The role of human ABC transporter ABCG2 (BCRP) in pharmacotherapy

doi:10.1016/j.addr.2008.12.001

Advanced Drug Delivery Reviews

Volume 61, Issue 1, 31 January 2009, Pages 1-2

https://doi.org/10.1016/j.addr.2008.12.001 Get rights and content

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Acknowledgements

As the theme editor, I wish to cordially thank all of the contributing authors for their excellent reviews that convey the latest information on and new aspects of our understanding of the protein structure and the physiological role of the human ABC transporter ABCG2. In addition, I am grateful to the ADDR editors, Prof. Vincent H.L. Lee (University of Hong Kong) and Prof. Yoshinobu Takakura (Kyoto University), as well as Ms. Brigitte Neilson (ELS-SHA) for their continuous support and

References (3)

L.A. Doyle et al.
A multidrug resistance transporter from human MCF-7 breast cancer cells
Proc. Natl. Acad. Sci. U. S. A.
(1998)

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Cited by (11)

miR-302a/b/c/d cooperatively inhibit BCRP expression to increase drug sensitivity in breast cancer cells
2016, Gynecologic Oncology
Citation Excerpt :
It is known that BCRP plays an important role in absorption, distribution, and elimination of its substrate anticancer drugs, and thus confers multidrug resistance in cancer cells [3]. BCRP overexpression represents an important mechanism for multidrug resistance in breast cancer [4–6]. Therefore, targeting BCRP expression and function is a promising strategy for reversing multidrug resistance in breast cancer.
BCRP is overexpressed in many tumors and mediates multidrug resistance in breast cancer. In this study, we determined the involvement of miR-302S in the development of drug resistance in breast cancer.
The differential miRNA expression profiling in parental MCF-7 cells and its derivative mitoxantrone (MX)-resistant MCF-7 (MCF-7/MX) cells was determined by the microarray analysis. The levels of miR-302S family and BCRP mRNA expression were determined by using Quantitative Real-Time PCR. The targeting effect between the individuals of miR-302S and BCRP mRNA-3'UTR were detected by dual-luciferase reporter assay. Proteins of BCRP are represented by Western blot assay. Cell viability was assessed by MTS assay. Efflux capacity was evaluated using flow cytometry.
The miR-302S family including miR-302a, miR-302b, miR-302c, and miR-302d was significantly down-regulated in BCRP-overexpressing MCF-7/MX cells. Luciferase activity assay showed that miR-302 inhibited BCRP expression by targeting the 3′-untranslated region (UTR) of the BCRP mRNA. Overexpression of miR-302 increased intracellular accumulation of MX and sensitized breast cancer cells to MX. Furthermore, intratumoral injection of miR-302 potentiated the inhibitory effect of MX on tumor growth in mice transplanted with MCF-7/MX cells. Most importantly, miR-302S produced stronger effects than each individual member alone.
These findings suggest that miR-302 inhibits BCRP expression via targeting the 3′-UTR of BCRP mRNA. miR-302 members may cooperatively downregulate BCRP expression to increase chemosensitivity of breast cancer cells. miR-302 gene cluster may be a potential target for reversing BCRP-mediated chemoresistance in breast cancer.
Radiosynthesis of [2- <sup>11</sup>C-carbonyl]dantrolene using [ <sup>11</sup>C]phosgene for PET
2010, Applied Radiation and Isotopes
Citation Excerpt :
ATP-binding cassette (ABC) transporters, as typified by P-glycoprotein (P-gp/ABCB1) and the multidrug resistance-associated protein (MRP/ABCC) family, are assumed to play significant roles in the blood–brain barrier (BBB) to limit the movement of drugs and other xenobiotic compounds from the blood into the brain (Gottesman et al., 2002; Borst and Oude, 2002). Breast cancer resistance protein (BCRP/ABCG2), which was isolated from atypical multidrug resistant MCF-7 human breast cancer cells, is an ABC transporter and mediates the efflux transport of xenobiotics (Doyle et al., 1998; Ishikawa, 2009). BCRP is expressed in various normal tissues (Maliepaard et al., 2001) as well as in tissue barriers such as those in brain, testis, and placenta similarly to P-gp and MRPs (Bart et al., 2004; Zhang et al., 2003).
Automated radiosynthesis of [2-¹¹C-carbonyl]dantrolene, the substrate of breast cancer resistance protein (BCRP/ABCG2), was performed for the first time through a multi-step/one-pot labeling sequence that started with ethyl 2-{2-[5-(4-nitrophenyl)furfurylidene]hydrazino}acetate and used [¹¹C]phosgene as a labeling agent. After optimization of the automated synthesis conditions and parameters, [2-¹¹C-carbonyl]dantrolene was obtained at a radiochemical yield of 34.0±8.4% (decay-corrected). The radiochemical purity was greater than 98% and the specific activity was 46.8±15.2 GBq/μmol at the end of the synthesis.
Application of model-based approaches to evaluate Hepatic transporter-mediated drug clearance: In vitro, in vivo, and in vitro-in vivo extrapolation
2016, Current Drug Metabolism
In vivo and ex vivo regulation of breast cancer resistant protein (Bcrp) by peroxisome proliferator-activated receptor alpha (PPARα) at the blood-brain barrier
2015, Journal of Neurochemistry
Breast cancer resistance protein (BCRP/ABCG2) localises to the nucleus in glioblastoma multiforme cells
2012, Xenobiotica
Regulation of breast cancer resistant protein by peroxisome proliferator-activated receptor α in human brain microvessel endothelial cells
2012, Molecular Pharmacology

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^☆: This preface is part of the Advanced Drug Delivery Reviews theme issue on "The Role of Human ABC Transporter ABCG2 (BCRP) in Pharmacotherapy".

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PrefaceThe role of human ABC transporter ABCG2 (BCRP) in pharmacotherapy☆

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Acknowledgements

A multidrug resistance transporter from human MCF-7 breast cancer cells

Proc. Natl. Acad. Sci. U. S. A.

Preface
The role of human ABC transporter ABCG2 (BCRP) in pharmacotherapy☆