Development of radiolabeled multivalent RGD peptides which display high and persistent uptake in cancerous tissues

2021 Fiscal Year Final Research Report

• Project/Area Number: 20K16803
• Research Category: Grant-in-Aid for Early-Career Scientists
• Allocation Type: Multi-year Fund
• Review Section: Basic Section 52040:Radiological sciences-related
• Research Institution: Hokkaido University
• Principal Investigator: Mizuno Yuki 北海道大学, アイソトープ総合センター, 助教 (90805194)
• Project Period (FY): 2020-04-01 – 2022-03-31
• Keywords: 多価効果 / がん / インテグリン / ペプチド / 核医学治療 / 核医学診断

Outline of Final Research Achievements

In this study, we synthesized several radiolabeled multivalent RGD peptides targeting integrin αvβ3 and evaluated how the difference in their molecular structures affects their interactions with integrin αvβ3. As a result, we found that the difference in their scaffold structures connecting each RGD peptide substantially affected their dissociation kinetics from integrin αvβ3 positive cells. Furthermore, our results also suggested that multivalent RGD peptides whose scaffold structure is an octahedral metal complex could simultaneously bind with more than one integrin αvβ3 receptors.

Free Research Field

放射性薬品科学

Academic Significance and Societal Importance of the Research Achievements

本研究を通して、多価RGDペプチドが複数のintegrin αvβ3と同時結合するために必要な化学構造について、新たな知見が得られた。これにより、integrin αvβ3を標的とした多価RGDペプチドの開発を、より合理的な薬剤設計に基づき実施することが可能となる。Integrin αvβ3は多くのがん種において発現が亢進することが知られているため、integrin αvβ3への高い集積性と滞留性を示すRI標識多価RGDの開発は、新たながん診断・治療法へとつながることが期待できる。