Chemical Methods for Peptide and Protein Backbone Cleavage

In biology, the specific enzyme‐mediated cleavage of peptide and protein backbones plays numerous regulatory roles. Being able to mimic the specificity and efficacy of enzymes, using chemical methods, is a grand challenge. Nevertheless, specific chemical cleavage of protein backbones at cysteine residues dates back to the 1960s. In this concept, recent insights and developments in chemical peptide and protein backbone cleavage as well as their applications for the selective manipulation and functionalization of proteins are discussed.