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Site‐Specific and Stoichiometric Modification of Antibodies by Bacterial Transglutaminase
Author(s) -
Jeger Simone,
Zimmermann Kurt,
Blanc Alain,
Grünberg Jürgen,
Honer Michael,
Hunziker Peter,
Struthers Harriet,
Schibli Roger
Publication year - 2010
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201004243
Subject(s) - tissue transglutaminase , lysine , homogeneous , antibody , stoichiometry , chemistry , in vivo , specific antibody , biochemistry , conjugated system , computational biology , combinatorial chemistry , enzyme , biology , amino acid , polymer , organic chemistry , immunology , microbiology and biotechnology , mathematics , combinatorics
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.