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Development of quantum scientific/therapeutic tool: Synthesis and therapeutic effect of At-211 labeled probe for melanoma with overexpressed metabotropic glutamate receptor 1
https://repo.qst.go.jp/records/72393
https://repo.qst.go.jp/records/7239307317c27-9cbf-40e8-a032-6080fae23433
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-07-27 | |||||
| タイトル | ||||||
| タイトル | Development of quantum scientific/therapeutic tool: Synthesis and therapeutic effect of At-211 labeled probe for melanoma with overexpressed 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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 |
Hanyu, Masayuki
× Hanyu, Masayuki× Fujinaga, Masayuki× Xie, Lin× Zhang, Yiding× Morokoshi, Yukie× Keiko, Li Huizi× Minegishi, Katsuyuki× Hasegawa, Sumitaka× Nagatsu, Kotaro× Zhang, Ming-Rong× 破入 正行× 藤永 雅之× 謝 琳× 張 一鼎× 諸越 幸恵× 峯岸 克行× 長谷川 純崇× 永津 弘太郎× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Metabotropic glutamate receptor 1 (mGluR1) is found ectopically in various kinds of cancers, such as melanoma and breast cancer. It has been reported that overexpressed mGluR1 exhibited oncogenic characteristics that independently trigger melanocyte tumorigenesis. Further, inhibition or inactivation of mGlu1 was demonstrated to prevent growth and progression of melanomas. Recently, we developed 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide ([18F]FITM) and its other halogen-substituted analogs as PET probes for in vivo imaging of mGluR1 in melanoma. In this study, we synthesized 4-[211At]astato-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide ([211At]1) and evaluated their antitumoral effects on mice bearing B16F10 melanoma. 211At was produced using a remotely controlled versatile system developed in house. Synthesis of [211At]1 was performed by reaction of tin precursor with 211At (74~222 MBq in 2%AcOH/MeOH) in the presence of N-chlorosccinimide (1 mg/mL) at room temperature for 20 min. After purification and formulation, [211At]1 was obtained in 25.7±7.8 % radiochemical yield and radiochemical purity of [211At]1 was >99% at the end of synthesis (n=3, based on the total 211At). Treatment the B16F10-bearing mice with [211At]1 at 1.85 MBq in 1 doses/mouse significantly reduced the tumor volumes (P < 0.05). | |||||
| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | QST第1回国際シンポジウム『量子生命科学 -Quantum Life Science-』 | |||||
| 発表年月日 | ||||||
| 日付 | 2017-07-25 | |||||
| 日付タイプ | Issued | |||||
