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Dynamic vs Static ABCG2 Inhibitors to Sensitize Drug Resistant Cancer Cells

Figure 5

Effect of PZ-34 and PZ-38 on sensitizing drug resistance.

A, potency of PZ-34 and PZ-38 in reversing mitoxantrone resistance. HEK293/ABCG2 cells were treated without or with 0.1 µM (IC10) mitoxantrone in the absence or presence of different concentrations of PZ-34 or PZ-38 followed by SRB assay. B, sensitization index of PZ-34 and PZ-38 in HEK293/ABCG2 cells. HEK293/ABCG2 cells were treated with various concentrations of mitoxantrone in the absence or presence of different concentrations of PZ-34 or PZ-38 followed by SRB assay. C and D, sensitization index of PZ-34 and PZ-38 in drug-selected MCF7/AdVp3000 cells. MCF7/AdVp3000 cells were treated with various concentrations of mitoxantrone (C), or Adriamycin (D) in the presence of DMSO (vehicle) or 500 nM of PZ-34 and PZ-38 followed by MTT assay. Sensitization index was calculated using IC50 of the anticancer drugs in the absence or presence of PZ-34, PZ-38, or FTC. The data shown are mean ± SD of three independent experiments.

Figure 5

doi: https://doi.org/10.1371/journal.pone.0015276.g005