Linkers for Antibody-Drug Conjugation (ADC)

Antibody–drug conjugates (ADCs) offer a unique-targeted therapeutic strategy combining the best features of both antibodies and small-molecule drugs to create a single moiety that is highly specific and cytotoxic. One of the biggest challenges in the development of ADCs has been the generation of suitable linkers for the conjugation of antibody and drug. Chemically labile linkers, such as hydrazones and disulfides, often suffer from limited plasma stability. Therefore, peptide-based linker technologies may offer better control of drug release. Peptidic bonds are expected to have good serum stability. Cleavable dipeptide linkers like Val-Ala and Val-Cit rely on processes inside the cell to liberate the payload, as they undergo rapid hydrolysis in the presence of lysosomal extracts or purified human cathepsin B.

Any other peptide based linker can be produced according to your individual requirements on custom basis. Please send your enquiry to info@iris-biotech.de.

• Linker Technologies for Antibody–Drug Conjugates; Nolting B. in Antibody-Drug Conjugates, Ducry L. (ed.), Methods in Molecular Biology 2013; 1045: 71-100. doi:10.1007/978-1-62703-541-5_5
• Proteinases 1: lysosomal cysteine proteinases; H. Kirschke, A. J. Barrett and N. D. Rawlings; Protein Profile 1995; 2: 1581-643.
• Cysteine Proteases and Their Inhibitors; H.-H. Otto and T. Schirmeister; Chem Rev 1997; 97: 133-172. doi:10.1021/cr950025u