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Aldolase Antibody Activation of Prodrugs of Potent Aldehyde‐Containing Cytotoxics for Selective Chemotherapy
Author(s) -
Sinha Subhash C.,
Li LianSheng,
Watanabe Shinichi,
Kaltgrad Eiton,
Tanaka Fujie,
Rader Christoph,
Lerner Richard A.,
Barbas Carlos F.
Publication year - 2004
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.200400419
Subject(s) - prodrug , in vitro , pharmacology , chemistry , drug , doxorubicin , chemotherapy , antibody , aldolase a , monoclonal antibody , aldehyde , cell growth , biochemistry , medicine , enzyme , immunology , catalysis
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.