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研究業績Research Achevements

2018年以降の業績

  • Koizumi, K., Maeda, Y., Kano, T., Yoshida, H., Sakamoto, T., Yamagishi, K. and Ueno, Y.*: Synthesis of 4'-C-aminoalkyl-2'-O-methyl modified RNA and their biological properties. Bioorg. Med. Chem. 26: 521-3534, 2018.

  • Nakamoto, K., Akao, Y. and Ueno, Y.*: Diazirine-containing tag-free RNA probes for efficient RISC-loading and photoaffinity labeling of microRNA targets. Bioorg. Med. Chem. Lett. 28: 2906-2909, 2018.

  • Nakamoto, K., Akao, Y., Furuichi, Y. and Ueno, Y.*: Enhanced intercellular delivery of cRGD-siRNA conjugates by an additional oligospermine modification. ACS Omega. 3: 8226-8232, 2018.

  • Kano, T., Katsuragi, Y., Maeda, Y. and Ueno, Y.*: Synthesis and properties of 4'-C-aminoalkyl-2'-fluoro-modified RNA oligomers. Bioorg. Med. Chem. 26: 4574-4582, 2018.

  • Chandela, A. and Ueno, Y.*: Systemic delivery of small interfering RNA therapeutics; obstacles and advances. Reviews in Agricultural Science 7: 10-28, 2019.

  • Chandela, A., Watanabe, T., Yamagishi, K. and Ueno Y.*: Synthesis and characterization of small interfering RNAs with haloalkyl groups at their 3'-dangling ends. Bioorg. Med. Chem. 27:1341-1349, 2019.

  • Kajino, R., Maeda, Y., Yoshida, H., Yamagishi, K. and Ueno, Y.*: Synthesis and biophysical characterization of RNAs containing (R)- and (S)-5'-C-aminopropyl-2'-O-methyluridines. J. Org. Chem. 84: 3388-3404, 2019.

  • Chandela, A. and Ueno, Y.*: Design, synthesis and evaluation of novel, branched trident small interfering RNA nanostructures for sequence-​specific RNAi activity. RSC Advances 9: 34166-34171, 2019.

  • Uematsu, A., Kajino, R., Maeda, Y. and Ueno, Y.*: Synthesis and characterization of 4'-C-guanidinomethyl-2'-O-methyl-modified RNA oligomers. Nucleotides & Nucleic Acids 39: 280-291, 2020.

  • Yoshikawa, R., Heishima, K., Ueno, Y., Kawade, M., Maeda, Y., Yoshida, K., Murakami, M., Sakai, H., Akao, Y. and Mori, T.: Development of synthetic microRNA-​214 showing enhanced cytotoxicity and RNase resistance for treatment of canine hemangiosarcoma. Veterinary and Comparative Oncology 18: 570-579, 2020.

  • Tsuchihira, T., Kajino, R., Maeda, Y. and Ueno, Y.*: 4'-​C-​Aminomethyl-​2'-​deoxy-​2'-​fluoroarabinonucleoside increases the nuclease resistance of DNA without inhibiting the ability of a DNA​/RNA duplex to activate RNase H. Bioorg. Med. Chem. 28: 115611, 2020.

  • 梶野瞭平,上野義仁*: アンチセンス核酸の毒性発現メカニズムと毒性発現低減に向けた科学的アプローチ. 日本核酸医薬学会誌, 35-43, 2020.

  • Matsubara, M., Honda, K., Ozaki, K., Kajino, R., Kakisawa, Y., Maeda, Y. and Ueno, Y.*: Synthesis of siRNAs incorporated with cationic peptides R8G7 and R8A7 and the effect of the modifications on siRNA properties. RSC Advances 10: 34815-34824, 2020.

  • Takeuchi, A., Hisamatsu, K., Okumura, N., Sugimitsu, Y., Yanase, E., Ueno, Y. and Nagaoka, S.: IIAEK targets intestinal alkaline phosphatase (IAP) to improve cholesterol metabolism with a specific activation of iap and downregulation of ABCA1. Nutrients 12: 2859, 2020.

  • Zhou, Y., Kajino, R., Ishii, S., Yamagishi, K. and Ueno, Y.*: Synthesis and evaluation of (S)​-​5'-​C-​aminopropyl and (S)​-​5'-​C-​aminopropyl-​2'-​arabinofluoro modified DNA oligomers for novel RNase H-​dependent antisense oligonucleotides. RSC Advances 10: 41901-41914, 2020.

  • 上野義仁*,梶野瞭平: アンチセンス核酸の合成. In: 核酸科学ハンドブック.杉本直己 編.講談社,pp. 513-515, 2020.

  • Kajino, R. and Ueno, Y.*: (S)​-​5'-​C-​Aminopropyl-​2'-​O-​methyl nucleosides enhance antisense activity in cultured cells and binding affinity to complementary single-​stranded RNA. Bioorg. Med. Chem. 30: 115925, 2021.

  • Tsukimura, R., Kajino, R., Zhou, Y., Chandela, A. and Ueno, Y.*: 4'-C-Aminoethoxy modification enhanced nuclease resistance of RNAs and improved thermal stability of RNA duplexes. Results in Chemistry 3: 100231, 2021.

  • 梶野 瞭平,上野義仁*: 核酸医薬を指向したカチオン性側鎖を有する新規人工核酸の合成, 有機合成化学協会誌, 79: 1102-1112, 2021.

  • Yoshikawa, R., Maeda, A., Ueno, Y., Sakai, H., Kimura, S., Sawadaishi, T., Kohgo, S., Yamada, K. and Mori, T.: Intraperitoneal administration of synthetic microRNA-214 elicits tumor suppression in an intraperitoneal dissemination mouse model of canine hemangiosarcoma. Veterinary Research Communications, 2022. doi.org/10.1007/s11259-021-09869-1

  • Ueda, H. and Ueno, Y.*: Synthesis of 4'-C-(aminoethyl)thymidine and 4'-C-[(N-methyl)aminoethyl]thymidine by a new synthetic route and evaluation of the properties of the DNAs containing the nucleoside analogs. Bioorg. Med. Chem. 60: 116690, 2022.

  • Kajino, R., Sakamoto, S. and Ueno, Y.*: Synthesis, gene silencing activity, thermal stability, and serum stability of siRNA containing four (S)-5'-C-aminopropyl-2'-O-methylnucleosides (A, adenosine; U, uridine; G, guanosine; and C, cytidine). ASC Advances 12: 11454–11476, 2022.

  • Katsuzaki, Y., Tsukimura, R., Chandela, A., Chano, T. and Ueno, Y.*: 4'-C-Aminoethoxy-modified DNAs exhibit increased nuclease resistance, sustained RNase H activity, and inhibition of KRAS gene expression. Chem. Biodiversity 19: e202200125, 2022.

  • Chandela, A., Ueda, H. and Ueno, Y.*: Synthesis of 4'-C-(Aminoethyl)thymidine and 4'-C-[(N-methyl)aminoethyl]thymidine nucleosides to enhance DNA stability. Current Protocols 2(9): e501, 2022.

  • Zhou, Y., Sakamoto, S. and Ueno, Y.*: Antisense gapmers with LNA-Wings and (S)-5'-C-Aminopropyl-2'-arabinofluoro-nucleosides could efficiently suppress the expression of KNTC2. Molecules 27(21): 7384, 2022.

  • Sato, H.,Chandela,A., Ueno, Y.*: Synthesis and characterization of novel (S)-5'-C-aminopropyl-2'-fluorouridine modified oligonucleotides as therapeutic siRNAs,Bioorg. Med. Chem. 87 (2023) 117317,https://doi.org/10.1016/j.bmc.2023.117317

  • Koyasu, K., Chandela,A., Ueno, Y.*: Non-terminal conjugation of small interfering RNAs with spermine improves duplex binding and serum stability with position-specific incorporation, RSC Advances, 13, 25169–25181, 2023. https://doi.org/10.1039/D3RA04918C

  • Sawada, H., Kakisawa, Y. Ueno, Y.*: Properties and synergistic effects of a nonionic backbone and aminoalkyl modified nucleosides in RNAs, Bioorganic Chemistry, 144:107143, 2024. DOI:10.1016/j.bioorg.2024.107143

  • 梶野瞭平, 佐藤仁昴, 上野義仁*: 糖部5′-位アミノアルキル修飾ヌクレオシドの合成とsiRNA医薬への応用. 核酸医薬, 第2章 第2節, 75-82, 2024.

  • Onishi, S., Chandela, A. Ueno, Y.*: Synthesis and Evaluation of 4′-C-(S) and 4′-C-(R)-2-aminopropoxy-thymidine-modified DNAs for Thermal Stability, RNase H Digestion, and Nuclease Resistance, ChemistrySelect 2024, 9, e2023050. https://doi.org/10.1002/slct.202305090

  • Hibino, H., Zhou, Y., Saito, Y., Ueno, Y.*: Novel synthesis and evaluation of oligonucleotides containing (S)-5′-C-aminopropyl-modified thymidine analogs for RNase H-dependent antisense therapy, Results in Chemistry, 9 (2024) 101648.

  • Zhou, Y., Sato, H., Kawade, M., Yamagishi, K., Ueno, Y.*: Application of 4′-C-α-aminoethoxy-2′-O-methyl-5-propynyl-uridine for antisense therapeutics, RSC Advances, in press.