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Breast cancer resistance protein (BCRP/ABCG2)

Frantisek Staud1, Petr Pavek

  • 1Department of Pharmacology and Toxicology, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Heyrovskeho 1203, Hradec Kralove 50005, Czech Republic. staud@faf.cuni.cz

The International Journal of Biochemistry & Cell Biology
|February 8, 2005
PubMed

Insights

Breast cancer resistance protein (BCRP) is a key transporter involved in drug resistance and pharmacokinetics. Inhibitors are sought to improve drug absorption and overcome resistance, with mutant BCRP used in stem cell therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Breast cancer resistance protein (BCRP) is a major ABC drug efflux transporter identified 7 years ago.
  • BCRP (655 amino acid peptide) extrudes diverse chemical compounds, contributing significantly to drug resistance in mammalian cells.
  • It is expressed in epithelia crucial for drug disposition (placenta, liver, intestine) and plays a role in stem cell "side population" and hypoxia protection.

Purpose of the Study:

  • To investigate the multifaceted roles of BCRP in cellular processes.
  • To highlight the therapeutic potential of targeting BCRP for overcoming drug resistance.
  • To explore the applications of BCRP in stem cell biology and gene therapy.

Main Methods:

  • Biochemical analysis of BCRP structure and function.
  • Pharmacokinetic studies involving BCRP substrates.
  • Investigation of BCRP's role in stem cell phenotypes and hypoxia response.

Main Results:

  • BCRP identified as a major contributor to multidrug resistance.
  • BCRP's significant role in drug disposition across key organs.
  • BCRP's involvement in stem cell characteristics and cellular protection mechanisms.

Conclusions:

  • BCRP inhibitors are crucial for enhancing drug efficacy and pharmacokinetics.
  • Targeting BCRP offers potential therapeutic strategies for cancer and other diseases.
  • Mutant BCRP holds promise as a selectable marker in stem cell gene therapy applications.

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