Apoptozole Modulates ABCG2-Mediated Multidrug Resistance in Lung Cancer

Lung cancer is a widespread malignant tumor with a highmortality rate, often difficult to treat effectively due to chemoresistance. Given the close association between ABCG2 overexpression and cancer multidrug resistance, overcoming the issue of MDR caused by ABCG2 is still a challenge. In this study, we found that the small molecule apoptozole effectively suppresses the transport activity of ABCG2, thus mitigating multidrug resistance in lung cancer cells, overexpressing ABCG2, and improving the therapeutic effects of chemotherapy drugs mitoxantrone and topotecan. Additionally, apoptozole does not affect the expression level of ABCG2 protein. Molecular docking studies have demonstrated that apoptozole can firmly bind to the binding pocket of ABCG2. Our data present that apoptozole is an ABCG2 inhibitor and modulates ABCG2-mediated multidrug resistance in lung cancer.