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Structure and function of the human breast cancer resistance protein (BCRP/ABCG2)

Zhanglin Ni1, Zsolt Bikadi, Mark F Rosenberg

  • 1Department of Pharmaceutics, School of Pharmacy, University of Washington, Health Science Building H272, 1959 NE Pacific Street, Seattle, Washington 98195-7610, USA.

Current Drug Metabolism
|September 4, 2010
PubMed

Insights

The breast cancer resistance protein (BCRP/ABCG2) is an ABC transporter that expels drugs from cells. This review covers BCRP

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • The human breast cancer resistance protein (BCRP/ABCG2) is an ATP-binding cassette transporter.
  • BCRP confers resistance to chemotherapy drugs by extruding them from cells.
  • It also transports various xenobiotics and is found in stem cells and normal tissues.

Purpose of the Study:

  • To review the current knowledge of the structure and function of BCRP/ABCG2.
  • To highlight BCRP's role in drug absorption, elimination, and distribution.
  • To discuss the challenges in understanding BCRP's transport mechanism for diverse substrates.

Main Methods:

  • Literature review of existing studies on BCRP/ABCG2.
  • Analysis of BCRP's known substrates and tissue expression.
  • Discussion of structure-function relationships and transport mechanisms.

Main Results:

  • BCRP is a significant efflux transporter involved in multidrug resistance.
  • It plays a crucial role in the pharmacokinetics of various drugs and xenobiotics.
  • BCRP's broad substrate specificity and transport mechanism remain areas of active research.

Conclusions:

  • BCRP/ABCG2 is a medically important transporter with implications in cancer therapy and drug disposition.
  • Further research into its structure and mechanism is needed to understand its broad substrate recognition.
  • Understanding BCRP function is key to optimizing drug efficacy and minimizing toxicity.

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