Optimization of an Enzymatic Antibody–Drug Conjugation Approach Based on Coenzyme A Analogs

Phosphopantetheine transferases (PPTases) can be used to efficiently prepare site-specific antibody–drug conjugates (ADCs) by enzymatically coupling coenzyme A (CoA)-linker payloads to 11–12 amino acid peptide substrates inserted into antibodies. Here, a two-step strategy is established wherein in a...

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