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Design of NK‐2‐derived peptides with improved activity against equine sarcoid cells
Author(s) -
Gross Stephanie,
Wilms Dominik,
Krause Jannike,
Brezesinski Gerald,
Andrä Jörg
Publication year - 2013
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.2540
Subject(s) - chemistry , computational biology , biology
Equine sarcoid is a topically accessible model for the evaluation of anticancer peptides acting by physical membrane disruption avoiding the complexity of a systemic application. We aim at evaluating and improving natural peptides for host defence as lead structures, where we focus on the cationic and amphipathic peptide NK‐2. Cytotoxicity tests, fluorescence microscopy and a chip‐based biosensor, which enabled real‐time monitoring of cell metabolism, were applied. Cancer cell killing was dynamic with an initial phase of increased cellular respiration, followed by membrane destruction. NK‐2 was substantially improved and shortened. Novel peptides exhibited a fivefold improved activity against sarcoid cells, while haemolysis remained almost unaltered. Similar Zeta potential and similar amount of surface phosphatidylserine of sarcoid and normal skin cells are responsible for a lack of selectivity between these two cell types. Copyright © 2013 European Peptide Society and John Wiley & Sons, Ltd.