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International Journal of Oncology
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Print ISSN: 1019-6439 Online ISSN: 1791-2423
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January-2015 Volume 46 Issue 1

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Journals

International Journal of Molecular Medicine

International Journal of Molecular Medicine

International Journal of Molecular Medicine is an international journal devoted to molecular mechanisms of human disease.

International Journal of Oncology

International Journal of Oncology

International Journal of Oncology is an international journal devoted to oncology research and cancer treatment.

Molecular Medicine Reports

Molecular Medicine Reports

Covers molecular medicine topics such as pharmacology, pathology, genetics, neuroscience, infectious diseases, molecular cardiology, and molecular surgery.

Oncology Reports

Oncology Reports

Oncology Reports is an international journal devoted to fundamental and applied research in Oncology.

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine is an international journal devoted to laboratory and clinical medicine.

Oncology Letters

Oncology Letters

Oncology Letters is an international journal devoted to Experimental and Clinical Oncology.

Biomedical Reports

Biomedical Reports

Explores a wide range of biological and medical fields, including pharmacology, genetics, microbiology, neuroscience, and molecular cardiology.

Molecular and Clinical Oncology

Molecular and Clinical Oncology

International journal addressing all aspects of oncology research, from tumorigenesis and oncogenes to chemotherapy and metastasis.

World Academy of Sciences Journal

World Academy of Sciences Journal

Multidisciplinary open-access journal spanning biochemistry, genetics, neuroscience, environmental health, and synthetic biology.

International Journal of Functional Nutrition

International Journal of Functional Nutrition

Open-access journal combining biochemistry, pharmacology, immunology, and genetics to advance health through functional nutrition.

International Journal of Epigenetics

International Journal of Epigenetics

Publishes open-access research on using epigenetics to advance understanding and treatment of human disease.

Medicine International

Medicine International

An International Open Access Journal Devoted to General Medicine.

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Article

The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells

  • Authors:
    • Stefan Brenner
    • Juliane Riha
    • Benedikt Giessrigl
    • Theresia Thalhammer
    • Michael Grusch
    • Georg Krupitza
    • Bruno Stieger
    • Walter Jäger

  • View Affiliations / Copyright

    Affiliations: Department of Clinical Pharmacy and Diagnostics, University of Vienna, Vienna, Austria, Department of Pathophysiology and Allergy Research, Center of Pathophysiology, Medical University of Vienna, Vienna, Austria, Department of Medicine I, Division of Cancer Research, Medical University of Vienna, Vienna, Austria, Clinical Pathology, Medical University of Vienna, Vienna, Austria, Department of Clinical Pharmacology and Toxicology, University Hospital Zurich, Zurich, Switzerland
  • Pages: 324-332
    |
    Published online on: October 24, 2014
       https://doi.org/10.3892/ijo.2014.2731
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Abstract

The contribution of organic anion transporting polypeptides (OATPs) to the cellular uptake of flavopiridol was investigated in OATP1B1-, OATP1B3- and OATP2B1-expressing Chinese hamster ovary (CHO) cells. Uptake of flavopiridol into these cells showed typical Michaelis-Menten kinetics with much higher transport capacity for OATP1B3 compared to OATP1B1 and OATP2B1 (Vmax/Km, 33.9 vs. 8.84 and 2.41 µl/mg/min, respectively). The predominant role of OATPs was further supported by a dramatic inhibition of flavopiridol uptake in the presence of the OATP substrate rifampicin. Uptake of flavopiridol by OATPs also seems to be an important determinant in breast cancer cells. The much higher mRNA level for OATP1B1 found in wild-type compared to ZR-75-1 OATP1B1 knockdown cells correlated with higher flavopiridol initial uptake leading to 4.6-fold decreased IC50 values in the cytotoxicity assay (IC50, 1.45 vs. 6.64 µM). Cell cycle profile also showed a clear incidence for a stronger cell cycle arrest in the G2/M phase for ZR-75-1 wild-type cells compared to OATP1B1 knockdown cells, further indicating an active uptake via OATP1B1. In conclusion, our results revealed OATP1B1, OATP1B3 and OATP2B1 as uptake transporters for flavopiridol in cancer cells, which may also apply in patients during cancer therapy.

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Copy and paste a formatted citation
Spandidos Publications style
Brenner S, Riha J, Giessrigl B, Thalhammer T, Grusch M, Krupitza G, Stieger B and Jäger W: The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells. Int J Oncol 46: 324-332, 2015.
APA
Brenner, S., Riha, J., Giessrigl, B., Thalhammer, T., Grusch, M., Krupitza, G. ... Jäger, W. (2015). The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells. International Journal of Oncology, 46, 324-332. https://doi.org/10.3892/ijo.2014.2731
MLA
Brenner, S., Riha, J., Giessrigl, B., Thalhammer, T., Grusch, M., Krupitza, G., Stieger, B., Jäger, W."The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells". International Journal of Oncology 46.1 (2015): 324-332.
Chicago
Brenner, S., Riha, J., Giessrigl, B., Thalhammer, T., Grusch, M., Krupitza, G., Stieger, B., Jäger, W."The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells". International Journal of Oncology 46, no. 1 (2015): 324-332. https://doi.org/10.3892/ijo.2014.2731
Copy and paste a formatted citation
x
Spandidos Publications style
Brenner S, Riha J, Giessrigl B, Thalhammer T, Grusch M, Krupitza G, Stieger B and Jäger W: The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells. Int J Oncol 46: 324-332, 2015.
APA
Brenner, S., Riha, J., Giessrigl, B., Thalhammer, T., Grusch, M., Krupitza, G. ... Jäger, W. (2015). The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells. International Journal of Oncology, 46, 324-332. https://doi.org/10.3892/ijo.2014.2731
MLA
Brenner, S., Riha, J., Giessrigl, B., Thalhammer, T., Grusch, M., Krupitza, G., Stieger, B., Jäger, W."The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells". International Journal of Oncology 46.1 (2015): 324-332.
Chicago
Brenner, S., Riha, J., Giessrigl, B., Thalhammer, T., Grusch, M., Krupitza, G., Stieger, B., Jäger, W."The effect of organic anion-transporting polypeptides 1B1, 1B3 and 2B1 on the antitumor activity of flavopiridol in breast cancer cells". International Journal of Oncology 46, no. 1 (2015): 324-332. https://doi.org/10.3892/ijo.2014.2731
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