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Aldolase antibody activation of prodrugs of potent aldehyde-containing cytotoxics for selective chemotherapy
Authors:Sinha Subhash C  Li Lian-Sheng  Watanabe Shin-Ichi  Kaltgrad Eiton  Tanaka Fujie  Rader Christoph  Lerner Richard A  Barbas Carlos F
Affiliation:Skaggs Institute for Chemical Biology and Department of Molecular Biology, Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA. subhash@scripps.edu
Abstract:Prodrugs of potent aldehyde analogues of the anticancer drug doxorubicin (Dox) were synthesized. These prodrugs were efficiently activated by antibody 93F3 and no drug formation was observed in the absence of 93F3 in either phosphate buffered saline or cell culture media. In the presence of antibody 93F3, these prodrugs were activated and decreased the proliferation of human cancer cells in in vitro proliferation assays.
Keywords:aldolase  antibodies  chemotherapy  doxorubicin  prodrugs
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