Discovery of the function of lipophilic ligand on metabolic disease

2010 Fiscal Year Final Research Report

• 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
• Keywords: GPCR / GPR30 / ERK / 心臓

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