One-step strategy to synthesize site-specific antibody-drug conjugates with LacNAc-based substrates

Antibody-drug conjugates (ADCs), a complex covalently linking a potent cytotoxin onto the antibody, has attracted great interest as a novel biotherapeutic approach. Site-specific conjugation of potent payloads can improve the therapeutic index of ADCs compared with random conjugation. Glycosite-specific ADCs (gsADCs), harnessing Asn297 N-glycan of IgG Fc as the conjugation site for drug payloads, usually require multi-steps for IgG glycoengineering with two or more enzymes, thus limiting the substrates diversification and complicating the preparation process.


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Source: Phys.org