title: Nucleobase modified neamines with a lysine as a linker, their inhibition specificity for TAR-Tat derived from HIV-1.
abstract: Nucleobase modified neamines with a lysine as the linker (NbK-neamines) were synthesized and their binding toward hairpin RNAs derived from HIV-1 activator region were studied. NbK-neamines were bind those RNAs with micro molar level of binding affinities and compete with corresponding activator peptide for TAR RNA, but not for RRE RNA. GbK-neamine denotes the highest binding affinity with TAR RNA, three to five times higher than other three NbK-neamines. GbK-neamine could be a candidate of potential inhibitor for TAR-Tat.
authors.affiliation: Shibaura Institute of Technology, Department of Applied Chemistry, Toyosu 3-7-5, Koto-ku, Tokyo 138-8548, Japan.
authors.forename: Ryo
authors.initials: R
authors.lastname: Inoue
authors.affiliation: Shibaura Institute of Technology, Department of Applied Chemistry, Toyosu 3-7-5, Koto-ku, Tokyo 138-8548, Japan.
authors.forename: Kentarou
authors.initials: K
authors.lastname: Watanabe
authors.affiliation: Shibaura Institute of Technology, Department of Applied Chemistry, Toyosu 3-7-5, Koto-ku, Tokyo 138-8548, Japan.
authors.forename: Toyofusa
authors.initials: T
authors.lastname: Katou
authors.affiliation: Shibaura Institute of Technology, Department of Applied Chemistry, Toyosu 3-7-5, Koto-ku, Tokyo 138-8548, Japan.
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Ikezawa
authors.affiliation: Shibaura Institute of Technology, Department of Applied Chemistry, Toyosu 3-7-5, Koto-ku, Tokyo 138-8548, Japan. Electronic address: hamie@shibaura-it.ac.jp.
authors.forename: Keita
authors.initials: K
authors.lastname: Hamasaki
mesh_terms: D000225:Adenine / Q000737:chemistry; D003596:Cytosine / Q000737:chemistry; D005601:Framycetin / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006147:Guanine / Q000737:chemistry; D016325:HIV Long Terminal Repeat / Q000187:drug effects*; D015497:HIV-1 / Q000737:chemistry* / Q000235:genetics*; D008239:Lysine / Q000737:chemistry*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013941:Thymine / Q000737:chemistry; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000037:antagonists & inhibitors*
chemical_list: D054322:tat Gene Products, Human Immunodeficiency Virus; D005601:Framycetin; C488396:neamine; D006147:Guanine; D003596:Cytosine; D000225:Adenine; D008239:Lysine; D013941:Thymine
keywords: Aminoglycoside; Neamine; Nucleobase; Potential inhibitor; RRE RNA; TAR RNA