Chemical approach towards identifying a putative receptor of N-phosphorylated proteins

2020 Fiscal Year Final Research Report

• Project/Area Number: 17K08382
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Nagasaki International University
• Principal Investigator: Yamaguchi Yasuchika 長崎国際大学, 薬学部, 教授 (10183980)
• Project Period (FY): 2017-04-01 – 2021-03-31
• Keywords: N-リン酸化 / ホスホヒスチジン / ペプチドライブラリー

Outline of Final Research Achievements

The original aim of this project was to develop a new methodology for finding unknown receptor proteins that recognize N-phosphorylated proteins. We used chemically stable N-phosphorylated amino acid analogs and peptides for our purpose. Thus, we tried to find out a new information system that uses N-phosphorylation as an intermediate.
So far what we have achieved are following: We have synthesized several stable phopho-amino acid analogs, which could be incorporated into peptide libraries. Within our library we discovered exceptionally active lead compounds for an infectious disease project. Since the medical need of this field is huge, we continue medicinal chemistry efforts with these findings.

Free Research Field

医薬品化学

Academic Significance and Societal Importance of the Research Achievements

当初の目的は、N－リン酸化タンパク質の受容体タンパク質を見つけ出す方法論の開発という基礎的なものであった。研究の過程で多くの新規化合物を合成した。これらを感染症プロジェクトの評価系にかけたところ、これまでの知見では説明できない活性化合物を発見できた。つまり新しいメカニズムをもつ医薬品創成に役立つ結果である。感染症分野の新薬の期待は大きいことから、この発見を実際の創薬につなげていく予定である。