了肿瘤发生程序。