化学
腙
阿霉素
结合
连接器
共轭体系
细胞毒性
组合化学
衍生工具(金融)
硫醇
立体化学
有机化学
生物化学
聚合物
体外
化疗
外科
经济
数学分析
操作系统
金融经济学
医学
计算机科学
数学
作者
David Willner,Pamela A. Trail,Sandra J. Hofstead,Dalton King,Shirley J. Lasch,Gary R. Braslawsky,Robert S. Greenfield,Takushi Kaneko,Raymond A. Firestone
摘要
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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