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Published on: December 23, 2016
Peptide-Pegylated Lipid Conjugation Via Copper-Catalyzed Alkyne-Azide 1,3-Dipolar Cycloaddition
Waleed M Hussein1, Istvan Toth2
1School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, QLD, Australia. w.hussein@uq.edu.au.
Abstract:
Targeted drug delivery is an important strategy in the treatment of many diseases. However, cancer cells are very difficult to target, making this a substantial obstacle in chemotherapy treatment. Bombesin fragment (BBN(6-14)) has been found to target gastrin-releasing peptide receptor (GRPR), which is overexpressed in many cancer cells. In this chapter, BBN peptide was used as a targeting moiety on the surface of polymeric-based nanoparticles to deliver its payload into prostate cancer PC-3 cell lines. Copper-catalyzed alkyne-azide 1,3-dipolar cycloaddition (CuAAC) click reaction was utilized to link the BBN peptide with an alkyne derivative of Pegylated lipid.
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