(6-Maleimidocaproyl)hydrazone of doxorubicin. A new derivative for the preparation of immunoconjugates of doxorubicin
Bioconjugate Chemistry1993Vol. 4(6), pp. 521–527
Citations Over TimeTop 10% of 1993 papers
David Willner, Pamela A. Trail, Sandra J. Hofstead, Dalton King, Shirley J. Lasch, Gary R. Braslawsky, Robert S. Greenfield, Takushi Kaneko, Raymond A. Firestone
Abstract
The (6-maleimidocaproyl)hydrazone of doxorubicin was synthesized and conjugated to several mAbs, including chimeric BR96, via a Michael addition reaction to thiol-containing mAbs. DTT reduction of disulfides present in the mAb was a reliable and general method for generating a consistent number of reactive SH groups. The conjugates, after purification by Bio-Beads, were free of unreacted linker and/or doxorubicin. All conjugates released doxorubicin under acidic conditions that mimic the lysosomal environment, while they were relatively stable at neutral pH. BR96 conjugates showed antigen-specific cytotoxicity.
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