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Development of Imaging Agents for Glutamine Transporter: In silico Binding Assay and Synthesis of Derivatives Derived from Tamoxifen and Tetrahydrobenzopyran
https://repo.qst.go.jp/records/72617
https://repo.qst.go.jp/records/72617a66869eb-0a72-45d8-ac57-8e1070358106
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-12-28 | |||||
| タイトル | ||||||
| タイトル | Development of Imaging Agents for Glutamine Transporter: In silico Binding Assay and Synthesis of Derivatives Derived from Tamoxifen and Tetrahydrobenzopyran | |||||
| 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 |
Yamaguchi, Hiroshi
× Yamaguchi, Hiroshi× Sumi, Takuya× Kang, Jiyoung× Yamashiro, Keiichi× Okada, Maki× Tateno, Masaru× Kato, Katsuhiko× Zhang, Ming-Rong× Watanabe, Hirohisa× Sobue, Gen× 山口 博司× 岡田 真希× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: The positoron emission tomography (PET) imaging is a useful method to investigate biological functions of receptor and transporter in CNS. The detection of the functional changes would also lead us to an early diagnosis of various brain diseases. In order to develope useful imaging agents that bind to glutamine transporter, we have examined tamoxifen delivatives that are known to affect the functions of glutamine transporter, by labelling some of the compounds with [18F] F- or [11C] CH3I, [11C] methyl trifluoromethanesulfonate. Methods: First, we performed an in silico binding assay by generating various derivetives of tamoxifen and tetrahydrobenzopyran, employing our protein-ligand docking calculation. Next, we synthesized the precursors of the obtianed delivatives: The derivatives derived from tamoxifen were conjugated to those of ketone by using the McMurry coupling reaction. The derivatives of tetrahydrobenzopyran were synthesized from diketone components and cyano analogues. After purification of the reaction mixture with the flash column chromatography procedure and recrystallization, we obtained the precursors, for labelling, which were reacted with [18F] F-or [11C] CH3I, [11C] methyl triflate on automatic synthesis system. Results: In the present study, we synthesized the 11C- or 18F-labelled derivatives derived from tamoxifen and tetrahydrobenzopyran. Currently, we are attempting to improve the yields and the resultant compounds in the labelling reaction. Conclusions: We have conducted an in silico binding assay and synthesized the labelled derivatives of tamoxifen and tetrahydrobenzopyran, that are thus possible ligands of glutamate transporter. The experiments using an in vivo small animal imaging device are also ongoing in our group. | |||||
| 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 | 22nd International symposium on radiopharmaceutical science (ISRS) | |||||
| 発表年月日 | ||||||
| 日付 | 2017-05-18 | |||||
| 日付タイプ | Issued | |||||
