Synthesis of anticancer heptapeptides containing a unique lipophilic β 2,2 ‐amino acid building block

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 pote...

Full description

Saved in:
Bibliographic Details
Published in:Journal of peptide science 2012-03, Vol.18 (3), p.170-176
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
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:1075-2617
1099-1387
DOI:10.1002/psc.1434