Collectively, our data showed that ART potentiated ADR cytotoxicity by inhibiting glycolysis and downregulating mdr1 and abcg2 gene expression in ADR-resistant K562 cells, indicating the values of ART and ADR combined therapy in reducing drug resistance in leukemia and further elucidating the crucial roles of glycolysis in drug resistance. Here, ABCB1 is linked to leukemia.