ATP-binding cassette efflux transporters and MDR in cancer

Of the many multidrug resistance (MDR) mechanisms, the ATP binding cassette (ABC) transporters expelling drug molecules out of cells is a major culprit in limiting the efficacy of present-day anticancer drugs. The present review offers an updated infor-mation on structure, function, and regulatory mechanisms of major MDR related ABC transporters such as P-glycoprotein, MRP1, BCRP and effect of modulators on their functions. An attempt has been made to provide a focused information on different modulators of ABC transporters so as utilize them in clinical practice for amelioration of emerging MDR crisis in cancer treatment. Finally, the importance ABC transporters as therapeutic targets has been discussed in the light of future strategic planning for translating the ABC transporter inhibitors in clinical practice.

Automated summary

This review provides updated information on the structure, function, and regulatory mechanisms of major multidrug resistance (MDR) related ATP binding cassette (ABC) transporters, which play a significant role in limiting the efficacy of anticancer drugs. The effects of modulators on the functions of ABC transporters such as P-glycoprotein, MRP1, and BCRP are discussed. Additionally, the potential use of these ABC transporter modulators in clinical practice to alleviate the emerging MDR crisis in cancer treatment is highlighted.