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Effect of hydrocarbon stapling on the properties of alpha-helical antimicrobial peptides isolated from the venom of hymenoptera

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    0384565 - ÚOCHB 2013 RIV AT eng J - Journal Article
    Chapuis, Hubert Jean - Slaninová, Jiřina - Bednárová, Lucie - Monincová, Lenka - Buděšínský, Miloš - Čeřovský, Václav
    Effect of hydrocarbon stapling on the properties of alpha-helical antimicrobial peptides isolated from the venom of hymenoptera.
    Amino Acids. Roč. 43, č. 5 (2012), s. 2047-2058. ISSN 0939-4451. E-ISSN 1438-2199
    R&D Projects: GA ČR GA203/08/0536
    Institutional research plan: CEZ:AV0Z40550506
    Keywords : antimicrobial peptides * stapled peptides * amphipathic helix * CD spectroscopy
    Subject RIV: CC - Organic Chemistry
    Impact factor: 3.914, year: 2012

    Introducing all-hydrocarbon staples into short alpha-helical amphipathic antimicrobial peptides increases their hydrophobicity, hydrophobic moment, rigidity and generally alpha-helicity in water. Stapling generally makes the peptides more resistant to proteolytic degradation, particularly those that are doubly stapled. The introduction of olefinic amino acid residues and conformational restriction by stapling make the peptides significantly more hemolytic, and lead to a decrease of their antimicrobial potency against pathogenic bacteria. Unfortunately, the stapling of those peptides is not rendering compounds that would have better pharmacological qualities than the native unmodified potent peptides.
    Permanent Link: http://hdl.handle.net/11104/0007467

     
     
Number of the records: 1  

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