Action mechanism study of PF1171 hexapeptides focused on their 3D structures

2016 Fiscal Year Final Research Report

• Project/Area Number: 26850068
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Bioorganic chemistry
• Research Institution: Mie University (2015-2016); Tohoku University (2014)
• Principal Investigator: MASUDA Yuichi 三重大学, 生物資源学研究科, 准教授 (90617755)
• Co-Investigator(Renkei-kenkyūsha): KAI Kenji 大阪府立大学, 大学院生命環境科学研究科, 講師 (40508404)
• Research Collaborator: TANAKA Ren 東北大学, 大学院薬学研究科, 大学院生
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: 環状ペプチド / カイコ / アポリポタンパク質B / X線結晶構造解析 / 核磁気共鳴 / 三次元構造 / 構造活性相関 / 分子プローブ

Outline of Final Research Achievements

We achieved organic synthesis of PF1171 hexapeptides, cyclic peptides with paralytic activity against silkworms and inhibitory activity against production of apolipoprotein B. X-ray crystallography and nuclear magnetic resonance revealed significance of intramolecular hydrogen bonds in maintaining 3D structure of PF1171 hexapeptides. 3D structure-activity relationship study suggested that the 3D structure observed in the crystal is closely related to bioactivity. Based on the structure-activity relationship, we designed and synthesized molecular probes of PF1171 hexapeptides which can search for their target biomolecules.

Free Research Field

農芸化学、生物有機化学、ペプチド化学、核磁気共鳴