Unified total synthesis and biological evaluation of natural and artificial ryanoids

2016 Fiscal Year Final Research Report

• Project/Area Number: 15K14928
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Chemical pharmacy
• Research Institution: The University of Tokyo
• Principal Investigator: Inoue Masayuki 東京大学, 大学院薬学系研究科(薬学部), 教授 (70322998)
• Research Collaborator: NAGATOMO Masanori 東京大学, 大学院薬学系研究科, 助教 (70634161)
• Project Period (FY): 2015-04-01 – 2017-03-31
• Keywords: 合成化学 / 全合成 / 生物活性分子の設計 / 生理活性 / イオンチャネル / リアノジン / リアノジンレセプター

Outline of Final Research Achievements

Dysfunction of ion channels leads to various diseases. Rational development of pharmaceuticals that modulate functions of ion channels is an urgent task in modern science. Ryanodine receptors are calcium ion release channels, and are selectively activated by ryanodine. Our study aimed at unified total synthesis and biological evaluation of ryanodine, natural and artificial ryanoids.
In this study, we developed a new strategy for assembly of the architecturally complex structure of ryanodine, and achieved unified total synthesis of ryanodine and five other natural ryanoids. Our practical syntheses enabled us to prepare the ryanoids for detailed investigation of their various biological functions. Moreover, the fluorescent labeled ryanodine was prepared for investigation of the molecular interaction between the synthetic molecules and ryanodine receptors.

Free Research Field

天然物合成化学・生物有機化学