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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/73078
259b83c2-abac-4b46-8a53-9888f4251004
アイテムタイプ 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 output
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

WEKO 720115

Yamaguchi, Hiroshi

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Sumi, Takuya

× Sumi, Takuya

WEKO 720116

Sumi, Takuya

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Kang, Jiyoung

× Kang, Jiyoung

WEKO 720117

Kang, Jiyoung

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Okada, Maki

× Okada, Maki

WEKO 720118

Okada, Maki

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Yamashiro, Keiichi

× Yamashiro, Keiichi

WEKO 720119

Yamashiro, Keiichi

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Tateno, Masaru

× Tateno, Masaru

WEKO 720120

Tateno, Masaru

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山口 博司

× 山口 博司

WEKO 720121

en 山口 博司

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岡田 真希

× 岡田 真希

WEKO 720122

en 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.
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
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