title: Cellular uptake of covalent conjugates of oligonucleotide with membrane-modifying peptide, peptaibol.
abstract: Using the membrane-modifying peptide, trichorovin-XIIa (TV-XIIa), which is an 11-residual peptaibol isolated from the fungus Trichoderma viride, we synthesized covalent conjugates of 20-mer oligonucleotide with TV-XIIa to examine the potential use of TV-XIIa in cellular delivery. The results indicated that the conjugates were progressively taken up by human lung carcinoma A549 cells. Next, the antisense effects of the conjugates on p53 protein expression were examined. The p53 expression was significantly decreased by ca. 20-50% in the presence of the conjugates upon treatment with the transfection solution at the concentration of 5 μM.
authors.affiliation: Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan. wada@gly.oups.ac.jp
authors.forename: Shun-ichi
authors.initials: S
authors.lastname: Wada
authors.forename: Yasunari
authors.initials: Y
authors.lastname: Hitora
authors.forename: Saori
authors.initials: S
authors.lastname: Yokoe
authors.forename: Osamu
authors.initials: O
authors.lastname: Nakagawa
authors.forename: Hidehito
authors.initials: H
authors.lastname: Urata
mesh_terms: D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D018613:Microscopy, Confocal; D016376:Oligonucleotides, Antisense / Q000737:chemistry* / Q000494:pharmacology; D054848:Peptaibols / Q000737:chemistry* / Q000378:metabolism; D010455:Peptides / Q000737:chemistry / Q000378:metabolism; D016159:Tumor Suppressor Protein p53 / Q000378:metabolism
chemical_list: D016376:Oligonucleotides, Antisense; D054848:Peptaibols; D010455:Peptides; D016159:Tumor Suppressor Protein p53; C532914:trichorovin-XIIa