Advances of Site-Specific Antibody Conjugations: Design and Development for ADCs and Beyond
A special issue of Antibodies (ISSN 2073-4468). This special issue belongs to the section "Antibody Discovery and Engineering".
Deadline for manuscript submissions: closed (30 July 2024) | Viewed by 182
Special Issue Editor
Interests: antibody–drug conjugates; antibody glycan engineering; medicinal chemistry
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Antibody–drug conjugates (ADCs) are emerging as powerful precision medicines that deliver highly toxic chemotherapy agents specifically to antigen-bearing cancer cells. As one of the most powerful and successful avenues for cancer treatment, ADCs combine the advantage of high specificity of antibodies to avoid damaging effects on healthy cells and extreme potency of the cytotoxic payload to achieve cancer cell killing. The overall efficacy of an ADC is determined by the rational combination of the cell target, the antibody, the payload, the linker that connects the payload, and the bioconjugation method. The first generation of approved ADCs mainly relies on non-specific conjugation at lysine and/or hinge cysteines. This random conjugation strategy usually results in heterogeneous ADCs, which will likely affect the stability, characterization, process control and pharmacokinetic properties. To overcome the issues, site-specific conjugation strategies to generate homogeneous ADCs with tunable drug-to-antibody (DARs) ratios have been developed rapidly in recent years, which leads to more consistent quality attributes, improved pharmacokinetics, and an enhanced therapeutic index. Site-specific ADCs are likely to be the future of targeted cancer therapeutics. In this Special Issue, advances will be presented in the discovery and development of novel site-specific ADCs, including the exploration of novel conjugate chemistries, novel linker and payloads, novel target antigens and the evaluation of ADCs. Besides the preparation of ADCs, novel site-specific conjugation methods will also be applied in the generation of antibody immunoconjugates and PROTAC/ligand/antibiotic/radioisotope/siRNA/fluorophore conjugates, etc., for both therapeutic and diagnostic purposes.
Dr. Guanghui Zong
Guest Editor
Manuscript Submission Information
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Keywords
- antibody–drug conjugates
- site-specific conjugation
- antibody–PROTAC conjugates
- antibody–antibiotic conjugates
- small molecule–antibody conjugates
- targeted cancer therapy
- linker-payloads
- efficacy
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