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Synthesis of anticancer heptapeptides containing a unique lipophilic β2,2-amino acid building block

✍ Scribed by Veronika Tørfoss; Dominik Ausbacher; Cristiane de A. Cavalcanti-Jacobsen; Terkel Hansen; Bjørn-Olav Brandsdal; Martina Havelkova; Morten B. Strøm

Book ID
105360054
Publisher
John Wiley and Sons
Year
2012
Tongue
English
Weight
230 KB
Volume
18
Category
Article
ISSN
1075-2617

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✦ Synopsis

We report a series of synthetic anticancer heptapeptides (H‐KKW__β__^2,2^WKK‐NH~2~) containing eight different central lipophilic β^2,2^‐amino acid building blocks, which have demonstrated high efficiency when used as scaffolds in small cationic antimicrobial peptides and peptidomimetics. The most potent peptides in the present study had IC~50~ values of 9–23 µm against human Burkitt's lymphoma and murine B‐cell lymphoma and were all nonhaemolytic (EC~50~ > 200 µm). The most promising peptide 10e also demonstrated low toxicity against human embryonic lung fibroblast cells and peripheral blood mononuclear cells and exceptional proteolytic stability. Copyright © 2012 European Peptide Society and John Wiley & Sons, Ltd.

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