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Antibodies 2018, 7(1), 4;

Enzyme-Based Labeling Strategies for Antibody–Drug Conjugates and Antibody Mimetics

Cellular and Molecular Biotechnology, Faculty of Technology, Bielefeld University, Universitätsstr. 25, 33615 Bielefeld, Germany
Author to whom correspondence should be addressed.
Received: 1 November 2017 / Revised: 15 December 2017 / Accepted: 18 December 2017 / Published: 4 January 2018
(This article belongs to the Special Issue Therapeutic Antibodies)
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Strategies for site-specific modification of proteins have increased in number, complexity, and specificity over the last years. Such modifications hold the promise to broaden the use of existing biopharmaceuticals or to tailor novel proteins for therapeutic or diagnostic applications. The recent quest for next-generation antibody–drug conjugates (ADCs) sparked research into techniques with site selectivity. While purely chemical approaches often impede control of dosage or locus of derivatization, naturally occurring enzymes and proteins bear the ability of co- or post-translational protein modifications at particular residues, thus enabling unique coupling reactions or protein fusions. This review provides a general overview and focuses on chemo-enzymatic methods including enzymes such as formylglycine-generating enzyme, sortase, and transglutaminase. Applications for the conjugation of antibodies and antibody mimetics are reported. View Full-Text
Keywords: chemo-enzymatic labeling; armed antibody; antibody coupling; antibody conjugation chemo-enzymatic labeling; armed antibody; antibody coupling; antibody conjugation

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Falck, G.; Müller, K.M. Enzyme-Based Labeling Strategies for Antibody–Drug Conjugates and Antibody Mimetics. Antibodies 2018, 7, 4.

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