Studies to develop peptide ligation catalysts enabling easier and faster protein synthesis

2022 Fiscal Year Final Research Report

• Project/Area Number: 19H03348
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Review Section: Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
• Research Institution: The University of Tokyo
• Principal Investigator: Yamatsugu Kenzo 東京大学, 大学院薬学系研究科(薬学部), 助教 (30646807)
• Project Period (FY): 2019-04-01 – 2023-03-31
• Keywords: タンパク質 / ペプチド / ライゲーション / 触媒

Outline of Final Research Achievements

This research aims to develop chemical catalysts that simplify the chemical synthesis of proteins. Specifically, we aimed to develop a catalyst that simultaneously activates a peptide C-terminal thioester and a peptide N-terminus and ligates them. As a result, we succeeded in finding catalysts that activate the C-terminus and the N-terminus respectively, but were unable to fuse them into a single catalyst while maintaining their activity. Based on the knowledge obtained in this study, we will focus on developing N-terminal activating catalysts that can coexist with C-terminal activating catalysts, in order to develop catalysts that will revolutionize and simplify protein chemical synthesis.

Free Research Field

有機化学

Academic Significance and Societal Importance of the Research Achievements

本研究ではタンパク質の化学合成を革新的に簡単にする化学触媒の開発を目指し、ペプチドC末端チオエステルとペプチドN末端を同時に活性化して連結する触媒の開発を目的とした。結果として、C末端、N末端それぞれを活性化する触媒を見出すことに成功したが、それらを一つの触媒として融合させることは出来なかった。得られた知見をもとに検討を重ねることで、タンパク質の化学合成を簡便にする触媒の開発を可能にしたい。