Discovery of the function of lipophilic ligand on metabolic disease

亲脂性配体在代谢疾病中的作用的发现

• 批准号: 21700692
• 负责人: ADACHI Tetsuya
• 金额: $ 2.75万
• 依托单位: Kyoto Prefectural University of Medicine
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (B)
• 财政年份: 2009
• 资助国家: 日本
• 起止时间: 2009 至 2010
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-21700692/
• 关键词: 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

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.

本研究的目的是发现亲脂配体受体在脂肪组织、骨骼肌、肝脏和心脏等代谢紊乱相关器官中的功能。雌激素的膜受体GPR30在心肌梗死后的脂肪组织、骨骼肌、肝脏、原代心肌细胞和心肌成纤维细胞中均有表达。17β-雌二醇可诱导心肌细胞和肌成纤维细胞上ERK的磷酸化。这些结果表明，雌激素通过GPR30在心脏具有非基因组效应。

项目成果

Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation

• DOI: 10.1124/mol.110.066324
• 发表时间: 2010-11-01
• 期刊: MOLECULAR PHARMACOLOGY
• 影响因子: 3.6
• 作者: Sun, Qi;Hirasawa, Akira;Tsujimoto, Gozoh
• 通讯作者: Tsujimoto, Gozoh

Association of Estrogen receptor-a gene polymorphisms with cardiac autonomic nervous activity in healthy young Japanese males.

雌激素受体基因多态性与健康年轻日本男性心脏自主神经活动的关联。

• 发表时间: 2010
• 期刊: Clinica Chimica Acta. 411
• 作者: Matsunaga T;Gu N;Yamazaki H;Adachi T;Yasuda K;Moritani T;Tsuda K;Nishiyama T;Nonaka M.
• 通讯作者: Nonaka M.

Novel selective ligands for free fatty acid receptors GPR120 and GPR40

• DOI: 10.1007/s00210-009-0425-9
• 发表时间: 2009-09-01
• 期刊: NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
• 影响因子: 3.6
• 作者: Hara, Takafumi;Hirasawa, Akira;Tsujimoto, Gozoh
• 通讯作者: Tsujimoto, Gozoh