title: Synthesis and influenza virus inhibitory activities of carbosilane dendrimers peripherally functionalized with hemagglutinin-binding Peptide.
abstract: A series of carbosilane dendrimers uniformly functionalized with hemagglutinin (HA) binding peptide (sialic acid-mimic peptide, Ala-Arg-Leu-Pro-Arg) was systematically synthesized, and their anti-influenza virus activity was evaluated. The carbosilane-based peptide dendrimers, unlike sialylated dendrimers, cannot be digested by virus neuraminidases. The peptide dendrimers exhibited intriguing biological activities depending on the form of their core frame, with a dumbbell-type peptide dendrimer showing particularly strong inhibitory activities against two human influenza viruses, A/PR/8/34 (H1N1) and A/Aichi/2/68 (H3N2). The IC50 values of the dumbbell-type peptide dendrimer for both strains were 0.60 μM, the highest activity among the HA-binding peptide derivatives. The results suggest that a dumbbell-shaped carbosilane dendrimer is the most suitable core scaffold for HA-binding peptide dendrimers.
authors.affiliation: Division of Materials Science, Graduate School of Science and Technology, Saitama University , 255 Shimo-Ohkubo, Sakura-ku, Saitama 338-8570, Japan.
authors.forename: Ken
authors.initials: K
authors.lastname: Hatano
authors.forename: Teruhiko
authors.initials: T
authors.lastname: Matsubara
authors.forename: Yosuke
authors.initials: Y
authors.lastname: Muramatsu
authors.forename: Masakazu
authors.initials: M
authors.lastname: Ezure
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Koyama
authors.forename: Koji
authors.initials: K
authors.lastname: Matsuoka
authors.forename: Ryunosuke
authors.initials: R
authors.lastname: Kuriyama
authors.forename: Haruka
authors.initials: H
authors.lastname: Kori
authors.forename: Toshinori
authors.initials: T
authors.lastname: Sato
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D050091:Dendrimers / Q000138:chemical synthesis*; D004285:Dogs; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004912:Erythrocytes / Q000187:drug effects; D006388:Hemagglutinins / Q000378:metabolism; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects; D020128:Inhibitory Concentration 50; D061985:Madin Darby Canine Kidney Cells / Q000187:drug effects / Q000821:virology; D009975:Orthomyxoviridae / Q000187:drug effects*; D012821:Silanes / Q000737:chemistry*
chemical_list: D000998:Antiviral Agents; D050091:Dendrimers; D006388:Hemagglutinins; D012821:Silanes; C504072:carbosilane