Synthesis and evaluation of hydrophilic linkers for antibody-maytansinoid conjugates.

  title={Synthesis and evaluation of hydrophilic linkers for antibody-maytansinoid conjugates.},
  author={Robert Yongxin Zhao and Sharon D Wilhelm and Charlene A. Audette and Gregory Jones and Barbara A Leece and Alexandru C. Lazar and Victor S. Goldmacher and Rajeeva Singh and Yelena V. Kovtun and Wayne C Widdison and J. G. Lambert and Ravi V. J. Chari},
  journal={Journal of medicinal chemistry},
  volume={54 10},
The synthesis and biological evaluation of hydrophilic heterobifunctional cross-linkers for conjugation of antibodies with highly cytotoxic agents are described. These linkers contain either a negatively charged sulfonate group or a hydrophilic, noncharged PEG group in addition to an amine-reactive N-hydroxysuccinimide (NHS) ester and sulfhydryl reactive termini. These hydrophilic linkers enable conjugation of hydrophobic organic molecule drugs, such as a maytansinoid, at a higher drug/antibody… CONTINUE READING