title: Interaction of a novel antitumor agent TAS-103 with DNA.
abstract: Interaction of a novel antitumor agent TAS-103 with DNA has been studied by a variety of methods including thermal melting study, UV-Visible spectroscopy, 1H- and 31P-NMR spectroscopy. Thermal melting study indicated that TAS-103 stabilizes the double stranded form of DNA and the relative binding strength of TAS-103 is equal to that of ethidium bromide (EtBr). UV-Visible spectroscopy demonstrated that titration curves are nearly identical with all DNA oligomers producing a hypochromic and hypsochromic effect. A hypsochromic effect of TAS-103 is differ from typical intercalators such as EtBr and Actinomycin D that exhibit a bathochromic effect. 1H- and 31P-NMR spectroscopy revealed that TAS-103 has mainly two binding modes. Major binding mode is outside binding and minor binding mode is intercalation.
authors.affiliation: Chemistry Laboratory, Taiho Pharmaceutical Co. Ltd., Saitama, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Ishida
authors.forename: T
authors.initials: T
authors.lastname: Asao
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry* / Q000494:pharmacology; D001483:Base Sequence; D001665:Binding Sites; D004247:DNA / Q000737:chemistry*; D003609:Dactinomycin / Q000737:chemistry; D004996:Ethidium / Q000737:chemistry; D007192:Indenes / Q000737:chemistry* / Q000494:pharmacology; D007364:Intercalating Agents; D019906:Nuclear Magnetic Resonance, Biomolecular; D009690:Nucleic Acid Conformation / Q000187:drug effects; D009691:Nucleic Acid Denaturation; D009838:Oligodeoxyribonucleotides / Q000737:chemistry*; D011067:Poly dA-dT / Q000737:chemistry; D011089:Polydeoxyribonucleotides / Q000737:chemistry; D013053:Spectrophotometry
chemical_list: D000634:Aminoquinolines; D007192:Indenes; D007364:Intercalating Agents; D009838:Oligodeoxyribonucleotides; D011089:Polydeoxyribonucleotides; D003609:Dactinomycin; D011067:Poly dA-dT; C019530:poly(dC-dG); D004247:DNA; D004996:Ethidium; C106647:6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one