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This is of particular interest in the field of peptide drug development. Methods that enable straightforward modification of peptides with non\u2010canonical residues are therefore in high demand. On\u2010resin late\u2010stage functionalization is a powerful, cost\u2010 and time\u2010efficient tool for modifying peptides. It also allows for high\u2010throughput experimentation, making it well suited to streamlining the development of peptide therapeutics. In this minireview, we provide an overview of the chemical approaches for on\u2010resin late\u2010stage peptide functionalization , most of which have been developed over the past decade. These reactions range from nucleophilic substitution and carbonyl chemistry to metal catalysis and photocatalysis. Many of the presented approaches have been shown to be compatible with short and long peptides, and to modulate their bioactivity. 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