Figure 2.
TP-3654 increases the intracellular accumulation of pheophorbide A (PhA) in ABCG2-overexpressing cells. (A) Flow cytometry analysis of PhA accumulation in parental HEK293 cells and ABCG2-transfected R482-HEK293 cells (left panels), parental S1 and ABCG2-overexpressing S1-M1-80 cells (middle panels), and parental H460 and ABCG2-overexpressing H460-MX20 cells (right panels) treated with DMSO (control, solid lines), 1 μM of TP-3654 (filled solid lines), or 1 μM of Ko143 as a positive control (dotted lines) for ABCG2. (B) Effect of increasing concentrations (0–1 μM) of TP-3654 on ABCG2-mediated efflux of PhA (left panel) in ABCG2-overexpressing R482-HEK293 cells (open circles), S1-M1-80 (filled circles), and H460-MX20 cells (open squares), and on ABCB1-mediated efflux of calcein-AM (right panel) in ABCB1-overexpressing MDR19-HEK293 cells (open circles), NCI-ADR-RES (filled circles), and KB-V-1 cells (open squares). Data represent means ± S.D. from at least three independent experiments.