| Project/Area Number |
17H07110
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| Research Category |
Grant-in-Aid for Research Activity Start-up
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| Allocation Type | Single-year Grants |
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| Research Field |
Radiation science
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| Research Institution | Showa Pharmaceutical University |
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Principal Investigator |
MIZUNO Yuki 昭和薬科大学, 薬学部, 特任助教 (90805194)
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| Research Collaborator |
AKIZAWA hiromichi
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| Project Period (FY) |
2017-08-25 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
Fiscal Year 2018: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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| Keywords | SPECT / メラノーマ / 多価効果 / テクネチウム-99m / インジウム-111 / イソニトリル |
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| Outline of Final Research Achievements |
In this study, we have developed α-MSH peptide based molecular imaging agents which target MC1R, overexpressed on metastatic melanoma. At the beginning of this project, we had planned to synthesize 99mTc-labeled hexavalent α-MSH peptides from monovalent isonitrile ligands. However, because we could not obtain the objective 99mTc-labeled hexavalent α-MSH probes due to unexpected side reactions, we instead synthesized DOTA conjugated bivalent MSH analogues and evaluated them in vitro. We compared linear MSH peptides and cyclic MSH peptides as an α-MSH analogue, and the results showed that 111In-labeled bivalent cyclic MSH peptides possessed superior targeting capability to melanoma compared with the linear MSH counterparts. These results show the potential of 111In-labeled bivalent cyclic MSH peptides as a novel melanoma imaging agent.
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| Academic Significance and Societal Importance of the Research Achievements |
今回の研究成果は、イソニトリル1価配位子から99mTc標識6価体を作製する薬剤設計が適応可能な標的指向性分子ついて、化学構造の観点から新たな知見を与えた。更に、環状MSHを分子内に2つ有する111In標識2価環状MSHを世界で初めて合成し、環状MSH間をつなぐスペーサ構造とメラノーマ細胞集積性との関係について評価した。これらの成果は、多価効果を基盤とした新たなMC1Rイメージング薬剤の開発において、有用な指針を与えるものであると考えられる。
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