ATP-binding cassette efflux transporters and MDR in cancer

Abstract

Of the many known multidrug resistance (MDR) mechanisms, ATP-binding cassette (ABC) transporters expelling drug molecules out of cells is a major factor limiting the efficacy of present-day anticancer drugs. In this review, we highlights updated information on the structure, function, and regulatory mechanisms of major MDR-related ABC transporters, such as P-glycoprotein (P-gp), multidrug resistance protein 1 (MRP1), and breast cancer resistance protein (BCRP), and the effect of modulators on their functions. We also provide focused information on different modulators of ABC transporters that could be utilized against the emerging MDR crisis in cancer treatment. Finally, we discuss the importance of ABC transporters as therapeutic targets in light of future strategic planning for translating ABC transporter inhibitors into clinical practice.