reviewThe AAPS JournalSep 18, 2014HYBRID OA

Role of the Breast Cancer Resistance Protein (BCRP/ABCG2) in Drug Transport—an Update

University of Washington

PubMed
Indexed incrossrefpubmed

Abstract

The human breast cancer resistance protein (BCRP, gene symbol ABCG2) is an ATP-binding cassette (ABC) efflux transporter. It was so named because it was initially cloned from a multidrug-resistant breast cancer cell line where it was found to confer resistance to chemotherapeutic agents such as mitoxantrone and topotecan. Since its discovery in 1998, the substrates of BCRP have been rapidly expanding to include not only therapeutic agents but also physiological substances such as estrone-3-sulfate, 17β-estradiol 17-(β-D-glucuronide) and uric acid. Likewise, at least hundreds of BCRP inhibitors have been identified. Among normal human tissues, BCRP is highly expressed on the apical membranes of the placental…

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Authors

2

Topics & keywords

Keywords
  • Abcg2
  • Pharmacology
  • ABCC1
  • ATP-binding cassette transporter
  • Efflux
  • Mitoxantrone
  • Multidrug Resistance-Associated Proteins
  • Drug
UN Sustainable Development Goals
  • Good health and well-being
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