Preparation of Peptide and Other Biomolecular Conjugates Through Chemoselective Ligations

The synthesis of molecular conjugates through chemoselective ligations represents a very convenient strategy to prepare complex macromolecules with diverse functional elements. Herein, we describe chemical methods based on the preparation of chemoselectively addressable peptides allowing successive oxime ligations and/or alkyne–azide cycloaddition (“click”) reactions of various biomolecules. This modular synthetic approach can be applied to a broad range of purposes.