作者: Satoshi Obika , Takeshi Uneda , Tomomi Sugimoto , Daishu Nanbu , Takashi Minami
DOI: 10.1016/S0968-0896(00)00325-4
关键词: Chemistry 、 Binding constant 、 Molecule 、 Methylene 、 Chemical synthesis 、 Bicyclic molecule 、 Stereochemistry 、 Oligonucleotide 、 Biological activity 、 Biochemistry 、 Bridged nucleic acid
摘要: Abstract For development of ideal antisense and antigene molecules, various chemical modifications oligonucleotides have been studied. However, despite their importance, there is only limited information available on the triplex-forming ability conformationally restricted or locked oligonucleotides. We report herein that 2′-O,4′-C-methylene bridged nucleic acid (2′,4′-BNA) modification oligonucleotide (TFO) significantly enhances binding affinity towards target dsDNA. On Tm measurements, triplex with 2′,4′-BNA were found to be stabilized ΔTm/modification +4.3 +5 °C at pH 6.6 compared triplexes unmodified oligonucleotide. By means gel-retardation assay, constant 7.0 was least 300-fold higher than natural In addition, clearly showed inhibition NF-κB transcription factor (p50)-target dsDNA by forming a stable 7.0.