title: Enhancing membrane disruption by targeting and multivalent presentation of antimicrobial peptides.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry and Chemical Biology, Utrecht University, Utrecht, The Netherlands.
authors.forename: Cristina
authors.initials: C
authors.lastname: Chamorro
authors.forename: Marcel A
authors.initials: MA
authors.lastname: Boerman
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Arnusch
authors.forename: Eefjan
authors.initials: E
authors.lastname: Breukink
authors.forename: Roland J
authors.initials: RJ
authors.lastname: Pieters
mesh_terms: D023181:Antimicrobial Cationic Peptides / Q000138:chemical synthesis / Q000737:chemistry*; D001703:Biophysics / Q000379:methods; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D015195:Drug Design; D005452:Fluoresceins / Q000737:chemistry; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D008956:Models, Chemical; D010455:Peptides / Q000737:chemistry; D010713:Phosphatidylcholines / Q000737:chemistry; D010715:Phosphatidylglycerols / Q000737:chemistry; D011506:Proteins / Q000138:chemical synthesis* / Q000737:chemistry; D014640:Vancomycin / Q000737:chemistry; D014862:Wasp Venoms / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D023181:Antimicrobial Cationic Peptides; D005452:Fluoresceins; D008055:Lipids; D010455:Peptides; D010713:Phosphatidylcholines; D010715:Phosphatidylglycerols; D011506:Proteins; D014862:Wasp Venoms; C443041:anoplin; C104501:temporin; C024098:6-carboxyfluorescein; C051388:1,2-dioleoyl-sn-glycero-3-phosphoglycerol; D014640:Vancomycin; C017251:1,2-oleoylphosphatidylcholine