Novel modification method of oligonucleotides for siRNA medicine

• Project/Area Number: 22790107
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Drug development chemistry
• Research Institution: Gifu University
• Principal Investigator: KITAMURA Yoshiaki 岐阜大学, 工学部, 助教 (10503659)
• Research Collaborator: KITADE Yukio 岐阜大学, 工学部, 教授 (20137061) ; UENO Yoshihito 岐阜大学, 応用生物科学部, 教授 (20250467) ; IKEDA Masato 岐阜大学, 工学部, 准教授 (20432867)
• Project Period (FY): 2010 – 2012
• Project Status: Completed (Fiscal Year 2012)
• Budget Amount: ¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000); Fiscal Year 2012: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000); Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000); Fiscal Year 2010: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
• Keywords: 核酸医薬 / siRNA / オリゴ核酸修飾

Research Abstract

Small interfering RNAs (siRNAs) are considered to be attractive candidates as nucleic acid drugs, owing to their powerful regulation of gene expression in a sequence-specific manner. In this study, novel some solid supports and synthetic method of artificial nucleic acids for chemically modified siRNA were developed.

Research Products

• [Journal Article] Stereoselective synthesis of 1-deoxy-1-ethynyl-β-D-ribofura- nose as a versatile scaffold (2012)
  • Author(s): Yoshiaki Kitamura、 Kana Edayoshi 、 Yukio Kitad
  • Journal Title: Tetrahedron Lett Volume: 53 Pages: 6987-6989
  • Peer Reviewed
• [Journal Article] Synthesis and biological properties of chemically modified siRNAs bearing 1-deoxy-D-ribofuranose in their 3′-overhang region (2012)
  • Author(s): Kazumi Taniho、Remi Nakashima、Mahmoud Kandeel、 Yoshiaki Kitamura、 Yukio Kitade
  • Journal Title: Bioorg. Med. Chem. Lett Volume: 22 Pages: 2518-2521
  • Peer Reviewed
• [Journal Article] Stereoselective synthesis of 1-deoxy-1-ethynyl-β-D-ribofuranose as a versatile scaffold (2012)
  • Author(s): Yoshiaki Kitamura, Kana Edayoshi, Yukio Kitade
  • Journal Title: Tetrahedron Letters Volume: 53 Issue: 51 Pages: 6987-6989
  • DOI: 10.1016/j.tetlet.2012.10.053
  • Peer Reviewed
• [Journal Article] Synthesis and biological properties of chemically modified siRNAs bearing 1-deoxy-D-ribofuranose in their 3'-overhang region (2012)
  • Author(s): Kazumi Taniho, Remi Nakashima, Mahmoud Kandeel, Yoshiaki Kitamura, Yukio Kitade
  • Journal Title: Bioorganic & Medicinal Chemistry Letters Volume: 22 Issue: 7 Pages: 2518-2521
  • DOI: 10.1016/j.bmcl.2012.01.132
  • Peer Reviewed
• [Presentation] Stereoselective synthesis of 1-deoxy-1-ethynyl-β-D-ribofuranose and its applications (2012)
  • Author(s): Kana Edayoshi 、 Yoshiaki Kitamura、Masato Ikeda 、 Yukio Kitade
  • Organizer: 第39回国際核酸化学シンポジウム
  • Place of Presentation: 名古屋
• [Presentation] 1-Deoxy-1-ethynyl-β-D-ribofuranoseの立体選択的合成 (2012)
  • Author(s): 枝吉佳奈、喜多村徳昭、北出幸夫
  • Organizer: 平成 24 年度日本薬学会東海支部例会
  • Place of Presentation: 静岡
• [Presentation] Synthesis of 1-deoxy-D-ribofuranose and its application for RNAi studies (2011)
  • Author(s): Kazumi Taniho, Yoshiaki Kitamura, Yukio Kitade
  • Organizer: 第38回国際核酸化学シンポジウム(ISNAC2011)
  • Place of Presentation: 北海道大学(札幌)
  • Year and Date: 2011-11-09
• [Presentation] 塩基部欠損型ヌクレオシドを導入した2-5Aアナログの合成とその生物活性 (2011)
  • Author(s): 谷保和美、喜多村徳昭、北出幸夫
  • Organizer: 平成23年度日本薬学会東海支部例会
  • Place of Presentation: 金城学院大学(名古屋)
  • Year and Date: 2011-07-09
• [Presentation] Synthesis of 1-deoxy-D-ribo- furanose and its application for RNAi studies (2011)
  • Author(s): Kazumi Taniho、Yoshiaki Kitamura、Yukio Kitade
  • Organizer: 第38回国際核酸化学シンポジウム
  • Place of Presentation: 札幌
• [Presentation] 1-Deoxy-1-ethynyl-β-D-ribofuranoseの立体選択的合成
  • Author(s): 枝吉佳奈, 喜多村徳昭, 北出幸夫
  • Organizer: 平成24年度日本薬学会東海支部例会
  • Place of Presentation: 静岡県立大学（静岡）
• [Presentation] Stereoselective synthesis of 1-deoxy-1-ethynyl-β-D-ribofuranose and its applications
  • Author(s): Kana Edayoshi, Yoshiaki Kitamura, Masato Ikeda, Yukio Kitade
  • Organizer: 第39回国際核酸化学シンポジウム（ISNAC2012）
  • Place of Presentation: 名古屋大学（名古屋）