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Synthesis of anticancer heptapeptides containing a unique lipophilic β 2,2 ‐amino acid building block
Author(s) -
Tørfoss Veronika,
Ausbacher Dominik,
CavalcantiJacobsen Cristiane de A.,
Hansen Terkel,
Brandsdal BjørnOlav,
Havelkova Martina,
Strøm Morten B.
Publication year - 2012
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.1434
Subject(s) - peptide , peptidomimetic , chemistry , amino acid , fibroblast , peripheral blood mononuclear cell , embryonic stem cell , biochemistry , microbiology and biotechnology , combinatorial chemistry , stereochemistry , in vitro , biology , gene
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 µ m against human Burkitt's lymphoma and murine B‐cell lymphoma and were all nonhaemolytic (EC 50 > 200 µ m ). 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.