大阪大学大学院 薬学研究科
生物有機化学分野チャンネル
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2017
■論文
Hydrogen peroxide-triggered gene silencing in mammalian cells through boronated antisense oligonucleotides
S. Mori, K. Morihiro, T. Okuda, Y. Kasahara, S. Obika
Chem. Sci. 2018; Advance Article

A Novel Human Muscle Cell Model of Duchenne Muscular Dystrophy Created by CRISPR/Cas9 and Evaluation of Antisense-Mediated Exon Skipping
T. Shimo, K. Hosoki, Y. Nakatsuji, T. Yokota, S. Obika
J. Hum. Genet. ;in press

Synthesis and thermal stabilities of oligonucleotides containing 2’-O,4’-C-methylene bridged nucleic acid with a phenoxazine base
Y. Kishimoto, A. Fujii, O. Nakagawa, T. Nagata, T. Yokota, Y. Hari, S. Obika
Org. Biomol. Chem. 2017;38(15):8145-52.

Small Nucleolar Noncoding RNA SNORA23, Upregulated in Human Pancreaic Ductal Adenocarcinoma, Regulates Expression of SYNE2 to Promote Growth and Metastasis of Xenograft Tumors in Mice.
L. Cui, K. Nakano, S. Obchoei, K. Setoguchi, M. Matsumoto, T. Yamamoto, S. Obika, K. Shimada, N. Hiraoka.
Gastroenterogy 2017 July;153:292-306.

Synthesis, duplex-forming ability, enzymatic stability, and in vitro antisense potency of oligonuclreotides including 2’-C, 4’-C-ethyleneoxy-bridged thymedine derivatives.
T. Osawa, M. Sawamura, F. Wada, T. Yamamoto, S. Obika, Y.Hari.
Org. Biomol. Chem. 2017 May;15(18):3955-63.

Synthesis of the 5-Methyluridine Monomer of 3’-O,4’-C-Ethyleneoxy-bridged Nucleic Acid.
T. Osawa, M. Dohi, Y. Hitomi, Y. Ito, S. Obika, Y. Hari.
J Heterocycles. 2017;95(1):342-52.

Phospholamban Inhibition by a Single Dose of Locked Nucleic Acid Antisense Oligonucleotide Improves Cardiac Contractility in Pressure Overload-Induced Systolic Dysfunction in Mice.
H. Morihara, T, Yamamoto, H. Oiwa, K. Tonegawa, D. Tsuchiyama, I. Kawakatsu, M. Obana, M. Maeda, T. Mohri, S. Obika, Y Fujio, H. Nakayama.
J. Cardiovasc. Pharmacol. Ther. 2017 May;22(3):273-82.

Evaluation of size-exclusion chromatography for the analysis of phosphorothioate oligonucleotides.
A. Shimoyama, A. Fujisaka, S. Obika.
J. Pharm. Biomed. Anal. 2017 Mar. 20;136:55-65.

Synthesis and Properties of 7-Deazapurine- and 8-Aza-7-deazapurine-Locked Nucleic Acid Analogues: Effect of the Glycosidic Torsion Angle.
T. Hara, T. Kodama, Y. Takegaki, K. Morihiro, K.R. Ito, S. Obika.
J. Cardiovasc. Pharmacol. Ther. 2017 Jan. 6;82(1):25-36.

Triazole- and Tetrazole-Bridged Nucleic Acids: Synthesis, Duplex Stability, Nuclease Resistance, and in Vitro and in Vivo Antisense Potency.
Y. Mitsuoka, T. Yamamoto, A. Kugimiya, R. Waki, F. Wada, S. Tahara, M. Sawamura, M. Noda, Fujimura Y, Y. Kato, Y. Hari, S. Obika.
J Org. Chem. 2017 Jan. 6;82(1):12-24.

■総説
Designing Effective Antisense Oligonucleotides for Exon Skipping.
T. Shimo, R. Maruyama, T. Yokota.
Methods Mol Biol. 2017;1687:143-55.

Biological applications of xeno nucleic acids.
K. Morihiro, Y. Kasahara, S. Obika.
Mol. Biosyst. 2017 Jan. 31;13(2):235-45.

核酸医薬開発における化学
小比賀 聡、笠原 勇矢
日本発次世代創薬のための化学, 2017, 70-1, 020-2, 化学と工業

2016
■論文
Systematic Evaluation of Biophysical and Functional Characteristics of Selenomethylene-Locked Nucleic Acid-Mediated Inhibition of miR-21.
S. Nahar, A. Singh, K. Morihiro, Y. Moai, T. Kodama, S. Obika, S. Maiti.
Biochemistry. 2016 Dec. 20;55(50):7023-32.

In vitro and in vivo biophysical properties of oligonucleotides containing 5'-thio nucleosides.
M.A. Islam, R. Waki, A. Fujisaka, K.R. Ito, S. Obika.
Drug Discov. Ther. 2016;10(5):263-70.

Synthesis of scpBNA-mC, -A, and -G Monomers and Evaluation of the Binding Affinities of scpBNA-Modified Oligonucleotides toward Complementary ssRNA and ssDNA.
M. Horiba, T. Yamaguchi, S. Obika.
J Org. Chem. 2016 Nov. 18;81(22):11000-8.

Synthesis and properties of novel 2'-C,4'-C-ethyleneoxy-bridged 2'-deoxyribonucleic acids with exocyclic methylene groups.
T. Osawa, S. Obika, Y. Hari.
Org. Biomol. Chem. 2016 Oct. 12;14(40):9481-4.

Synthesis and Properties of 4-(Diarylmethylene)imidazolinone-conjugated Fluorescent Nucleic Acids
T. Okuda, S. Mori, Y. Kasahara, K. Morihiro, M. Ikejiri, K. Miyashita, S. Obika.
Tetrahedron Lett. 2016 July 20;57:3129-32.

Nuclear expression of Y-box binding protein-1 is associated with poor prognosis in patients with pancreatic cancer and its knockdown inhibits tumor growth and metastasis in mice tumor models.
K. Shinkai, K. Nakano, L. Cui, Y. Mizuuchi, H. Onishi, Y. Oda, S. Obika, M. Tanaka, M. Katano.
Int. J. Cancer. 2016 July 15;139(2):433-45.

Effect of an N-substituent in sulfonamide-bridged nucleic acid (SuNA) on hybridization ability and duplex structure.
Y. Mitsuoka, H. Aoyama, A. Kugimiya, Y. Fujimura, T. Yamamoto, R. Waki, F. Wada, S. Tahara, M. Sawamura, M. Noda, Y. Hari, S. Obika.
Org. Biomol. Chem. 2016 July 6;14(27):6531-8.

Evaluation of the effects of chemically different linkers on hepatic accumulations, cell tropism and gene silencing ability of cholesterol-conjugated antisense oligonucleotides.
S. Wada, H. Yasuhara, F. Wada, M. Sawamura, R. Waki, T. Yamamoto, M. Harada-Shiba, S. Obika.
J. Control. Release. 2016 Mar. 28;226:57-65.

Crystal structure of a 2',4'-BNANC[N-Me]-modified antisense gapmer in complex with the target RNA.
J. Kondo, Y. Nomura, Y. Kitahara, S. Obika, H. Torigoe.
Chem. Commun. 2016 Jan. 28;52(11):2354-7.

Wavelength-selective light-triggered strand exchange reaction.
K. Morihiro, T. Kodama, S. Mori, S. Tsunoda, S. Obika.
Org. Biomol. Chem. 2016 Jan. 27;14(5):1555-8.

Consecutive incorporation of functionalized nucleotides with amphiphilic side chains by novel KOD polymerase mutant.
H. Hoshino, Y. Kasahara, H. Fujita, M. Kuwahara, K. Morihiro, S. Tsunoda, S. Obika.
Bioorg. Med. Chem. Lett. 2016 Jan. 15;26(2):530-3.

Serial incorporation of a monovalent GalNAc phosphoramidite unit into hepatocyte-targeting antisense oligonucleotides.
T. Yamamoto, M. Sawamura, F. Wada, M. Harada-Shiba, S. Obika.
Bioorg. Med. Chem. 2016 Jan. 1;24(1):26-32.

■総説
核酸医薬品開発における修飾核酸
(The modified oligonucleotides for nucleic acid drug discovery)
藤坂 朱紀、小比賀 聡
Medical Science Digest 2016 Sep.;42(10):22-5.

Design of antisense oligonucleotides.
S. Obika, Y. Kasahara.
Nihon Yakurigaku Zasshi. 2016 Aug.;148(2):100-4.

化学的アプローチを駆使した核酸医薬の最前線
小比賀 聡、中川 治
今、着実に実り始めた遺伝子治療(遺伝子医学MOOK30), メディカルドゥ, 2016 Jun. 20, 125-31

Synthesis and Properties of 2',4'-Bridged Nucleic Acids Containing Multiple Heteroatoms in the Bridges
Y. Hari, S. Obika.
J. Syn. Org. Chem., Jpn., 2016 Mar. 22, 74, 141-53.

■著書
ヌクレオシドおよび核酸塩基アナログを有する代表的医薬品を列挙し、化学構造に基づく性質について説明できる(第11章 SBO27)
藤坂 朱紀、小比賀 聡
スタンダード薬学シリーズⅡ3, 化学系薬学Ⅱ. 生体分子・医薬品の化学による理解, 日本薬学会(編), 2016, 225-31, 東京化学同人

糖部架橋型核酸の新たな展開(第4章)
小比賀 聡
核酸医薬の創製と応用展開, 和田 猛(監), 2016, 29-39, シーエムシー出版

大阪大学大学院 薬学研究科 生物有機化学分野
〒565‐0871 大阪府吹田市山田丘1-6
TEL: 06-6879-8200    FAX: 06-6879-8204
obika@phs.osaka-u.ac.jp