Development of membrane-permeable Aib-containing peptide for delivery of oligonucleotide drugs

2012 Fiscal Year Final Research Report

• Project/Area Number: 22590109
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Osaka University of Pharmaceutical Sciences
• Principal Investigator: WADA Shun-ichi 大阪薬科大学, 薬学部, 准教授 (30278593)
• Co-Investigator(Kenkyū-buntansha): URATA Hidehito 大阪薬科大学, 薬学部, 教授 (80211085)
• Project Period (FY): 2010 – 2012
• Keywords: Aib / 膜透過性ペプチド / ヘリックス / 核酸医薬 / アンチセンス

Research Abstract

Oligonucleotide (ODN) drugs have interesting therapeuticpotentials in various biological applications. However, charged polar ODNs typicallyexhibit poor membrane permeabilization. My designed Aib-containing peptides showmembrane permeable properties, and have the potential for delivery of ODNs into cells.

Research Products

• [Journal Article] Cellular Uptake of Covalent Conjugates of Oligonucleotide with Membrane-modifying Peptide, Peptaibol (2012)
  • Author(s): Shun-ichi Wada, Yasunari Hitora, Saori Yokoe, Osamu Nakagawa, and Hidehito Urata
  • Journal Title: Bioorg. & Med. Chem Volume: 20 Pages: 3219-3222
  • Peer Reviewed
• [Journal Article] Cellular Uptake of Aib-containing Amphi- pathic Helix Peptide (2011)
  • Author(s): Shun-ichi Wada, Hirokazu Tsuda, Terumi Okada, and Hidehito Urata
  • Journal Title: Bioorg. & Med. Chem. Lett Volume: 21 Pages: 5688-5691
  • URL: http://dx.doi.org/10.1016/j.bmcl.2011.08.030
  • Peer Reviewed
• [Presentation] Aib 含有両親媒性へリックスペプチドを用いたオリゴヌクレオチドの細胞内移送 (2013)
  • Author(s): 橋本佑樹,津田浩和,中川治,和田俊一,浦田秀仁
  • Organizer: 日本薬学会第133年会
  • Place of Presentation: 横浜
  • Year and Date: 2013-03-27
• [Presentation] Designed Aib-containing amphipathic helix peptide for oligonucleotide delivery into cells (2012)
  • Author(s): 和田俊一,橋本侑樹,津田浩和,中川治, 浦田 秀仁
  • Organizer: 第49回ペプチド討論会
  • Place of Presentation: 鹿児島
  • Year and Date: 2012-11-08
• [Presentation] TV-XIIa-オリゴヌクレオチド複合体のアンチセンス効果の検討 (2012)
  • Author(s): 和田俊一,横江沙緒里,人羅康匠,中川 治,浦田秀仁
  • Organizer: 日本薬学会第132 年会
  • Place of Presentation: 札幌
  • Year and Date: 2012-03-30
• [Presentation] Aib 含有両親媒性ヘリックスペプチ ドを用いたオリゴヌクレオチドの細胞膜透過性検討 (2011)
  • Author(s): 津田浩和,岡田てる美,和田俊一,浦田 秀仁
  • Organizer: 第61回日本薬学会近畿支部総会・大会
  • Place of Presentation: 神戸
  • Year and Date: 2011-11-22
• [Presentation] Conjugates of antisense oligonucleotides with (2011)
  • Author(s): 和田俊一,人羅康匠,横江沙緒里,浦田 秀仁
  • Organizer: Aib-containing peptide: effects on cellular uptake and antisense effect
  • Place of Presentation: 札幌
  • Year and Date: 2011-09-28
• [Presentation] Aib 含有両親媒性ヘリックスペプチ ドの細胞膜透過性 (2011)
  • Author(s): 津田浩和,岡田てる美,和田俊一,浦田 秀仁
  • Organizer: 日本薬学会第131年会
  • Place of Presentation: 静岡
  • Year and Date: 2011-03-31