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Updated: Feb 12, 2026

Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein
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Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein

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Revisiting the role of ABC transporters in multidrug-resistant cancer

Robert W Robey1, Kristen M Pluchino1, Matthew D Hall2

  • 1Laboratory of Cell Biology, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA.

Nature Reviews. Cancer
|April 13, 2018
PubMed

Insights

Investigating ATP-binding cassette (ABC) transporters, like multidrug resistance protein 1 (MDR1), is crucial for overcoming cancer drug resistance. New evidence suggests revisiting these transporters for improved cancer therapy and drug delivery, especially at the blood-brain barrier.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Multidrug resistance (MDR) in cancer, often due to ATP-binding cassette (ABC) transporters, limits therapeutic efficacy.
  • Multidrug resistance protein 1 (MDR1/P-glycoprotein/P-gp), encoded by ABCB1, is a key transporter implicated in chemotherapy resistance.
  • Past efforts to target MDR1 therapeutically were hindered by a lack of adequate tools and understanding.

Purpose of the Study:

  • To re-evaluate the clinical significance of ABC transporters in mediating multidrug resistance in various cancer types.
  • To explore the potential of targeting ABC transporters for enhancing drug delivery, particularly across the blood-brain barrier.
  • To present recent evidence supporting a renewed investigation into ABC transporters as therapeutic targets.

Main Methods:

  • Review and synthesis of recent scientific literature and emerging data on ABC transporters in cancer.
  • Analysis of the role of MDR1, ABCC1 (MRP1), and ABCG2 in drug resistance mechanisms.
  • Examination of the implications of ABC transporter activity at the blood-brain barrier.

Main Results:

  • Evidence suggests that ABC transporters, including MDR1, MRP1, and ABCG2, continue to play a significant role in cancer multidrug resistance.
  • Recent advancements in technology and data provide new opportunities for characterizing and targeting these transporters.
  • The blood-brain barrier presents a critical area where ABC transporters influence drug penetration and efficacy.

Conclusions:

  • It is timely to revisit the investigation of ABC transporters as therapeutic targets in oncology.
  • Targeting ABC transporters could offer novel strategies for improving chemotherapy effectiveness and drug delivery in cancer patients.
  • Further research into ABC transporter function is warranted to overcome drug resistance and enhance treatment outcomes.

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