What goes around comes around-a comparative study of the influence of chemical modifications on the antimicrobial properties of small cyclic peptides

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dc.contributor.authorScheinpflug, Kathien_ZA
dc.contributor.authorNikolenko, Heikeen_ZA
dc.contributor.authorKomarov, Igor V.en_ZA
dc.contributor.authorRautenbach, Marinaen_ZA
dc.contributor.authorDathe, Margittaen_ZA
dc.date.accessioned2014-07-06T17:35:01Z
dc.date.available2014-07-06T17:35:01Z
dc.date.issued2013
dc.descriptionCITATION: Scheinpflug, K., et al. 2013. What goes around comes around-a comparative study of the influence of chemical modifications on the antimicrobial properties of small cyclic peptides. Pharmaceuticals, 6(9):1130-1144, doi:10.3390/ph6091130.en_ZA
dc.descriptionThe original publication is available at http://www.mdpi.comen_ZA
dc.description.abstractTryptophan and arginine-rich cyclic hexapeptides of the type cyclo-RRRWFW combine high antibacterial activity with rapid cell killing kinetics, but show low toxicity in human cell lines. The peptides fulfil the structural requirements for membrane interaction such as high amphipathicity and cationic charge, but membrane permeabilisation, which is the most common mode of action of antimicrobial peptides (AMPs), could not be observed. Our current studies focus on elucidating a putative membrane translocation mechanism whereupon the peptides might interfere with intracellular processes. These investigations require particular analytical tools: fluorescent analogues and peptides bearing appropriate reactive groups were synthesized and characterized in order to be used in confocal laser scanning microscopy and HPLC analysis. We found that minimal changes in both the cationic and hydrophobic domain of the peptides in most cases led to significant reduction of antimicrobial activity and/or changes in the mode of action. However, we were able to identify two modified peptides which exhibited properties similar to those of the cyclic parent hexapeptide and are suitable for subsequent studies on membrane translocation and uptake into bacterial cellsen_ZA
dc.description.urihttp://www.mdpi.com/1424-8247/6/9/1130
dc.description.versionPublisher's versionen_ZA
dc.format.extent15 pages : illustrationsen_ZA
dc.identifier.citationScheinpflug, K., et al. 2013. What goes around comes around-a comparative study of the influence of chemical modifications on the antimicrobial properties of small cyclic peptides. Pharmaceuticals, 6(9):1130-1144, doi:10.3390/ph6091130en_ZA
dc.identifier.issn1424-8247 (online)
dc.identifier.otherdoi:10.3390/ph6091130
dc.identifier.urihttp://hdl.handle.net/10019.1/90594
dc.language.isoen_ZAen_ZA
dc.publisherMDPIen_ZA
dc.rights.holderAuthors retain copyrighten_ZA
dc.subjectCyclic hexapeptidesen_ZA
dc.subjectAntimicrobial peptidesen_ZA
dc.subjectChemical modificationen_ZA
dc.subjectMembrane permeabilisationen_ZA
dc.titleWhat goes around comes around-a comparative study of the influence of chemical modifications on the antimicrobial properties of small cyclic peptidesen_ZA
dc.typeArticleen_ZA
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