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131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1
https://repo.qst.go.jp/records/78127
https://repo.qst.go.jp/records/78127743d1503-bee8-4a09-9719-fdfaf836f9b5
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2019-12-20 | |||||
| タイトル | ||||||
| タイトル | 131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1 | |||||
| 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 |
Xie, Lin
× Xie, Lin× Hanyu, Masayuki× Fujinaga, Masayuki× Zhang, Yiding× Kuan, Hu× Minegishi, Katsuyuki× Jiang, Cuiping× Kurosawa, Fuki× Morokoshi, Yukie× Li, Huizi× Hasegawa, Sumitaka× Nagatsu, Kotaro× Ming-Rong, Zhang× Lin, Xie× Masayuki, Hanyu× Masayuki, Fujinaga× Zhang, Yiding× Kuan, Hu× Katsuyuki, Minegishi× Fuki, Kurosawa× Yukie, Morokoshi× Li, Huizi× Sumitaka, Hasegawa× Kotaro, Nagatsu× Zhang, Ming-Rong |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Targeted radionuclide therapy (TRT) targeting oncoproteins facilitates the delivery of therapeutic radionuclides to tumor tissues with high precision. Herein, we developed two new radiopharmaceuticals, 4-131I-iodo- and 4-211At-astato-N-[4-(6-(isopropylamino)pyridine-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide (131I-IITM and 211At-AITM), targeting the ectopic metabotropic glutamate receptor 1 (mGluR1) in melanomas for TRT studies. Methods: 131I-IITM and 211At-AITM were synthesized by reacting a stannyl precursor with 131I-NaI and 211At in the presence of an oxidizing agent. The therapeutic efficacy and safety of the two radiopharmaceuticals were investigated using mGluR1-expressing B16F10 melanoma cells and melanoma-bearing mice. Results: 131I-IITM and 211At-AITM were obtained with radiochemical purity of >99% and radiochemical yields of 42.7% ± 10.4% and 28.9% ± 9.9%, respectively, based on the total radioactivity of used radionuclides. 131I-IITM and 211At-AITM exhibited maximum uptakes of 4.66% ± 0.70% ID/g and 7.68% ± 0.71% ID/g in the targeted melanomas, respectively, and were rapidly cleared from non-target organs after intravenous injection. Both agents markedly inhibited melanoma growth compared with the controls (61.00% and 95.68%, respectively). In the melanoma model, considerably greater therapeutic efficacy with negligible toxicity was observed using 211At-AITM. Conclusion: The non-toxic radiopharmaceuticals 131I-IITM and 211At-AITM are useful high-precision TRT agents that can be used to target the oncoprotein mGluR1 for melanoma therapy. | |||||
| 書誌情報 |
The Journal of Nuclear Medicine 巻 61, 号 2, p. 242-248, 発行日 2019-08 |
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| 出版者 | ||||||
| 出版者 | Society of Nuclear Medicine and Molecular Imaging | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0161-5505 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.2967/jnumed.119.230946 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | http://jnm.snmjournals.org/content/61/2/242.long | |||||
