→2025   →2024   →バックナンバー

2025

■論文

Separation of deaminated impurities from the desired oligonucleotides using supercritical fluid chromatography
Momoka Hayashida, Risa Suzuki, Shinnosuke Horie, Junichi Masuda, Takao Yamaguchi, Satoshi Obika
J. Chromatogr. A 1744 465731

Synthesis and structural analysis of dinucleotides containing 2′,3′-trans-bridged nucleic acids with trans-5,6- or 5,7-fused ring skeleton
T. Osawa, R. Nakanishi, K. Uda, S. Muramoto, S. Obika
Commun. Chem 8 87

Antisense oligonucleotide targeting nicotinamide N-methyltransferase exhibits antitumor effects
T. Hara, S. Meng, Y. Kasahara, T. Osawa, D. Motooka, H. Sato, Y. Arao, Y. Saito, K. Inoue, Y. Hamano, Y. Doki, H. Eguchi, S. Obika, H. Ishii
Mol. Ther. Nucleic Acids 36(2) 102548

Effects of acid-mediated deamination of cytidine and 5-methylcytidine on solid-phase synthesis of oligonucleotides
Y. Isono, C. Karasugi, T. Akisawa, T. Osawa, Q. Ren, M. Tatsuno, F. Ito, T. Inoue, J. Kawakami, S. Obika, M. Shinoda
Tetrahedron 185 134840

Phthalimide: a potential warhead for switchable and bioorthogonal conjugation
Kosuke Chiba, Takumi Yoshida, Kana Okada, Minory Ishikawa, Yuichi Hashimoto, Satoshi Obika, Takao Yamaguchi
Chem. Commun. 61 13417–13420

■総説

Developing Methods for the Synthesis of Ligand–Oligonucleotide Conjugates for Drug Discovery Applications
T. Osawa
Chem. Pharm. Bull. 73 762–771

■著書

未来の核酸医薬に貢献できる技術開発を目指して
大澤昂志
生産と技術 77 57–59

2024

■論文

Light-controllable cell-membrane disturbance for intracellular delivery
W. Huo, K. Miki, H. Mu, T. Osawa, H. Yamaguma, Y. Kasahara, S. Obika, Y. Kawaguchi, H. Hirose, S. Futaki, Y. Miyazaki, W. Shinoda, S. Akai, K. Ohe
J. Mater. Chem. B, 12(17), 4138–4147.

A novel transient receptor potential C3/C6 selective activator induces the cellular uptake of antisense oligonucleotides
H. Kohashi, R. Nagata, Y. Tamenori, T. Amatani, Y. Ueda, Y. Mori, Y. Kasahara, S. Obika, M. Shimojo
Nucleic Acids Res.

Separation of the diastereomers of phosphorothioated siRNAs by anion-exchange chromatography under non-denaturing conditions
H. Togawa, T. Okubo, K. Horiuchi, T. Yamaguchi, E. Tomita-Sudo, T. Akita, J. Kawakami, S. Obika
J. Chromatogr. A, 1721, 464847.

Favorable Efficacy and Reduced Acute Neurotoxicity by Antisense Oligonucleotides with 2',4'-BNA/LNA with 9-(aminoethoxy)phenoxazine
T. Matsubayashi, K. Yoshioka, S. S. L. Mon, M. Katsuyama, C. Jia, T. Yamaguchi, R. Iwata-Hara, T. Nagata, O. Nakagawa, S. Obika, T. Yokota
Mol. Ther. Nucleic Acids

Synthesis of coumarin-conjugated oligonucleotides via Knoevenagel condensation to prepare an oligonucleotide library
T. Osawa, S. Obika
Chem. Pharm. Bull., 72(2), 143–148.

Synthesis, duplex-forming ability, and enzymatic stability of oligonucleotides modified with amide-linked dinucleotides containing a 3′,4′-tetrahydropyran-bridged nucleic acid
T. Osawa, T. Akino, S. Obika
J. Org. Chem. 89(1), 269–280.

Development of a simple purification method for oligonucleotides synthesized by using a phosphoramidite for 5'-end modification as a capping reagent
Q. Ren, T. Osawa, S. Obika
Tetrahedron, 150, 133774.

Introduction of sugar-modified nucleotides into CpG-containing antisense oligonucleotides inhibits TLR9 activation
Tokuyuki Yoshida, Tomoko Hagihara, Yasunori Uchida, Yoshiyuki Horiuchi, Kiyomi Sasaki, Takenori Yamamoto, Takuma Yamashita, Yukihiro Goda, Yoshiro Saito, Takao Yamaguchi, Satoshi Obika, Seiji Yamamoto and Takao Inoue
Sci. Rep. 14 11540

In vitro screening of chemically synthesized dipeptide-antisense oligonucleotide conjugates to identify ligand molecules enhancing their activity
T. Osawa, R. Kita, Y. Kasahara, H. Yamaguma, T. Nakayama, H. Kamada, S. Obika
Bioorg. Med. Chem. 110 117814

THF peroxide as a factor in generating desulphurised products from the solid-phase synthesis of phosphorothioate-modified oligonucleotides
Q. Ren, T. Osawa, M. Tatsuno, S. Obika
RSC Adv. 14(30) 21590–21596

Separation and characterization of therapeutic oligonucleotide isomer impurities by cyclic ion mobility-mass spectrometry
S. Omuro, T. Yamaguchi, T. Kawase, K. Hirose, T. Yoshida, T. Inoue, S. Obika
J. Am. Soc. Mass Spectrom. 35 2156-2164

DNAコード化ライブラリーへの応用を志向したクマリン−オリゴ核酸コンジュゲートの合成
大澤昂志
薬学雑誌 144(10) 931–936

■著書

アンチセンス核酸およびsiRNA技術
大澤昂志、小比賀聡
The Lipid, 35(1), 14–19.

アンチセンス核酸
山口卓男
核酸医薬〜モダリティ・合成・分析・DDSの最新動向〜, 17–25.

修飾核酸の合成
大澤昂志
核酸医薬〜モダリティ・合成・分析・DDSの最新動向〜, 67–74.

安全で有効なアンチセンス核酸医薬の開発に向けて
山口卓男、小比賀聡
未来社会共創を目指す 研究シーズ集2024, 54.

Chapter 9: Oligonucleotide Synthesis and State-of-the-Art Drug Discovery
T. Osawa, S. Obika
Sustainability in Tides Chemistry: Green Approaches to Oligonucleotides and Oligopeptides Synthesis 194–227