ABCG2 inhibition as a therapeutic approach for overcoming multidrug resistance in cancer View Full Text


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Article Info

DATE

2016-04-05

AUTHORS

Maryam Hosseini Hasanabady, Fatemeh Kalalinia

ABSTRACT

Breast cancer resistance protein (BCRP, ABCP or MXR)/ATP-binding cassette subfamily G member 2 (ABCG2) was characterized as a multidrug resistance efflux transporter in 1998. ABCG2 physiologically acts as a part of a self-defence mechanism for the organism; it enhances eliminating of toxic xenobiotic substances and harmful agents in the intestine, as well as through the blood–brain barrier and placenta. ABCG2 recognizes and transports numerous anticancer drugs including conventional chemotherapeutic and new targeted small therapeutic molecules in clinical usage. Development of ABCG2 inhibitors for clinical usage may allow increased penetration of therapeutic agents into sanctuary sites and increases their intestinal absorption. Here we review the mechanisms that modulate MDR mediated by the ABC transporter ABCG2 in normal and cancer cells by different levels including, epigenetic modifications, transcriptional, post-transcriptional, translation and post-translational regulation. Some clinical applications of ABCG2 inhibitors are also explained. More... »

PAGES

313-324

References to SciGraph publications

  • 2001-01. An ATP-binding cassette gene (ABCG3) closely related to the multidrug transporter ABCG2 (MXR/ABCP) has an unusual ATP-binding domain in MAMMALIAN GENOME
  • 2009-07-24. Structure–Activity Relationships and Quantitative Structure–Activity Relationships for Breast Cancer Resistance Protein (ABCG2) in THE AAPS JOURNAL
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  • 2003-10-20. Multidrug resistance mediated by the breast cancer resistance protein BCRP (ABCG2) in ONCOGENE
  • 2001-09. The ABC transporter Bcrp1/ABCG2 is expressed in a wide variety of stem cells and is a molecular determinant of the side-population phenotype in NATURE MEDICINE
  • 2013-08-29. Transcription factors Sp1 and Sp3 regulate expression of human ABCG2 gene and chemoresistance phenotype in MOLECULES AND CELLS
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  • 2003-10-20. Transcriptional regulation of ABC drug transporters in ONCOGENE
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  • 2011-12-23. Pro-inflammatory cytokines interleukin-1 beta, interleukin 6, and tumor necrosis factor-alpha alter the expression and function of ABCG2 in cervix and gastric cancer cells in MOLECULAR AND CELLULAR BIOCHEMISTRY
  • 2014-01-22. Phase I dosage finding and pharmacokinetic study of intravenous topotecan and oral erlotinib in adults with refractory solid tumors in CANCER CHEMOTHERAPY AND PHARMACOLOGY
  • 2013-04-30. Melatonin-induced methylation of the ABCG2/BCRP promoter as a novel mechanism to overcome multidrug resistance in brain tumour stem cells in BRITISH JOURNAL OF CANCER
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  • 2011-05-30. ABCG2 is a direct transcriptional target of hedgehog signaling and involved in stroma-induced drug tolerance in diffuse large B-cell lymphoma in ONCOGENE
  • 2009-10-05. Mechanisms of Multidrug Resistance in Cancer in MULTI-DRUG RESISTANCE IN CANCER
  • 2004-06-21. Breast cancer resistance protein (BCRP/MXR/ABCG2) in acute myeloid leukemia: discordance between expression and function in LEUKEMIA
  • 2012-02-14. Expressions of putative cancer stem cell markers ABCB1, ABCG2, and CD133 are correlated with the degree of differentiation of gastric cancer in GASTRIC CANCER
  • Identifiers

    URI

    http://scigraph.springernature.com/pub.10.1007/s12038-016-9601-5

    DOI

    http://dx.doi.org/10.1007/s12038-016-9601-5

    DIMENSIONS

    https://app.dimensions.ai/details/publication/pub.1049256945

    PUBMED

    https://www.ncbi.nlm.nih.gov/pubmed/27240991


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