Study toward Development Ionotropic Glutamate Receptore Subytpe Selective Ligand

2015 Fiscal Year Final Research Report

• Project Area: Chemical Biology using bioactive natural products as specific ligands: identification of molecular targets and regulation of bioactivity
• Project/Area Number: 23102009
• Research Category: Grant-in-Aid for Scientific Research on Innovative Areas (Research in a proposed research area)
• Allocation Type: Single-year Grants
• Review Section: Science and Engineering
• Research Institution: Osaka City University
• Principal Investigator: Shianda Tetsuro 大阪市立大学, 大学院理学研究科, 教授 (30271513)
• Co-Investigator(Kenkyū-buntansha): Ohfune Yasufumi 大阪市立大学, 大学院理学研究科, 名誉教授 (20142078)
• Co-Investigator(Renkei-kenkyūsha): Shimamoto Keiko (公益財団法人)サントリー生命科学財団, 主幹研究員 (70235638) ; Sakaguchi Kazuhiko 大阪市立大学, 大学院理学研究科, 准教授 (80264795)
• Project Period (FY): 2011-04-01 – 2016-03-31
• Keywords: グルタミン酸受容体 / 天然物 / カイトセファリン / アクロメリン酸 / リガンド / 超活性

Outline of Final Research Achievements

Chemical biology of natural products focusing on naturally occurring ionotropic glutamte receptor ligands, acromelic acid A and kaitocephalin was studied. Studies involving total synthesis of these natural products, their analog synthesis, ionotropic glutamate receptor binding assay, and structure analysis of ligand-protein complexes of these natural products bound to ionotropic glutamate receptors were conducted. As a result, the target receptor subtype of kaitocephalin was identified. Moreover, (7S)-kaitocephalin was discovered as a more potent NMDA receptor selective ligand than kaitocephalin.

Free Research Field

ケミカルバイオロジー