临床肿瘤学杂志
臨床腫瘤學雜誌
림상종류학잡지
CHINESE CLINICAL ONCOLOGY
2015年
8期
755-759
,共5页
刘思文(综述)%冯继锋(审校)
劉思文(綜述)%馮繼鋒(審校)
류사문(종술)%풍계봉(심교)
肺癌%表皮生长因子受体-酪氨酸激酶抑制剂%耐药%肝X受体激动剂%逆转耐药
肺癌%錶皮生長因子受體-酪氨痠激酶抑製劑%耐藥%肝X受體激動劑%逆轉耐藥
폐암%표피생장인자수체-락안산격매억제제%내약%간X수체격동제%역전내약
Lung cancer%Epidermal growth factor receptor tyrosine kinase inhibitor( EGFR-TKI)%Drug resistance%Liver X receptor agonist%Reversing resistance
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。
錶皮生長因子受體?酪氨痠激酶抑製劑( EGFR?TKI)是目前應用最廣汎的肺癌靶嚮藥物,但幾乎所有治療有效的患者最終都會對EGFR?TKI產生繼髮耐藥,耐藥機製主要為EGFR下遊通路被再度激活。肝X受體( LXR)屬于覈受體傢族,多項研究錶明LXR激動劑對EGFR最重要的下遊通路PI3K/AKT/NF?κB多箇主要環節均有不同程度的抑製作用。因此, LXR激動劑可能是逆轉EGFR?TKI繼髮耐藥的新選擇。本文主要對近年來LXR激動劑對PI3K/AKT/NF?κB通路的抑製作用進行綜述。
표피생장인자수체?락안산격매억제제( EGFR?TKI)시목전응용최엄범적폐암파향약물,단궤호소유치료유효적환자최종도회대EGFR?TKI산생계발내약,내약궤제주요위EGFR하유통로피재도격활。간X수체( LXR)속우핵수체가족,다항연구표명LXR격동제대EGFR최중요적하유통로PI3K/AKT/NF?κB다개주요배절균유불동정도적억제작용。인차, LXR격동제가능시역전EGFR?TKI계발내약적신선택。본문주요대근년래LXR격동제대PI3K/AKT/NF?κB통로적억제작용진행종술。
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 EG?FR?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 resist?ance of EGFR?TKI. This paper summarizes the recent findings about the inhibitory effects of LXR agonists on PI3K/AKT/NF?κB path?way.