Design, Synthesis and Functional Analysis of Ion-Channel-Forming Molecules Based on Polytheonamide Structure

2016 Fiscal Year Final Research Report

• Project/Area Number: 15H06156
• Research Category: Grant-in-Aid for Research Activity Start-up
• Allocation Type: Single-year Grants
• Research Field: Chemical pharmacy
• Research Institution: The University of Tokyo
• Principal Investigator: Itoh Hiroaki 東京大学, 大学院薬学系研究科(薬学部), 助教 (20758205)
• Project Period (FY): 2015-08-28 – 2017-03-31
• Keywords: 固相合成 / 有機化学 / 合成化学 / ペプチド / イオンチャネル

Outline of Final Research Achievements

Polytheonamide B is an ion-channel-forming 48-mer natural peptide that displays extraordinarily potent cytotoxicity. This study focuses on establishment of highly efficient solid-phase synthetic strategy for detailed functional and biological investigations of polytheonamide B and its analogues. Novel strategy of protective groups for component amino acids enabled full solid-phase total synthesis of polytheonamide B and its analogues. The newly established synthetic strategy significantly reduced the number of solution-phase synthetic steps and HPLC purification steps, leading to the efficient and facile synthesis of the total structure of polytheonamide B.

Free Research Field

有機化学、ケミカルバイオロジー