Towards Peptide Vasodilators as Anticancer Drug Delivery Vehicles

摘要

Controlled drug release has been studied in depth for many years aiming for the treatment of cancer. Although there are a number of methods that have been successful, they often come with unwanted side effects. Bradykinin (BK) offers potential as a targeting vehicle in the fight against cancer. Composites of BK with the carrier potential of cyclodextrin and the advantages of sulfonamide drugs have great potential for successful drug targeting [1,2]. Herein we report for the first time the selective derivatisation of beta-cyclodextrin (β-CD) with a series of model peptides using solid phase peptide synthesis. This versatile and robust method enables the attachment of one or more peptides using SPPS (and solution synthesis if desired) by the selective removal of the Fmocprotecting group. This versatility allows for the addition and growth of C- and/or N-terminal peptides with the same and/or different functional properties (Figure 1). Peptide attachment of resin in solution using stepwise or ligation synthetic protocols is also possible.