Development of a halogenated derivative of aromatic amino acids for the targeted alpha-radionuclide therapy with high tumor specificity and low renal background.
Project/Area Number |
16H06942
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Research Category |
Grant-in-Aid for Research Activity Start-up
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Allocation Type | Single-year Grants |
Research Field |
General pharmacology
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Research Institution | Osaka University |
Principal Investigator |
Wei Ling 大阪大学, 医学系研究科, 特任助教(常勤) (80783638)
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Project Period (FY) |
2016-08-26 – 2017-03-31
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Project Status |
Completed (Fiscal Year 2016)
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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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Keywords | 癌 / α線内用療法 / トランスポーター / 構造活性相関 / ハロゲン化芳香族アミノ酸誘導体 |
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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Report
(2 results)
Research Products
(4 results)
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[Journal Article] Interaction of the Sodium/Glucose Cotransporter (SGLT) 2 inhibitor Canagliflozin with SGLT1 and SGLT2: Inhibition kinetics, sidedness of action, and transporter-associated incorporation accounting for its pharmacodynamic and pharmacokinetic features.2016
Author(s)
Ohgaki R, Wei L, Yamada K, Hara T, Kuriyama C, Okuda S, Ueta K, Shiotani M, Nagamori S, Kanai Y.
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Journal Title
J Pharmacol Exp Ther.
Volume: 358
Issue: 1
Pages: 94-102
DOI
Related Report
Peer Reviewed / Int'l Joint Research
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[Journal Article] Expression of a human NPT1/SLC17A1 missense variant which increases urate export.2016
Author(s)
Sakiyama M, Matsuo H, Nagamori S, Wei L, Kawamura Y, Nakayama A, Higashino T, Chiba T, Ichida K, Kanai Y, Shinomiya N.
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Journal Title
Nucleosides Nucleotides Nucleic Acids.
Volume: 35
Pages: 536-542
Related Report
Peer Reviewed
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