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5,8-二取代喹唑啉类化合物LJK-11对HER2高表达肿瘤细胞的作用和分子机制初探
引用本文:秦莉莉,金毅,龙亚秋,俞强,何建勇. 5,8-二取代喹唑啉类化合物LJK-11对HER2高表达肿瘤细胞的作用和分子机制初探[J]. 沈阳药科大学学报, 2007, 24(1)
作者姓名:秦莉莉  金毅  龙亚秋  俞强  何建勇
作者单位:1. 沈阳药科大学,制药工程学院,辽宁,沈阳,110016
2. 中国科学院,上海药物所,上海,201203
摘    要:目的观察LJK-11对HER2高表达细胞的作用。方法检测LJK-11对不同肿瘤细胞作用的剂量效应;用Western blot检测药物引起的细胞内酪氨酸激酶信号表达变化。结果随着药物浓度的增加,LJK-11对肿瘤细胞的增殖抑制作用逐渐明显,并能够引起肿瘤细胞的凋亡;Western blot检测显示受体酪氨酸激酶HER2磷酸化表达降低。结论LJK-11可能是一种新型的酪氨酸激酶抑制剂,这一作用机制将为研制出新型的抗肿瘤药提供理论依据。

关 键 词:LJK-11  酪氨酸激酶抑制剂  肿瘤  HER2  细胞死亡

Effects and molecular mechanism of 5, 8-disubstituted quinazolines-LJK-11 in HER2 overexpressing cells
QIN Li-li,JIN Yi,LONG Ya-qiu,YU Qiang,HE Jian-yong. Effects and molecular mechanism of 5, 8-disubstituted quinazolines-LJK-11 in HER2 overexpressing cells[J]. Journal of Shenyang Pharmaceutical University, 2007, 24(1)
Authors:QIN Li-li  JIN Yi  LONG Ya-qiu  YU Qiang  HE Jian-yong
Abstract:Objective To investigate the effects and molecular mechanism of LJK-11 on tumor cell.Methods The growth inhibition effects of LJK-11 on different tumor cell were measured by MTT assay.The effects on the expression and phosphorylation of HER2 were analyzed by western blot analysis.Results LJK-11 inhibited tumor cell growth in concentration-dependent manner.LJK-11 inhibited the phosphorylation of HER2.Conclusions LJK-11 may be developed as a novel kinase inhibitor.The inhibitory mechanism of LJK-11 provides a theoretical guidance for the development of novel anti-cancer agents.
Keywords:LJK-11  HER2
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