Laboratory of Molecular Gastroenterology and Hepatology, Department of Internal Medicine I, Kiel, Germany.
Oncogenesis. 2012 Nov 26;1(11):e35. doi: 10.1038/oncsis.2012.35.
Pancreatic ductal adenocarcinoma (PDAC) represents one of the deadliest malignancies, with an overall life expectancy of 6 months. Despite considerable advances in the understanding of the molecular mechanisms involved in the carcinogenesis of PDAC, the outcome of the disease was not significantly improved over the last 20 years. Although some achievements in molecular-targeted therapies have been made (that is, targeting the epidermal growth factor receptor by erlotinib), which already entered clinical settings, and despite the promising outcome of the FOLFIRINOX trial, there is an urgent need for improvement of the chemotherapy in this disease. A plethora of molecular alterations are thought to be responsible for the profound chemoresistance, including mutations in oncogenes and tumor suppressors. Besides these classical hallmarks of cancer, the constitutive or inducible activity of transcription factor pathways are characteristic changes in PDAC. Recently, three transcription factors-nuclear factor-κB (NF-κB), nuclear factor of activated T cells (NFAT) and nuclear factor-E2-related factor-2 (Nrf2)-have been shown to be crucial for tumor development and chemoresistance in pancreatic cancer. These transcription factors are key regulators of a variety of genes involved in nearly all aspects of tumorigenesis and resistance against chemotherapeutics and death receptor ligands. Furthermore, the pathways of NF-κB, NFAT and Nrf2 are functional, interacting on several regulatory steps, and, especially, natural compounds such as curcumin interfere with more than one pathway. Thus, targeting these pathways by established inhibitors or new drugs might have great potential to improve the outcome of PDAC patients, most likely in combination with established anticancer drugs. In this article, we summarize recent progress in the characterization of these transcription-factor pathways and their role in PDAC and therapy resistance. We also discuss future concepts for the treatment of PDAC relying on these pathways.
胰腺导管腺癌(PDAC)是最致命的恶性肿瘤之一,总体预期寿命仅为 6 个月。尽管在理解 PDAC 癌变涉及的分子机制方面取得了相当大的进展,但在过去 20 年中,该疾病的预后并未得到显著改善。尽管已经取得了一些分子靶向治疗的成就(即通过厄洛替尼靶向表皮生长因子受体),这些成就已经进入临床应用,并且尽管 FOLFIRINOX 试验的结果很有希望,但仍迫切需要改善该疾病的化疗方法。许多分子改变被认为是导致深度化疗耐药的原因,包括癌基因和肿瘤抑制基因的突变。除了这些癌症的经典特征外,转录因子通路的组成型或诱导性活性是 PDAC 的特征性变化。最近,三种转录因子——核因子-κB(NF-κB)、激活 T 细胞的核因子(NFAT)和核因子-E2 相关因子-2(Nrf2)——已被证明对胰腺癌的肿瘤发展和化疗耐药至关重要。这些转录因子是涉及肿瘤发生和对化疗药物及死亡受体配体耐药性的几乎所有方面的多种基因的关键调节剂。此外,NF-κB、NFAT 和 Nrf2 通路是功能性的,在几个调节步骤上相互作用,特别是天然化合物如姜黄素会干扰不止一种通路。因此,通过已有的抑制剂或新药靶向这些通路可能具有极大的潜力来改善 PDAC 患者的预后,最有可能与现有的抗癌药物联合使用。在本文中,我们总结了这些转录因子通路的特征及其在 PDAC 和治疗耐药性中的作用的最新进展。我们还讨论了基于这些通路治疗 PDAC 的未来概念。