多药耐药蛋白2
Abcg2型
安普列那韦
流出
免疫印迹
细胞培养
ATP结合盒运输机
化学
运输机
碳酸钙-2
P-糖蛋白
分子生物学
拓扑替康
药理学
细胞
生物
生物化学
内科学
多重耐药
医学
酶
遗传学
蛋白酶
化疗
HIV-1蛋白酶
基因
抗生素
作者
Laurent Salphati,Emile G. Plise,Guangmin Li
标识
DOI:10.1016/j.ejps.2009.04.001
摘要
The human colorectal carcinoma cell line LS513 exhibits epithelial morphology, adherent properties and can grow subcutaneously to form tumors in nude mice. Thus, it is a potential model for mouse xenograft efficacy studies. The present study characterized the expression and activity of P-gp, BCRP and MRP2 in LS513 cells. We investigated the expression of these ATP-binding cassette transporters by Western blot and their activity was also examined using cell culture inserts, where the LS513 cells were grown to confluence for 9 days. The transport of model substrates of P-gp (amprenavir, ritonavir and topotecan), BCRP (topotecan) and MRP2 (SN-38) was studied in the apical to basolateral (A-B) and basolateral to apical (B-A) directions. P-gp, BCRP and MRP2 could be detected by western blot. The LS513 cells exhibited markedly higher transport in the B-A direction than in the A-B direction for the probe substrates tested, with efflux ratios (ERs; B-A/A-B) of 10, 21, 40 and 50 for amprenavir, ritonavir, topotecan and SN38, respectively. The ER could be significantly reduced with the addition of inhibitors of P-gp (GF120918), BCRP (FTC), and MRP2 (MK571), confirming the activity of these transporters in the LS513 cells.
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