An Aptamer–Doxorubicin Physical Conjugate as a Novel Targeted Drug-Delivery Platform

Authors

  • Vaishali Bagalkot,

    1. Department of Life Science, Gwangju Institute of Science and Technology, 1 Oryoung-dong, Buk-gu, Gwangju 500712, South Korea, Fax: (+82) 62-970-2504
    2. Department of Anaesthesiology, Brigham and Women's Hospital and Harvard Medical School, 75 Francis Street, Boston, MA 02115, USA, Fax: (+1) 617-730-2801
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  • Omid C. Farokhzad Prof. Dr.,

    1. Department of Anaesthesiology, Brigham and Women's Hospital and Harvard Medical School, 75 Francis Street, Boston, MA 02115, USA, Fax: (+1) 617-730-2801
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  • Robert Langer Prof. Dr.,

    1. Department of Chemical Engineering, Massachusetts Institute of Technology, E25-342, 45 Carleton Street, Cambridge, MA 02139, USA
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  • Sangyong Jon Prof. Dr.

    1. Department of Life Science, Gwangju Institute of Science and Technology, 1 Oryoung-dong, Buk-gu, Gwangju 500712, South Korea, Fax: (+82) 62-970-2504
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  • This work was supported by Korea Science and Technology Foundation grant R01-2006-000-10818-0 (S.J. and V.B.) and USA National Institutes of Health grants CA 119349 (R.L., O.F., and V.B.) and EB 003647 (O.F.). We also thank Prof. C. S. Park for helpful discussions. This work is dedicated to the families of patients with cancer.

Abstract

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Trojan aptamer: A novel strategy for targeted drug delivery to cancer cells was developed through the formation of a physical conjugate (see scheme) between doxorubicin (Dox) and the A10 RNA aptamer that binds to the prostate-specific membrane antigen (PSMA). The aptamer–Dox conjugate could efficiently bind to PSMA-expressing cells, thereby resulting in its uptake and the intracellular release of Dox.

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