An adamantyl amino acid containing gramicidin S analogue with broad spectrum antibacterial activity and reduced hemolytic activity

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Kapoerchan, V.V.

Knijnenburg, A.D.

Niamat, M.

Spalburg, E.

Neeling, A.J. de

Nibbering, P.H.

Mars-Groenendijk, R.H.

Noort, D.

Otero, J.M.

Llamas-Saiz, A.L.

Raaij, M.J. van

Marel, G.A. van der

Overkleeft, H.S.

Overhand, M.
The cyclic cationic antimicrobial peptide gramicidin S (GS) is an effective topical antibacterial agent that is toxic for human red blood cells (hemolysis). Herein, we present a series of amphiphilic derivatives of GS with either two or four positive charges and characteristics ranging between very polar and very hydrophobic. Screening of this series of peptide derivatives identified a compound that combines effective antibacterial activity with virtually no toxicity within the same concentration range. This peptide acts against both Gram-negative and Gram-positive bacteria, including several MRSA strains, and represents an interesting lead for the development of a broadly applicable antibiotic. © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Topics




Amino acidsAntibioticsGramicidinMethicillin-resistant Staphylococcus aureus (MRSA)Peptides
TNO Identifier
425161
Repository link
https://resolver.tno.nl/uuid:c94bbca4-ca6e-44e9-84b0-3c95e8f9553d
ISSN
0947-6539
Source
Chemistry - A European Journal, 16(40), pp. 12174-12181.
Pages
12174-12181
Files
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