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Updated: Mar 23, 2026

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Current Status: Site-Specific Antibody Drug Conjugates
Dominik Schumacher1, Christian P R Hackenberger1, Heinrich Leonhardt2
1Chemical Biology and Department of Chemistry, Leibniz-Institut für Molekulare Pharmakologie and Humboldt Universität zu Berlin, Berlin, Germany.
Abstract:
Antibody drug conjugates (ADCs), a promising class of cancer biopharmaceuticals, combine the specificity of therapeutic antibodies with the pharmacological potency of chemical, cytotoxic drugs. Ever since the first ADCs on the market, a plethora of novel ADC technologies has emerged, covering as diverse aspects as antibody engineering, chemical linker optimization and novel conjugation strategies, together aiming at constantly widening the therapeutic window for ADCs. This review primarily focuses on novel chemical and biotechnological strategies for the site-directed attachment of drugs that are currently validated for 2nd generation ADCs to promote conjugate homogeneity and overall stability.
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