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• W2079486099 startingPage "12783" @default.
• W2079486099 abstract "The development of small molecules that bind DNA sequence specifically has the potential to modulate gene expression in a general way. One mode of DNA binding is intercalation, or the insertion of molecules between DNA base pairs. We have developed a modular polyintercalation system in which intercalating naphthalene diimide (NDI) units are connected by flexible linkers that alternate between the minor and major grooves of DNA when bound. We recently reported a threading tetraintercalator with a dissociation half-life of 16 days, the longest reported to date, from its preferred 14 bp binding site. Herein, three new tetraintercalator derivatives were synthesized with one, two, and three additional methylene units in the central major groove-binding linker. These molecules displayed dissociation half-lives of 57, 27, and 18 days, respectively, from the 14 bp site. The optimal major groove-binding linker was used in the design of an NDI hexaintercalator that was analyzed by gel-shift assays, DNase I footprinting, and UV-vis spectroscopy. The hexaintercalator bound its entire 22 bp binding site, the longest reported specific binding site for a synthetic, non-nucleic acid-based DNA binding molecule, but with a significantly faster dissociation rate compared to the tetraintercalators." @default.
• W2079486099 created "2016-06-24" @default.
• W2079486099 creator A5001186757 @default.
• W2079486099 creator A5056732850 @default.
• W2079486099 date "2013-08-20" @default.
• W2079486099 modified "2023-10-08" @default.
• W2079486099 title "Threading Polyintercalators with Extremely Slow Dissociation Rates and Extended DNA Binding Sites" @default.
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• W2079486099 doi "https://doi.org/10.1021/ja4057344" @default.
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• W2079486099 hasPublicationYear "2013" @default.
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