Previous studies have shown that BLU-258 at non-toxic concentrations can impair the function of the ATP-binding transporters (ABC) ABCB1 and ABCG2 in vitro and restore chemosensitivity in multidrug-resistant cancer cells overexpressing ABCB1 and ABCG2 [14,17]. The gene discussed is ABCB1; the disease is cancer.