2′-O,4′-C-methylene bridged nucleic acid (2′,4′-BNA)

Satoshi Obika, Takeshi Uneda, Tomomi Sugimoto, Daishu Nanbu, Takashi Minami, Takefumi Doi, Takeshi Imanishi

doi:10.1016/s0968-0896(00)00325-4

For development of ideal antisense and antigene molecules, various chemical modifications of oligonucleotides have been studied. However, despite their importance, there is only limited information available on the triplex-forming ability of the conformationally restricted or locked oligonucleotides. We report herein that 2'-O,4'-C-methylene bridged nucleic acid (2',4'-BNA) modification of triplex-forming oligonucleotide (TFO) significantly enhances the binding affinity towards target dsDNA. On Tm measurements, the triplex with the 2',4'-BNA oligonucleotides were found to be stabilized with deltaTm/modification of +4.3 to +5 degrees C at pH 6.6 compared to the triplexes with the unmodified oligonucleotide. By means of gel-retardation assay, the binding constant of the 2',4'-BNA oligonucleotide at pH 7.0 was at least 300-fold higher than that of the natural oligonucleotide. In addition, the 2',4'-BNA oligonucleotide clearly showed the inhibition of the NF-kappaB transcription factor (p50)-target dsDNA binding by forming a stable triplex at pH 7.0.

2′-O,4′-C-methylene bridged nucleic acid (2′,4′-BNA)

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2′-O,4′-C-methylene bridged nucleic acid (2′,4′-BNA)

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この論文をさがす

説明

収録刊行物

被引用文献 (20)*注記

キーワード

詳細情報 詳細情報について

書き出し

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