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Human ABC transporter ABCG2 in cancer chemotherapy and pharmacogenomics

Toshihisa Ishikawa1, Hiroshi Nakagawa

  • 1Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, Nagatsuta 4259-B-60, Yokohama 226-8501, Japan. toshi-i@gsc.riken.jp

Journal of Experimental Therapeutics & Oncology
|October 16, 2009
PubMed

Insights

Multidrug resistance in cancer is often due to ATP-binding cassette (ABC) transporters like ABCG2. Understanding ABCG2

Area of Science:

  • Molecular Pharmacology
  • Cancer Biology
  • Drug Resistance Mechanisms

Background:

  • Multidrug resistance (MDR) in cancer is a major challenge, frequently mediated by ATP-binding cassette (ABC) transporters.
  • ABCG2 (breast cancer resistance protein, BCRP) is a key ABC transporter implicated in MDR, intrinsic resistance, and stem cell protection.
  • ABCG2's broad substrate specificity and role in photodynamic therapy are areas of significant research interest.

Purpose of the Study:

  • To review recent advances in the molecular pharmacology and pharmacogenomics of ABCG2.
  • To explore novel strategies for improving cancer chemotherapy by targeting ABCG2.
  • To discuss the regulation of ABCG2 expression and its implications in cancer treatment.

Main Methods:

  • Review of current literature on ABCG2 function, regulation, and clinical relevance.
  • Analysis of high-throughput screening and quantitative structure-activity relationship (QSAR) studies for ABCG2 substrates.
  • Examination of genetic polymorphisms in ABCG2 and their impact on chemotherapy.

Main Results:

  • ABCG2 overexpression is linked to acquired and intrinsic drug resistance in various cancers.
  • ABCG2 plays a crucial role in stem cell populations, contributing to cellular protection.
  • Regulation of ABCG2 involves transcriptional control and protein degradation pathways (endosomal, proteasomal).
  • Genetic variations in ABCG2 influence chemotherapy efficacy and adverse effects.

Conclusions:

  • Targeting ABCG2 presents a promising avenue for overcoming multidrug resistance in cancer.
  • Pharmacogenomic approaches considering ABCG2 polymorphisms can personalize cancer therapy.
  • Further research into ABCG2's molecular pharmacology is essential for developing more effective anticancer strategies.

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