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Novel 18F‑Labeled α‑Methyl-Phenylalanine Derivative with High Tumor Accumulation and Ideal Pharmacokinetics for Tumor-Specific Imaging
https://repo.qst.go.jp/records/76482
https://repo.qst.go.jp/records/76482ba2632d4-77f4-4795-83a0-adc82214b1e7
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2019-08-02 | |||||
| タイトル | ||||||
| タイトル | Novel 18F‑Labeled α‑Methyl-Phenylalanine Derivative with High Tumor Accumulation and Ideal Pharmacokinetics for Tumor-Specific Imaging | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
花岡, 宏史 群馬大学大学院医学系研究科
× 花岡, 宏史 群馬大学大学院医学系研究科× Oshima, Yasuhiro× 山口, 藍子 群馬大学大学院医学系研究科× 鈴木, 博元 千葉大学大学院薬学研究院× Ishioka, Noriko× 樋口, 徹也 群馬大学大学院医学系研究科× 荒野, 泰 千葉大学大学院薬学研究院× 対馬, 義人 群馬大学大学院医学系研究科× Oshima, Yasuhiro× Ishioka, Noriko |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Positron emission tomography (PET) imaging with 18F-labeled α-methyl-substituted amino acids exerts significant influence on differential diagnosis of malignant tumors and tumor-like lesions. We newly designed 18F-labeled α-methyl-phenylalanine (18F-FAMP) regioisomers (2-, 3-, or 4-18F-FAMP) and stereoisomers (L- or D-form), and we evaluated their potential as tumor-imaging agents. In tumor bearing mice, L-2-18F-FAMP exhibited significantly higher tumor accumulation than the D-18F-FAMPs or a clinically relevant tracer, L-3-18F-α-methyl-tyrosine (18F-FAMT) (p < 0.05). Specificity of L-2-18F-FAMP for L-type amino acid transporter-1, a tumor-specific transporter, was validated in the cellular uptake studies. The PET imaging with L-2-18F-FAMP clearly visualized the tumor as early as 1 h after injection, and the high tumor accumulation level was retained for 3 h. These findings suggest that L-2-18F-FAMP constitutes a potential PET tracer for tumor-specific imaging. | |||||
| 書誌情報 |
Molecular Pharmaceutics 巻 16, 号 8, p. 3609-3616, 発行日 2019-07 |
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| 出版者 | ||||||
| 出版者 | ACS Publications | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1543-8384 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/acs.molpharmaceut.9b00446 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.9b00446 | |||||
