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ABCG2 inhibition as a therapeutic approach for overcoming multidrug resistance in cancer

Maryam Hosseini Hasanabady1, Fatemeh Kalalinia

  • 1Department of Biology, Science and Research Branch, Islamic Azad University, Mashhad, Iran.

Journal of Biosciences
|June 1, 2016
PubMed

Insights

Breast cancer resistance protein (BCRP) / ATP-binding cassette subfamily G member 2 (ABCG2) is a transporter that affects drug efficacy. Understanding its regulation is key to improving cancer therapy and drug delivery.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Breast cancer resistance protein (BCRP), also known as ATP-binding cassette subfamily G member 2 (ABCG2), functions as a crucial efflux transporter.
  • ABCG2 plays a physiological role in eliminating xenobiotics and protecting organs like the brain and placenta.

Purpose of the Study:

  • To review the regulatory mechanisms of ABCG2-mediated multidrug resistance (MDR).
  • To explore the clinical applications of ABCG2 inhibitors in cancer treatment.

Main Methods:

  • Literature review of studies on ABCG2.
  • Analysis of epigenetic, transcriptional, post-transcriptional, translational, and post-translational regulation of ABCG2.
  • Examination of clinical data on ABCG2 inhibitors.

Main Results:

  • ABCG2 transports various anticancer drugs, impacting treatment outcomes.
  • Inhibitors of ABCG2 show potential for enhancing drug penetration and absorption.
  • Multiple regulatory levels influence ABCG2 activity in normal and cancer cells.

Conclusions:

  • Modulating ABCG2 activity through inhibitors can overcome multidrug resistance.
  • Targeting ABCG2 offers a promising strategy for improving cancer chemotherapy and drug delivery.

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