Tumor-specific novel taxoid-monoclonal antibody conjugates |
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Authors: | Ojima Iwao Geng Xudong Wu Xinyuan Qu Chuanxing Borella Christopher P Xie Hongsheng Wilhelm Sharon D Leece Barbara A Bartle Laura M Goldmacher Victor S Chari Ravi V J |
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Affiliation: | Department of Chemistry, State University of New York at Stony Brook, Stony Brook, New York 11794-3400, USA. iojima@notes.cc.sunysb.edu |
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Abstract: | Taxoids bearing methyldisulfanyl(alkanoyl) groups for taxoid-antibody immunoconjugates were designed, synthesized and their activities evaluated. A highly cytotoxic C-10 methyldisulfanylpropanoyl taxoid was conjugated to monoclonal antibodies recognizing the epidermal growth factor receptor (EGFR) expressed in human squamous cancers. These conjugates were shown to possess remarkable target-specific antitumor activity in vivo against EGFR-expressing A431 tumor xenografts in severe combined immune deficiency mice, resulting in complete inhibition of tumor growth in all the treated mice. |
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