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Design and synthesis of paclitaxel conjugated with an ErbB2-Recognizing pepticle, EC-1

  1. Author:
    Li, P.
    Jiang, S.
    Pero, S. C.
    Oligino, L.
    Krag, D. N.
    Michejda, C. J.
    Roller, P. P.

  2. Author Address

    NCI, NIH, Med Chem Lab, CCR, Frederick, MD 21701 USA. NCI, NIH, Struct Biophys Lab, Mol Aspects Drug Design Sect, Frederick, MD USA. Univ Vermont, Vermont Canc Ctr, Sch Med, Dept Surg, Burlington, VT 05405 USA.;Roller, PP, Intra Cellular Therapies Inc, New York, NY 10032 USA.;proll@helix.nih.gov
    1. Year: 2007
    2. Date: Nov
  2. Journal: Biopolymers
    1. 87
    2. 4
    3. Pages: 225-230
  4. Type of Article: Article
  5. ISSN: 0006-3525
  1. Abstract:

    The selective delivery of therapeutic agents to receptors overexpressed in cancer cells without harming the rest of the body is a major challenge in clinical oncology today. In this study, we report the design and synthesis of paclitaxel (PTX) conjugated with an erbB2- recognizing peptide (EC-1). The cyclic peptide EC-1 specifically binds to the extracellular domain of ErbB2 and selectively inhibits proliferation of breast cancer cells overexpressing ErbB2. PTX is a potent antitumor agent commonly used in the treatment of advanced metastatic breast cancer, yet patients have to suffer some side effects caused by its systemic toxicity. The aim of our conjugate is to specifically deliver antitumor agent PTX to breast cancer cells that overexpress oncogenic ErbB2 with the purpose to reduce toxicity and enhance selective killing of cancer cells. In this study, a concise and efficient synthetic route for the preparation of the PTX-EC-1 conjugate has been developed in 69,6 overall yield. This synthetic approach provides a general method for conjugating a highly functionalized and disulfide-bridge containing cyclopeptide to Taxol or other antitumor agents. (c) 2007 Wiley Periodicals.

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  1. View record in Web of Science®
  2. WOS: 000250210700003

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