Copper-Free Click Chemistry Modification of Nanovectors for Integrin-Targeted Cancer Therapy

Strain-promoted azide-alkyne cycloaddition (SPAAC) click chemistry is the chemical reaction between azide and cyclooctyne groups. This reaction can conjugate biological molecules, such as peptides, in a highly selective way under mild conditions without cross-reaction with the most widely existing reactive groups, such as amine, carboxylic acid, and hydroxide. Thus, the SPAAC reaction is very versatile for biomolecules conjugation. In this book chapter, we provide detailed protocols of conjugation of integrin targeting peptides to either amine or carboxylic acid terminated porous silicon nanovectors by SPAAC, which can be used to enhance the cellular uptake for intracellular cancer drug delivery and for in vivo cancer theranostics.