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

  • Chang-Fang Wang
  • Hélder A. SantosEmail author
Part of the Methods in Pharmacology and Toxicology book series (MIPT)


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.


Copper-free click chemistry Peptide conjugation Integrin Targeting drug delivery Nanomedicine Cancer therapy 



Financial support from Academy of Finland (decision nos. 252215 and 281300), University of Helsinki Research Funds, Biocentrum Helsinki, and European Research Council (grant no. 310892).


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  1. 1.Division of Pharmaceutical Chemistry and Technology, Faculty of PharmacyUniversity of HelsinkiHelsinkiFinland

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