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Fig. 1 | Journal of Hematology & Oncology

Fig. 1

From: In vitro and in vivo identification of ABCB1 as an efflux transporter of bosutinib

Fig. 1

Evaluation of drug-transporter expression and functionality. a Evaluation of ABCB1, SLC22A1, and ABCG2 drug-transporter expression by real-time qPCR (RT-qPCR). Housekeeping GAPDH was used for intra-sample normalization. For each transporter, expression levels were normalized over the expression levels in K562S. Results are the average of three independent experiments ± SD. The statistical differences between expression levels of overexpressing or silenced cells and K562S cells were calculated with two-tailed unpaired student’s t-test, and a p value of 0.05 was chosen as the limit of statistical significance (** = p < 0.05 *** = p < 0.01). b Evaluation of drug-transporter expression levels by immunoblotting performed on whole cell lysate of overexpressing, silenced, and K562S cell lines. Specific antibodies were used for each drug transporter. Actin was used as a loading control. c Intracellular incorporation of known fluorescent substrates was evaluated by FACS analysis. On the left panel, rhodamine 123 incorporation for ABCB1 activity analysis, in the middle panel, 4-Di-2-ASP for SLC22A1 analysis, and in the right panel, pheophorbide A for ABCG2 analysis. In each graph, the shaded area corresponds to the overexpressing cell line, the solid line to the silenced cell line, the dotted line to the overexpressing cell lines pre-treated with drug-transporter inhibitor, and shortly dashed line to K562S

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