The valine-citrulline (Val-Cit) linker is a cleavable peptide linker that can be cleaved by cathepsin B, a protease highly expressed in cancer cells, which confers specificity of the Antibody-drug conjugates (ADCs) to cancer cells. Although the Val-Cit linker is widely used in many FDA-approved ADCs, it is still associated with several limitations, including:
A recent study proposed a novel linker to address the intrinsic limitations of the Val-Cit linker (Fig 1). Breaking away from the conventional linear "Antibody-Linker-Payload" structure, the researchers developed an innovative design that repositions the cleavable peptide linker at the exo position of the p-aminobenzylcarbamate moiety (Fig 1). In this design, exolinkers offer a new strategy for improving therapeutic efficacy and safety profiles of ADCs.
Fig 1. Comparison of Val-Cit PAB (A) and exo-cleavable linkers (B)
ChemExpress leads the field for ADC drug development providing one-stop CRO & CDMO services for both linkers,payloads and ADC conjugation. We have a substantial inventory of 80+ payloads and 400+ linkers, in addition to 1000+ successful linker compound syntheses. These include hydrophilic polymer scaffolds like PEG, polysarcosine, cyclodextrins, peptides, and polyacetals.
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