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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

Effects and molecular mechanism of 5,8-disubstituted quinazolines-LJK-11 in HER2 overexpressing cells

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【作者】 秦莉莉金毅龙亚秋俞强何建勇

【Author】 QIN Li-li~1,JIN Yi~2,LONG Ya-qiu~2,YU Qiang~2,HE Jian-yong~1(1.School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China;2.Shanghai Institute of Medicine Research,Chinese Academic of Science,Shanghai 201203,China)

【机构】 沈阳药科大学制药工程学院中国科学院上海药物所沈阳药科大学制药工程学院 辽宁沈阳110016上海201203辽宁沈阳110016

【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。

【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.

【关键词】 LJK-11酪氨酸激酶抑制剂肿瘤HER2细胞死亡
【Key words】 LJK-11tyrosine kinase inhibitortumorHER2cell death
  • 【文献出处】 沈阳药科大学学报 ,Journal of Shenyang Pharmaceutical University , 编辑部邮箱 ,2007年01期
  • 【分类号】R730.5
  • 【被引频次】2
  • 【下载频次】187
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