Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade

Cancer Lett. 2016 Jan 1;370(1):153-64. doi: 10.1016/j.canlet.2015.10.010. Epub 2015 Oct 20.


Multidrug resistance (MDR) is a serious phenomenon employed by cancer cells which hampers the success of cancer pharmacotherapy. One of the common mechanisms of MDR is the overexpression of ATP-binding cassette (ABC) efflux transporters in cancer cells such as P-glycoprotein (P-gp/ABCB1), multidrug resistance-associated protein 2 (MRP2/ABCC2), and breast cancer resistance protein (BCRP/ABCG2) that limits the prolonged and effective use of chemotherapeutic drugs. Researchers have found that developing inhibitors of ABC efflux transporters as chemosensitizers could overcome MDR. But the clinical trials have shown that most of these chemosensitizers are merely toxic and only show limited or no benefits to cancer patients, thus new inhibitors are being explored. Recent findings also suggest that efflux pumps of the ABC transporter family are subject to epigenetic gene regulation. In this review, we summarize recent findings of the role of ABC efflux transporters in MDR.

Keywords: ABC transporters; Cancer therapy; Inhibitors; Multidrug resistance.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / antagonists & inhibitors
  • ATP-Binding Cassette Transporters / chemistry
  • ATP-Binding Cassette Transporters / physiology*
  • Animals
  • Drug Resistance, Multiple*
  • Drug Resistance, Neoplasm
  • Epigenesis, Genetic
  • Humans
  • Multidrug Resistance-Associated Protein 2


  • ABCC2 protein, human
  • ATP-Binding Cassette Transporters
  • Multidrug Resistance-Associated Protein 2