One-pot approach to well-defined biomolecular assemblies by orthogonal chemoselective ligations.

Click-click cyclopeptides: Well-defined biomolecular assemblies are synthesized using orthogonal oxime bond formation and copper(I)-mediated alkyne-azide cycloaddition reactions in a stepwise or in a one-pot approach. To illustrate this strategy, regioselective ligation of biologically relevant peptides onto a cyclopeptidic scaffold was performed.