Title
Inverted analogs of the antibiotic gramicidin S with an improved biological profile
Author
Kapoerchan, V.V.
Knijnenburg, A.D.
Keizer, P.
Spalburg, E.
de Neeling, A.J.
Mars-Groenendijk, R.H.
Noort, D.
Otero, J.M.
Llamas-Saiz, A.L.
van Raaij, M.J.
van der Marel, G.A.
Overkleeft, H.S.
Overhand, M.
Publication year
2012
Abstract
A series of gramicidin S derivatives 4-15 are presented that have four ornithine residues as polar protonated side chains and two central hydrophobic amino acids with unaltered turn regions. These peptides were screened against human erthrocytes and our standard panel of Gram negative- and Gram positive bacteria, including four MRSA strains. Based on the antibacterial- and hemolytic data, peptides 13 and 14 have an improved biological profile compared to the clinically applied topical antibiotic gramicidin S. © 2012 Elsevier Ltd. All rights reserved.
Subject
Life
CBRN - CBRN Protection
EELS - Earth, Environmental and Life Sciences
Healthy Living
Antibiotics
Cyclic peptide
Hemolysis
Improved properties
MRSA
To reference this document use:
http://resolver.tudelft.nl/uuid:2cfe4523-f756-43fc-a15e-0afb83dcd160
DOI
https://doi.org/10.1016/j.bmc.2012.08.038
TNO identifier
465237
ISSN
0968-0896
Source
Bioorganic and Medicinal Chemistry, 20 (20), 6059-6062
Document type
article