Study on precise stereoscopic control method by intramolecular crosslinking of bioactive peptide

2017 Fiscal Year Final Research Report

• Project/Area Number: 15H04494
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Bioorganic chemistry
• Research Institution: Tokyo University of Agriculture and Technology
• Principal Investigator: Chiba Kazuhiro 東京農工大学, (連合)農学研究科(研究院), 教授 (20227325)
• Co-Investigator(Kenkyū-buntansha): 岡田 洋平 東京農工大学, 工学(系)研究科(研究院), 助教 (80749268)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: ペプチド / 化学合成 / 立体構造 / 生物活性 / 電解反応

Outline of Final Research Achievements

It is essential to develop a new chemical synthesis method that can convert peptide related substances into precisely designed structures including the stereochemistry required for the expression of activity. In this study, a novel peptide molecular cyclization method and intramolecular crosslinking formation control method are established, preconditionally controlled with three or more pairs of crosslinks at arbitrary positions in the molecule, using Conotoxin as a model. In addition, it was aimed to establish a novel chemical synthesis method capable of obtaining a peptide with high purity and high yield. As a result, we developed a new method to relax the rigid structure (conformation) of the chain peptide which interferes with the ring-forming reaction and remove the barrier of intramolecular crosslinking derived from the rigid conformation of the peptide. Based on these results, it was succeeded in developing a precise control method of a new three-dimensional structure.

Free Research Field

生物有機化学