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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 被引量:2

Effects and molecular mechanism of 5,8-disubstituted quinazolines-LJK-11 in HER2 overexpressing cells
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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。 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.
出处 《沈阳药科大学学报》 CAS CSCD 北大核心 2007年第1期53-56,60,共5页 Journal of Shenyang Pharmaceutical University
关键词 LJK-11 酪氨酸激酶抑制剂 肿瘤 HER2 细胞死亡 LJK-11 tyrosine kinase inhibitor tumor HER2 cell death
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