Multivalent NHS-activated acrylates for orthogonal site-selective functionalisation of peptides at cysteine residues.

The site-selective chemical appendage of multiple functionalities on a native peptide backbone is a highly demanding and complex tool of modern chemical biology. Here, novel NHS-activated acrylates were designed to hold various payloads in a single bioconjugation handle that is able to site-selectively and orthogonally target the N -terminal cysteine of peptides.