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Reversing agents for ATP-binding cassette (ABC) transporters: application in modulating multidrug resistance (MDR)

Chow H Lee1

  • 1Chemistry Program, University of Northern British Columbia, Prince George, British Columbia V2N 4Z9, Canada. leec@unbc.ca

Current Medicinal Chemistry. Anti-Cancer Agents
|February 3, 2004
PubMed

Insights

Multidrug resistance (MDR) in cancer chemotherapy involves ATP-binding cassette (ABC) transporters. This review discusses agents that reverse MDR by targeting these transporters at the protein, mRNA, or DNA level.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Multidrug resistance (MDR) is a primary cause of cancer chemotherapy failure.
  • ATP-binding cassette (ABC) transporters, like P-glycoprotein (P-gp), mediate MDR.
  • Developing agents to overcome MDR is crucial for effective cancer treatment.

Purpose of the Study:

  • To review and discuss known MDR reversing agents targeting ABC transporters.
  • To explore strategies acting at the protein, mRNA, or DNA level.
  • To identify potential new agents and approaches for MDR reversal.

Main Methods:

  • Literature review of existing MDR reversing agents.
  • Analysis of agents targeting ABC transporters (P-gp, MRP, BCRP).
  • Discussion of strategies at molecular levels (protein, mRNA, DNA).

Main Results:

  • Several compounds have demonstrated efficacy in reversing MDR phenotypes.
  • Agents target ABC transporters through various mechanisms.
  • Strategies exist to inhibit transporter function, gene expression, or DNA.

Conclusions:

  • Targeting ABC transporters offers a promising strategy to combat MDR in cancer.
  • Further research into novel reversing agents and combination therapies is warranted.
  • Understanding MDR mechanisms is key to developing more effective chemotherapy.

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