Structure-Activity Relationship and Mechanistic Studies on Sodium 4-phenylbutyrate and its derivatives

• Project/Area Number: 15K08014
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Asahikawa Medical College
• Principal Investigator: OKUDA Katsuhiro 旭川医科大学, 医学部, 助教 (00389115)
• Co-Investigator(Kenkyū-buntansha): 佐能 正剛 広島大学, 医歯薬保健学研究科(薬), 助教 (00552267) ; 太田 茂 広島大学, 医歯薬保健学研究科(薬), 教授 (60160503) ; 酒井 規雄 広島大学, 医歯薬保健学研究科(医), 教授 (70263407)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Project Status: Completed (Fiscal Year 2017)
• Budget Amount: ¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000); Fiscal Year 2017: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000); Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000); Fiscal Year 2015: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
• Keywords: 化学シャペロン / 構造活性相関

Outline of Final Research Achievements

4PBA was valued its properties by 5 kind of assays. We have determined each criteria to compare the properties with those of other derivatives. Forty 4PBA derivatives were designed then purchased or synthesized as its sodium salt. The derivatives were applied for the assays. Coefficient of correlation values were calculated between some parameters and mRNA expression amount. Four and three genes correlated highly with chaperonic activity or HDAC inhibitory activity, respectively.

Research Products

• [Presentation] 化学シャペロンSodium 4-phenylbutyrate の構造活性相関研究（2） (2016)
  • Author(s): 奥田 勝博, 佐々木 律枝, 保科 千里, 酒井 規雄, 太田 茂, 清水 惠子
  • Organizer: 日本薬学会 第136年会
  • Place of Presentation: 横浜
  • Year and Date: 2016-03-29
• [Presentation] Structure-Activity Relationship and Mechanistic Studies on Sodium 4-phenylbutyrate and its derivatives (2015)
  • Author(s): Katsuhiro Okuda, Ritsue Sasaki, Chisato Hoshina, Norio Sakai, Shigeru Ohta, Keiko Shimizu
  • Organizer: 10th AFMC International Medicinal Chemistry Symposium
  • Place of Presentation: チェジュ、韓国
  • Year and Date: 2015-10-20
  • Int'l Joint Research