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ABC Transporter Inhibitors in Reversing Multidrug Resistance to Chemotherapy

Haigang Cui, Anna J Zhang, Mingwei Chen

  • 1School of Medicine, Faculty of Health, University of Tasmania. Private Bag 26 Hobart, Tasmania 7001 Australia. Johnson.liu@utas.edu.au.

Current Drug Targets
|April 23, 2015
PubMed

Insights

This review explores novel strategies to inhibit ATP-binding cassette (ABC) transporters, crucial in multidrug resistance (MDR) in cancer. It highlights investigational agents and new approaches targeting cancer stem cells for improved treatment outcomes.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • Human ATP-binding cassette (ABC) transporters are vital for physiological functions.
  • Certain ABC transporters, particularly ABCB1, ABCG2, and ABCC subfamily members, drive multidrug resistance (MDR) in cancer by effluxing anticancer drugs.
  • Previous inhibitor development for ABCB1 offers insights for new therapeutic strategies.

Purpose of the Study:

  • To review and evaluate current evidence on agents targeting ABC transporters for cancer MDR.
  • To emphasize experimental and investigational agents in preclinical and clinical development.
  • To discuss novel strategies targeting ABC transporters in cancer stem cells.

Main Methods:

  • Literature review and evidence evaluation.
  • Focus on preclinical and clinical investigational agents.
  • Analysis of novel chemical entities, natural products, microRNAs, and tyrosine kinase inhibitors.

Main Results:

  • Identified various classes of investigational agents targeting MDR-related ABC transporters.
  • Highlighted the role of tyrosine kinase inhibitors, natural products, microRNAs, and novel chemical entities.
  • Discussed emerging strategies for targeting ABC transporters in cancer stem cells.

Conclusions:

  • Novel strategies and agents are under investigation to overcome ABC transporter-mediated MDR in cancer.
  • Targeting ABC transporters in cancer stem cells presents a promising future direction.
  • Continued research is essential for developing effective therapies against multidrug-resistant cancers.

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