TABLE 2

IC50 values for rhodamine123 efflux inhibition by verapamil, vinblastine, and propafenone analogs

IC50 values were calculated from concentration response curves (shown in Figs 4–7). Results are represented as mean ± S.D. of at least three individual experiments performed in duplicate.

MutationIC50
VerapamilVinblastineGPV31GPV366
μM
Wild-type P-gp0.43 ± 0.102.68 ± 0.930.11 ± 0.062.60 ± 0.69
Q132A0.30 ± 0.072.58 ± 0.310.10 ± 0.032.57 ± 0.69
Q773A0.42 ± 0.152.80 ± 0.120.11 ± 0.052.40 ± 1.47
Q132A/Q773A0.44 ± 0.162.24 ± 0.430.12 ± 0.012.87 ± 0.63
Q132R1.24 ± 0.13*9.19 ± 1.20*0.71 ± 0.46*2.64 ± 0.59
Q773R0.14 ± 0.04*0.45 ± 0.16*0.02 ± 0.01*2.09 ± 0.90
  • * P < 0.05, significantly different from wild-type values.