Site‐Specific and Stoichiometric Modification of Antibodies by Bacterial Transglutaminase

作者：Simone Jeger, Kurt Zimmermann, Alain Blanc, Jürgen Grünberg, Michael Honer, Peter Hunziker, Harriet Struthers, Roger Schibli · 发表于：Angewandte Chemie International Edition · 年份：2010 · DOI：10.1002/anie.201004243 · 被引用次数：343 · 研究领域：Blood properties and coagulation、Protein purification and stability、Toxin Mechanisms and Immunotoxins

Spot on: Bacterial transglutaminase enables the site-specific modification of Gln side chains of tumor-targeting antibodies with various probes containing lysine or lysine surrogates. The method yields completely homogeneous immunoconjugates with a defined stoichiometry. In comparative in vivo studies with xenografted mice the pharmacological profiles for enzymatically conjugated antibodies were better than those of chemically modified analogues.