(6-Maleimidocaproyl)hydrazone of doxorubicin--a new derivative for the preparation of immunoconjugates of doxorubicin.

@article{Willner19936MaleimidocaproylhydrazoneOD,
  title={(6-Maleimidocaproyl)hydrazone of doxorubicin--a new derivative for the preparation of immunoconjugates of doxorubicin.},
  author={David Willner and Pamela A. Trail and Sandra J Hofstead and Harley D. King and Shirley J Lasch and Gary R. Braslawsky and Robert S. Greenfield and Takushi Kaneko and Raymond A. Firestone},
  journal={Bioconjugate chemistry},
  year={1993},
  volume={4 6},
  pages={521-7}
}
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… CONTINUE READING
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