A method for generating molecular-targeting tools: Protein kinase-oriented library based on conformationally constrained peptide

• Project/Area Number: 26870503
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Biomolecular chemistry; Chemical biology
• Research Institution: Osaka Prefecture University
• Principal Investigator: Fujiwara Daisuke 大阪府立大学, 理学(系)研究科(研究院), 助教 (30611420)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Project Status: Completed (Fiscal Year 2016)
• Budget Amount: ¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000); Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000); Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000); Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
• Keywords: プロテインキナーゼ / 阻害剤 / ペプチド / ライブラリー / ファージディスプレイ / オーロラキナーゼ / 細胞膜透過性 / オーロラキナーぜ

Outline of Final Research Achievements

Protein kinase takes roles of signal transduction or cell division of living cells. The biological functions of over 500 members of protein kinases are still not fully understood because of the lack of specific molecular tools to examine each protein kinase. Aberrant protein kinases cause diseases, and their specific inhibitors based on such molecular tools are expected to be therapeutics. Here we developed a new method to design and generate specific protein kinase inhibitors. This method would contribute to generate novel molecular tools in biology and also give therapeutic leads.

Research Products

• [Journal Article] Generation of Molecular-Targeting Peptides for Protein Kinases: A Phage-Displayed Library of Helix-Loop-Helix Peptides conjugated with Adenosine (2017)
  • Author(s): Daisuke Fujiwara, Kousuke Mihara, Yusuke Nakamura, Takeshi Tsumuraya, and Ikuo Fujii
  • Journal Title: Peptide Science Volume: 2016
  • Peer Reviewed
• [Presentation] Generation of Molecular-Targeting Peptides for Protein Kinases: A Phage-Displayed Library of Helix-Loop-Helix Peptides conjugated with Adenosine (2016)
  • Author(s): Daisuke Fujiwara, Kousuke Mihara, Yusuke Nakamura, Takeshi Tsumuraya, and Ikuo Fujii
  • Organizer: 第53回ペプチド討論会（日本ペプチド学会主催）
  • Place of Presentation: 京都テルサ（京都府）
  • Year and Date: 2016-10-26
• [Presentation] Molecular Design of Protien Kinase Inhibitors: Conjugation of ATP-Competitive Molecules with Kinase Surface-Targeted Peptides. (2014)
  • Author(s): Ryo Takayama, Daisuke Fujiwara, Ikuo Fujii
  • Organizer: 第51回ペプチド討論会（日本ペプチド学会）
  • Place of Presentation: 徳島大学（徳島県徳島市）
  • Year and Date: 2014-10-23
• [Patent(Industrial Property Rights)] プロテインキナーゼ阻害剤 (2016)
  • Inventor(s): 藤原大佑、藤井郁雄
  • Industrial Property Rights Holder: 公立大学法人大阪府立大学
  • Industrial Property Rights Type: 特許
  • Filing Date: 2016-01-19