Discovery of the function of lipophilic ligand on metabolic disease

• Project/Area Number: 21700692
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Applied health science
• Research Institution: Kyoto Prefectural University of Medicine
• Principal Investigator: ADACHI Tetsuya Kyoto Prefectural University of Medicine, 医学研究科, 助教 (60345014)
• Project Period (FY): 2009 – 2010
• Project Status: Completed (Fiscal Year 2010)
• Budget Amount: ¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000); Fiscal Year 2010: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000); Fiscal Year 2009: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
• Keywords: GPCR / GPR30 / ERK / 心臓 / G-タンパク共役型受容体 / 線維芽細胞 / シグナル伝達 / 脂溶性リガンド / 心筋細胞

Research Abstract

The aim of this study is the discovery of the function of lipophilic ligand receptors in metabolic disorder-related organ, such as adipose tissue, skeletal muscle, liver and heart. GPR30, membrane receptor of estrogen, was expressed in adipose tissue, skeletal muscle, liver, primary cardiac myocytes and cardiac myofibroblasts, which are detected in myocardial infarction. Administration of 17β-estradiol induced the phosphorylation of ERK on myocytes and myofibroblasts. These results suggest that estrogen possesses the non-genomic effect via GPR30 in heart.

Research Products

• [Journal Article] Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation. (2010)
  • Author(s): Sun Q, Hirasawa A, Hara T, Kimura I, Adachi T, Awaji T, Ishiguro M, Suzuki T, Miyata N, Tsujimoto G.
  • Journal Title: Mol Pharmacol. 78 Pages: 804-810
• [Journal Article] Association of Estrogen receptor-a gene polymorphisms with cardiac autonomic nervous activity in healthy young Japanese males. (2010)
  • Author(s): Matsunaga T, Gu N, Yamazaki H, Adachi T, Yasuda K, Moritani T, Tsuda K, Nishiyama T, Nonaka M.
  • Journal Title: Clinica Chimica Acta. 411 Pages: 505-509
• [Journal Article] Novel selective ligands for free fatty acid receptors GPR120 and GPR40. (2009)
  • Author(s): Hara T, Hirasawa A, Sun Q, Sadakane K, Itsubo C, Iga T, Adachi T, Koshimizu TA, Hashimoto T, Asakawa Y, Tsujimoto G.
  • Journal Title: Naunyn Schmiedebergs Arch Pharmacol. 380 Pages: 247-255