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Development and radiotherapeutic effect of two novel I-131 or At-211 labelled radioprobes for melanoma with overexpressed metabotropic glutamate receptor 1
https://repo.qst.go.jp/records/72760
https://repo.qst.go.jp/records/72760593af2cd-5904-40bd-bb7b-0f9b88d8ee32
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-04-27 | |||||
| タイトル | ||||||
| タイトル | Development and radiotherapeutic effect of two novel I-131 or At-211 labelled radioprobes 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× Xie, Lin× Fujinaga, Masayuki× Zhang, Yiding× Hatori, Akiko× Morokoshi, Yukie× Li, Huizi× Minegishi, Katsuyuki× Hasegawa, Sumitaka× Nagatsu, Kotaro× Zhang, Ming-Rong× 破入 正行× 謝 琳× 藤永 雅之× 張 一鼎× 羽鳥 晶子× 諸越 幸恵× 李 惠子× 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 | Background / Aims: Ectopically expressed metabotropic glutamate receptor 1 (mGluR1) independently induces melanocyte carcinogenesis [1], and it is therefore becoming an important target for personalized diagnosis and treatment strategies for melanomas [2,3]. Recently, we developed [18F]FITM and its other radiohalogen-substituted probes for PET imaging of mGluR1 in melanoma [3,4]. In this study, we synthesized 4-[131I]iodo ([131I]1)- or 4-[211At]astato ([211At]1)- N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide as two target-radionuclide-therapy probes and evaluated their antitumor effects on mice bearing B16F10 melanoma. Methods: Unlabeled 1 and its tin precursor for radiosynthesis were prepared according to the method reported by our laboratory [2,3]. Radiosynthesis of [131I]1 was performed by reaction of tin precursor with [131I]NaI in the presence of 30% H2O2 at room temperature for 2 h. 211At for radiolabeling was produced using a remotely controlled versatile system developed in house [5]. The anti-tumor effect of two radioprobes was evaluated in the mice bearing B16F10 melanoma with rich mGluR1 expression. Animal studies were approved by the Animal Ethics Committee of the National Institutes for Quantum and Radiological Science and Technology. \nResults: After purification and formulation, [131I]1 was obtained in 45 ± 20% radiochemical yield (n > 3, based on the total [131I]NaI). The molar radioactivity and radiochemical purity of [131I]1 were 40 ± 4 GBq/μmol and >99%. [211At]1 was successfully synthesized by the reaction of tin precursor with 211At in the presence of N-chlorosuccinimide at room temperature for 1 h. The radiochemical conversion of [211At]1 exceeded 40%. Treatment the B16F10-bearing mice with [131I]1 at 18 MBq and 9 MBq in 2 doses/mouse reduced the tumor volumes (P < 0.05), compared to the untreated group. Further, the administration of [211At]1 at 1.1 MBq in single doses/mouse significantly inhibited B16F10-melanoma growth, resulted in tumor regression and a durable anti-tumor response. \nConclusions: [131I]1 and [211At]1 are useful radioprobes for targeted radiotherapy of melanoma with overexpressed mGluR1. \nReferences: [1]. Pollock PM, et al. Nat Genet, 2003, 34,108-112. [2] L. Xie, et al. Int J Cancer, 2014, 135, 1852-59. [3] M. Fujinaga, et al. J Med Chem, 2015, 58, 1513-23. [4] M. Fujinaga, et al. J Med Chem, 2012, 55, 11042-51. [5] K. Nagatsu, et al. Appl Radiat Isot, 2014, 94, 363-71. |
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| 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 | 12th Congress of the World federation of Nuclear Medicine and Biology | |||||
| 発表年月日 | ||||||
| 日付 | 2018-04-23 | |||||
| 日付タイプ | Issued | |||||
