| Budget Amount *help |
¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Outline of Final Research Achievements |
Targeted α-radionuclide therapy (TAT) is an upcoming powerful method for cancer treatment. One of halogens, 211At, has been attracting increasing attention as a novel α-particle emitting-radionuclide. A halogenated derivative of aromatic amino acid, FAMT (L-[3-18F]-α-methyltyrosine), developed as a PET tracer for tumor imaging exhibits an excellent cancer specificity. Therefore, substitution of 18F of FAMT with 211At would be a promising approach to develop a novel 211At-delivery agent for TAT. However, FAMT shows a significant background accumulation in kidney, due to the interaction with organic ion transporters in the renal proximal tubule. In this study, we used FAMT-related aromatic amino acid derivatives to reveal the molecular structures involved in the recognition by the renal organic ion transporters. This study gives significant implications for the development of a novel compound for TAT with high tumor specificity and low renal background accumulation.
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