伊马替尼
细胞内
主旨
流出
药理学
间质瘤
运输机
Abcg2型
间质细胞
化学
细胞培养
癌症研究
生物
ATP结合盒运输机
生物化学
基因
遗传学
髓系白血病
作者
Qiang Zhang,Zheng Li,Kangjing Xu,Yi Qian,Ming Chen,Liang Sun,Shanshan Song,Xiaoxu Huang,Zhongyuan He,Fengyuan Li,Diancai Zhang,Li Yang,Yongqing Wang,Hao Xu,Zekuan Xu
标识
DOI:10.1080/00365521.2019.1577488
摘要
We aimed to investigate the role of intracellular imatinib concentration in drug resistance and the expression of candidate drug transporters in gastrointestinal stromal tumor (GIST) cell lines.The imatinib concentrations were measured by the liquid chromatography-tandem mass spectrometry (LC-MS/MS). The expression of candida te drug transporters was detected by qRT-PCR.The tissue imatinib concentrations in imatinib resistant patients were significantly lower than that of sensitive patients (p < .05). Compared with parental cell lines, the intracellular imatinib concentration was notably lower in imatinib resistant GIST cell lines. For candidate transporters, MRP1 and BCRP were overexpressed in resistant GIST cell lines.The intracellular imatinib concentration may play a crucial role in imatinib resistance and the intracellular differences of imatinib concentration may be induced by the upregulation of efflux transporters. Our study highlights the importance of intracellular imatinib concentration and the potential of using imatinib transporters as therapeutic targets for patients with GIST.
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