临床肿瘤学杂志

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肝X受体激动剂对EGFR下游通路的抑制作用

刘思文,冯继锋   

  1. 南京医科大学附属江苏省肿瘤医院肿瘤内科
  • 收稿日期:2014-08-14 修回日期:2015-03-05 出版日期:2015-08-31 发布日期:2015-08-31
  • 通讯作者: 冯继锋

The inhibitory effects of the liver X receptor agonists on the EGFR associated signal pathway

LIU Siwen, FENG Jifeng.   

  1. Department of Medical Oncology,Affiliated Jiangsu Province Tumor Hospital of Nanjing Medical University
  • Received:2014-08-14 Revised:2015-03-05 Online:2015-08-31 Published:2015-08-31
  • Contact: FENG Jifeng

摘要: 表皮生长因子受体-酪氨酸激酶抑制剂(EGFR-TKI)是目前应用最广泛的肺癌靶向药物,但几乎所有治疗有效的患者最终都会对 EGFR-TKI产生继发耐药,耐药机制主要为EGFR下游通路被再度激活。肝X受体(LXR)属于核受体家族,多项研究表明LXR激动剂对EGFR最重要的下游通路PI3K/AKT/NF-κB多个主要环节均有不同程度的抑制作用。因此,LXR激动剂可能是逆转EGFR-TKI继发耐药的新选择。本文主要对近年来LXR激动剂对PI3K/AKT/NF-κB通路的抑制作用进行综述。

Abstract: Epidermal growth factor receptor tyrosine kinase inhibitor(EGFR-TKI) is the most widely used drug in the targeted treatment of lung cancer. However, almost all patients who are effective to this drug will eventually develop secondary resistance to EGFR-TKI. The main mechanism of resistance is that the EGFR associated signal pathway was again activated. The liver X receptor(LXR) belongs to the family of nuclear receptor. Many studies showed the inhibitory effects of LXR agonists on the signal pathway of PI3K/AKT/NF-κB that are important to EGFR. Therefore, LXR agonists may be a potential new choice that can reverse the secondary resistance of EGFR-TKI. This paper summarizes the recent findings about the inhibitory effects of LXR agonists on PI3K/AKT/NF-κB pathway.

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