Novel inhibitor of serine threonine kinase for the treatment of cholangiocarcinoma and pancreas cancer

• Project/Area Number: 24390313
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Partial Multi-year Fund
• Section: 一般
• Research Field: Digestive surgery
• Research Institution: Nagoya University
• Principal Investigator: Nagino Masato 名古屋大学, 医学(系)研究科(研究院), 教授 (20237564)
• Co-Investigator(Kenkyū-buntansha): 江畑 智希 名古屋大学, 医学(系)研究科(研究院), 准教授 (60362258) ; 國料 俊男 名古屋大学, 医学(系)研究科(研究院), 特任講師 (60378023) ; 横山 幸浩 名古屋大学, 医学部附属病院, 講師 (80378091) ; 千賀 威 名古屋大学, 医学(系)研究科(研究院), 准教授 (80419431)
• Project Period (FY): 2012-04-01 – 2017-03-31
• Project Status: Completed (Fiscal Year 2016)
• Budget Amount: ¥18,200,000 (Direct Cost: ¥14,000,000、Indirect Cost: ¥4,200,000); Fiscal Year 2016: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000); Fiscal Year 2015: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000); Fiscal Year 2014: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000); Fiscal Year 2013: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000); Fiscal Year 2012: ¥8,190,000 (Direct Cost: ¥6,300,000、Indirect Cost: ¥1,890,000)
• Keywords: 胆管癌 / 膵癌 / セリンスレオニンキナーゼ

Outline of Final Research Achievements

Novel inhibitor of serine threonine kinase, T5467374 was identified using interactive machine learning method and Z'-LYTE Kinase Assay. T5467374 suppressed the proliferation and induced the cell death in pancreas cancer cell lines. This inhibitor suppressed the tumor growth in subcutaneous xenograft model of pancreas cancer. Bisabolol derivative were developed as the inhibitor of AKT serine threonine kinase. Bisabolol derivative showed the antitumor effect in subcutaneous xenograft model of pancreas cancer. This reagent suppressed the AKT expression in the tumor.