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A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
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Published on: December 7, 2014

Drug transporters: recent advances concerning BCRP and tyrosine kinase inhibitors

C Lemos1, G Jansen, G J Peters

  • 1Department of Medical Oncology, VU University Medical Center, Amsterdam, The Netherlands.

British Journal of Cancer
|February 7, 2008
PubMed

Insights

Multidrug resistance in cancer is linked to ATP-binding cassette (ABC) transporters. This review focuses on the breast cancer resistance protein (BCRP/ABCG2) and its impact on anticancer drug efficacy, especially tyrosine kinase inhibitors.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Multidrug resistance (MDR) is a major challenge in cancer therapy.
  • Overexpression of ATP-binding cassette (ABC) transporters is a key mechanism of MDR.
  • The breast cancer resistance protein (BCRP/ABCG2) is a significant ABC transporter implicated in drug efflux.

Purpose of the Study:

  • To review the role of BCRP/ABCG2 in the efficacy of novel anticancer agents.
  • To highlight the impact of BCRP/ABCG2 on the (pre)clinical outcomes of tyrosine kinase inhibitors (TKIs).

Main Methods:

  • Literature review of studies investigating BCRP/ABCG2.
  • Analysis of data on BCRP/ABCG2 expression and its correlation with drug response.
  • Focus on experimental anticancer drugs, particularly TKIs.

Main Results:

  • BCRP/ABCG2 overexpression is associated with reduced sensitivity to various anticancer drugs.
  • BCRP/ABCG2 significantly influences the efficacy of several TKIs in preclinical models.
  • Understanding BCRP/ABCG2's role can guide the development of strategies to overcome resistance.

Conclusions:

  • BCRP/ABCG2 is a critical determinant of therapeutic response to novel anticancer drugs, including TKIs.
  • Targeting or circumventing BCRP/ABCG2-mediated efflux is crucial for improving cancer treatment outcomes.
  • Further research into BCRP/ABCG2 modulation is warranted for effective cancer chemotherapy.

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