| |  Online-Ressource |
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| Verfasst von: | Storck, Philip [VerfasserIn]  |
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| | Umstätter, Florian [VerfasserIn] |
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| | Wohlfart, Sabrina [VerfasserIn] |
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| | Domhan, Cornelius [VerfasserIn] |
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| | Kleist, Christian [VerfasserIn] |
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| | Werner, Julia [VerfasserIn] |
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| | Brandenburg, Klaus [VerfasserIn] |
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| | Zimmermann, Stefan [VerfasserIn] |
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| | Haberkorn, Uwe [VerfasserIn] |
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| | Mier, Walter [VerfasserIn] |
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| | Uhl, Philipp [VerfasserIn] |
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| Titel: | Fatty acid conjugation leads to length-dependent antimicrobial activity of a synthetic antibacterial peptide (Pep19-4LF) |
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| Verf.angabe: | Philip Storck, Florian Umstätter, Sabrina Wohlfart, Cornelius Domhan, Christian Kleist, Julia Werner, Klaus Brandenburg, Stefan Zimmermann, Uwe Haberkorn, Walter Mier and Philipp Uhl |
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| E-Jahr: | 2020 |
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| Jahr: | 26 November 2020 |
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| Umfang: | 12 S. |
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| Fussnoten: | Gesehen am 15.02.2022 |
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| Titel Quelle: | Enthalten in: Antibiotics |
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| Ort Quelle: | Basel : MDPI, 2012 |
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| Jahr Quelle: | 2020 |
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| Band/Heft Quelle: | 9(2020), 12, Artikel-ID 844, Seite 1-12 |
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| ISSN Quelle: | 2079-6382 |
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| Abstract: | The increasing number of infections caused by multidrug-resistant bacteria requires an intensified search for new antibiotics. Pep19-4LF is a synthetic antimicrobial peptide (GKKYRRFRWKFKGKLFLFG) that was previously designed with the main focus on high antimicrobial activity. The hydrophobic motif, LFLFG, was found to be essential for antimicrobial activity. However, this motif shows several limitations such as aggregation in biological media, low solubility, and small yields in peptide synthesis. In order to obtain more appropriate peptide characteristics, the hydrophobic motif was replaced with fatty acids. For this purpose, a shortened variant of Pep19-4LF (Pep19-short; GKKYRRFRWKFKGK) was synthesized and covalently linked to saturated fatty acids of different chain lengths. The peptide conjugates were tested with respect to their antibacterial activity by microdilution experiments on different bacterial strains. The length of the fatty acid was found to be directly correlated to the antimicrobial activity up to an ideal chain length (undecanoic acid, C11:0). This conjugate showed high antimicrobial activity in absence of toxicity. Time-kill studies revealed a fast and bactericidal mode of action. Furthermore, the first in vivo experiments of the conjugate in rodents demonstrated pharmacokinetics appropriate for application as a drug. These results clearly indicate that the hydrophobic motif of the peptide can be replaced by a single fatty acid of medium length, simplifying the design of this antimicrobial peptide while retaining high antimicrobial activity in the absence of toxicity. |
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| DOI: | doi:10.3390/antibiotics9120844 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.3390/antibiotics9120844 |
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| | Volltext: https://www.mdpi.com/2079-6382/9/12/844 |
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| | DOI: https://doi.org/10.3390/antibiotics9120844 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | <i>Enterococcus faecium</i> |
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| | <i>Staphylococcus aureus</i> |
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| | antimicrobial activity |
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| | fatty acid conjugation |
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| | synthetic antimicrobial peptides |
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| K10plus-PPN: | 1789584760 |
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| Verknüpfungen: | → Zeitschrift |
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Fatty acid conjugation leads to length-dependent antimicrobial activity of a synthetic antibacterial peptide (Pep19-4LF) / Storck, Philip [VerfasserIn]; 26 November 2020 (Online-Ressource)
