Regulatory mechanisms of intracellular trafficking of Gq protein-coupled receptors

2014 Fiscal Year Final Research Report

• Project/Area Number: 23590119
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Biological pharmacy
• Research Institution: Meiji Pharmaceutical University
• Principal Investigator: HISHINUMA Shigeru 明治薬科大学, 薬学部, 准教授 (70211505)
• Co-Investigator(Renkei-kenkyūsha): FUKUI Hiroyuki 徳島大学大学院, HBS研究部, 教授 (90112052)
• Project Period (FY): 2011-04-28 – 2015-03-31
• Keywords: ヒスタミンH1受容体 / Gq蛋白質共役型受容体 / C末端 / 細胞内輸送 / クラスリン

Outline of Final Research Achievements

We evaluated regulatory mechanisms of agonist-induced internalization of Gq protein-coupled human histamine H1 receptors by mutation analyses of the N- and C-terminals of receptors expressed in Chinese hamster ovary cells. H1 receptors tagged with hemagglutinin at the N-terminal internalized via clathrin-dependent mechanisms upon stimulation with histamine. In contrast, H1 receptors failed to internalize by truncation of the serine 487 residue of the C-terminal. These results suggest that the C-terminal of H1 receptors plays a crucial role in agonist-induced and clathrin-dependent internalization.

Free Research Field

受容体薬理学