How to overcome ATP-binding cassette drug efflux transporter-mediated drug resistance?

Adrian C. Jaramillo, Farah Al Saig, Jacqueline Cloos, Gerrit Jansen, Godefridus J. Peters

Research output: Contribution to journalReview articleAcademicpeer-review

69 Citations (Scopus)


P-glycoprotein (ABCB1), multidrug resistance protein-1 (ABCC1) and breast cancer resistance protein (ABCG2) belong to the ATP-binding cassette (ABC) superfamily of proteins that play an important physiological role in protection of the body from toxic xenobiotics and endogenous metabolites. Beyond this, these transporters determine the toxicity profile of many drugs, and confer multidrug resistance (MDR) in cancer cells associated with a poor treatment outcome of cancer patients. It has long been hypothesized that inhibition of ABC drug efflux transporters will increase drug accumulation and thereby overcome MDR, but until now no approved inhibitor of these transporters is available in the clinic. In this review we present molecular strategies to overcome this type of drug resistance and discuss for each of these strategies their promising value or indicate underlying reasons for their limited success.

Original languageEnglish
Pages (from-to)6-29
Number of pages24
JournalCancer Drug Resistance
Issue number1
Publication statusPublished - 2018


  • ATP-binding cassette transporters
  • Breast cancer resistance protein
  • Multidrug resistance
  • Multidrug resistance protein

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