An Adamantyl Amino Acid Containing Gramicidin S Analogue with Broad Spectrum Antibacterial Activity and Reduced Hemolytic Activity
✍ Scribed by Dr. Varsha V. Kapoerchan; Dr. Annemiek D. Knijnenburg; Miquel Niamat; Emile Spalburg; Dr. Albert J. de Neeling; Dr. Peter H. Nibbering; Roos H. Mars-Groenendijk; Dr. Daan Noort; José M. Otero; Dr. Antonio L. Llamas-Saiz; Dr. Mark J. van Raaij; Prof. Dr. Gijs A. van der Marel; Prof. Dr. Herman S. Overkleeft; Dr. Mark Overhand
- Book ID
- 101836344
- Publisher
- John Wiley and Sons
- Year
- 2010
- Tongue
- English
- Weight
- 437 KB
- Volume
- 16
- Category
- Article
- ISSN
- 0947-6539
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✦ Synopsis
Abstract
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.