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Integrin Targeting Systems for Tumor Diagnosis and Therapy pp 35–49Cite as

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

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Part of the book series: Methods in Pharmacology and Toxicology ((MIPT))

Abstract

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.

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Acknowledgements

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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Authors and Affiliations

  1. Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, 00014, Helsinki, Finland

    Chang-Fang Wang & Hélder A. Santos

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  1. Chang-Fang Wang
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  2. Hélder A. Santos
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Correspondence to Hélder A. Santos .

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Editors and Affiliations

  1. Department of Gastroenterology and Hepatology, UniversitätsSpital Zürich, Zürich, Switzerland

    Eleonora Patsenker

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Wang, CF., Santos, H.A. (2015). Copper-Free Click Chemistry Modification of Nanovectors for Integrin-Targeted Cancer Therapy. In: Patsenker, E. (eds) Integrin Targeting Systems for Tumor Diagnosis and Therapy. Methods in Pharmacology and Toxicology. Humana Press, New York, NY. https://doi.org/10.1007/7653_2015_44

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  • DOI: https://doi.org/10.1007/7653_2015_44

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  • Publisher Name: Humana Press, New York, NY

  • Print ISBN: 978-1-4939-7443-6

  • Online ISBN: 978-1-4939-7445-0

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