2022 Fiscal Year Final Research Report
Develoment of Radiometal Complexes for Selective Modification of Specific Amino Acids
| Project/Area Number |
21K19446
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| Research Category |
Grant-in-Aid for Challenging Research (Exploratory)
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| Allocation Type | Multi-year Fund |
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| Review Section |
Medium-sized Section 52:General internal medicine and related fields
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| Research Institution | Kyoto University |
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Principal Investigator |
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| Project Period (FY) |
2021-07-09 – 2023-03-31
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| Keywords | ラジオセラノスティクス / アミノ酸 / ケミカルラベリング |
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| Outline of Final Research Achievements |
In this study, a novel compound (TBD-DO3A-1) was designed and synthesized by introducing DO3A, a DOTA derivative, into a triazabutadiene (TBD) scaffold for the purpose of modifying tyrosine residues. Then, cRGDyK was selected as a model peptide, and tyrosine modification and In-111 labeling were performed. As a result, we obtained [111In]In-Tyr-TBD-DO3A-1, the target labeled compound, in high radiochemical yield and with high radiochemical purity. Furthermore, it was stable in mouse plasma, suggesting the usefulness of this labeling method.
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| Free Research Field |
放射性医薬品学
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| Academic Significance and Societal Importance of the Research Achievements |
本研究において，放射性金属核種を用いたチロシン残基特異的標識法の開発に成功した．現在までに確立されている放射性金属核種を用いたアミノ酸修飾法は，リジン残基やN末端のアミノ酸残基のアミノ基をスクシンイミド基によって修飾する手法とシステイン残基のチオール基をマレイミド基によって修飾する手法の二つである.したがって，本手法の開発によって，従来に比べて多彩な分子設計が可能となり，放射性金属核種を用いたがんの診断・治療(セラノスティクス)に有効な新規薬剤の創出につながると考えられる．
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