Peptide foldamers in drug discovery

2021 Fiscal Year Final Research Report

• Project/Area Number: 17K08385
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: National Institute of Health Sciences
• Principal Investigator: Demizu Yosuke 国立医薬品食品衛生研究所, 有機化学部, 部長 (90389180)
• Project Period (FY): 2017-04-01 – 2022-03-31
• Keywords: ペプチド / 非天然型アミノ酸 / 二次構造 / DDS / 抗菌ペプチド / PROTAC

Outline of Final Research Achievements

Next-generation medium-sized molecular peptide drugs are being developed around the world. To facilitate their practical application, well-controlled manufacturing methods and quality and safety evaluation methods based on the characteristics of these drugs should be established. In particular, peptide design which is able to form stable helical structures is one of the most important approaches to develop highly functionalized peptide-based drugs. In this research, helix-stabilized peptides were developed for application using DDS carriers, antimicrobials, and peptide-based PROTACs.

Free Research Field

ペプチド化学

Academic Significance and Societal Importance of the Research Achievements

本研究により得られた成果は、リードペプチド探索の方法、スクリーリングヒット率の向上に貢献でき、中分子ペプチド医薬品の開発効率化に資するためのレギュラトリーサイエンス研究の推進（品質、有効性、安全性の確保）にも繋げることができる。