Synthesis of anticancer heptapeptides containing a unique lipophilic β(2,2) -amino acid building block

We report a series of synthetic anticancer heptapeptides (H-KKWβ(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 pot...

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Bibliographic Details
Published in:Journal of peptide science 2012-03, Vol.18 (3), p.170
Main Authors: Tørfoss, Veronika, Ausbacher, Dominik, Cavalcanti-Jacobsen, Cristiane de A, Hansen, Terkel, Brandsdal, Bjørn-Olav, Havelkova, Martina, Strøm, Morten B
Format: Article
Language:English
Subjects:
Amino Acids - chemistry
Animals
Antineoplastic Agents - chemical synthesis
Burkitt Lymphoma
Cell Line, Tumor
Humans
Inhibitory Concentration 50
Leukocytes, Mononuclear
Lymphoma, B-Cell
Mice
Oligopeptides - chemical synthesis
Oligopeptides - pharmacology
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Summary:We report a series of synthetic anticancer heptapeptides (H-KKWβ(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.
ISSN:1099-1387
DOI:10.1002/psc.1434