Intracellular delivery of functional peptides and maintain of the activity by "peptide nucleic acid zipper" method

2022 Fiscal Year Final Research Report

• Project/Area Number: 20K05714
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 37010:Bio-related chemistry
• Research Institution: Kindai University
• Principal Investigator: KITAMATSU Mizuki 近畿大学, 理工学部, 准教授 (60379716)
• Project Period (FY): 2020-04-01 – 2023-03-31
• Keywords: ペプチド / ペプチド核酸 / 細胞内運搬ペプチド / オートファジー

Outline of Final Research Achievements

The purpose of this study is to deliver functional peptides into cells without impairing their bioactivity. For this purpose, we developed a method (PNA zipper method) to connect and separate functional peptides and cell-penetrating peptides (CPP) via peptide nucleic acid (PNA). The intracellular activity of functional peptides delivered by this method was assessed.
As a result, we found that the PNA zipper can transport the functional peptide into the cell as expected, and that the functional peptide exhibits a stronger bioactivity in the cell than the direct conjugate. In addition, we optimized the chain length of PNA used for the PNA zipper method.

Free Research Field

生物有機化学

Academic Significance and Societal Importance of the Research Achievements

ペプチドを用いた医薬開発は、その多様性や副作用の低減を期待できます。しかし、現在のペプチド医薬の多くは、細胞表面の物質を標的にしています。細胞内部には病気と関係するより多くの物質が存在するため、ペプチド医薬を細胞内に安全に輸送する技術があれば、現行よりもさらに多くの病気をペプチド医薬によって治療することができます。本法は、この細胞内へのペプチド医薬の運搬と細胞内の物質を標的としたペプチド医薬の能力向上に役立ちます。