Enhancing membrane disruption by targeting and multivalent presentation of antimicrobial peptides

In order to enhance the membrane disruption of antimicrobial peptides both targeting and multivalent presentation approaches were explored. The antimicrobial peptides anoplin and temporin L were conjugated via click chemistry to vancomycin and to di- and tetravalent dendrimers. The vancomycin unit led to enhanced membrane disruption of large unilamellar vesicles (LUVs) displaying the vancomycin target lipid II, but only for temporin L and not for anoplin. The multivalent presentation led to enhanced LUV membrane disruption in the case of anoplin but not for temporin L.

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► A targeting unit was attached to antimicrobial peptides.
► Antimicrobial peptides were attached to a dendrimer.
► The targeting unit made temporin L more active but not anaoplin.
► The dendimer linkage made anoplin more active but not temporin L.