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Development of imaging agents specific to GLT excluding the off-target binding
https://repo.qst.go.jp/records/73078
https://repo.qst.go.jp/records/73078259b83c2-abac-4b46-8a53-9888f4251004
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-12-10 | |||||
| タイトル | ||||||
| タイトル | Development of imaging agents specific to GLT excluding the off-target binding | |||||
| 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× Okada, Maki× Yamashiro, Keiichi× Tateno, Masaru× 山口 博司× 岡田 真希 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | [Background] In this study, imaging agents for glutamate transporter were aimed to be developed. The off-target bindings were eliminated from the existing inhibitors by employing computational docking examinations and structural informatics techniques, which thereby led to discovery of PET imaging agents to monitor the distributions specific to GLT in the brain. [Methods] An in silico binding assay was performed by using our protein-ligand docking simulations, where tamoxifen, which binds to both GLT and ERα proteins, was employed as an initial probe for the analysis. [Result] As a result of our analysis, the GLT-binding derivatives, which were hindered to bind to ERα, were obtained as derivatives of tamoxifen and tetrahydrobenzopyran. [Outlook] Radiolabeling of the designed molecules obtained by our in silico binding assay is now being considered toward utilizing them as the PET imaging agents. |
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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 | 第58回日本核医学会学術総会 | |||||
| 発表年月日 | ||||||
| 日付 | 2018-11-15 | |||||
| 日付タイプ | Issued | |||||
