Overall, the results indicated that ART enhanced ADR cytotoxicity by inhibiting glycolysis and reducing mdr1 and abcg2 gene expression in K562/ADR cells, providing a deep insight into the function and molecular basis of ART in regulating MDR in leukemia cells and hinting at the potential values of ART in alleviating MDR in cancers. Here, ABCB1 is linked to leukemia.