title: Synthesis and biological evaluation of gramicidin S dimers.
abstract: The design and synthesis of analogues of the cyclic beta-sheet gramicidin S (GS), having additional functionalities in their turn regions, is reported. The monomeric GS analogues were transformed into dimers and their activities towards biological membranes, through antimicriobial and hemolytic assays, were evaluated. Finally, conductivity measurements have been performed to elucidate ion channel forming properties.
authors.affiliation: Leiden Institute of Chemistry, Gorlaeus Laboratories, P. O. Box 9502, 2300, RA Leiden, The Netherlands.
authors.forename: Gijsbert M
authors.initials: GM
authors.lastname: Grotenbreg
authors.forename: Martin D
authors.initials: MD
authors.lastname: Witte
authors.forename: Peter A V
authors.initials: PA
authors.lastname: van Hoof
authors.forename: Emile
authors.initials: E
authors.lastname: Spalburg
authors.forename: Philipp
authors.initials: P
authors.lastname: Reiss
authors.forename: Daan
authors.initials: D
authors.lastname: Noort
authors.forename: Albert J
authors.initials: AJ
authors.lastname: de Neeling
authors.forename: Ulrich
authors.initials: U
authors.lastname: Koert
authors.forename: Gijsbert A
authors.initials: GA
authors.lastname: van der Marel
authors.forename: Herman S
authors.initials: HS
authors.lastname: Overkleeft
authors.forename: Mark
authors.initials: M
authors.lastname: Overhand
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D019281:Dimerization; D006096:Gramicidin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006461:Hemolysis; D007473:Ion Channels / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D007473:Ion Channels; D006096:Gramicidin