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An efficient and rational method for selecting allosteric modulators to GABAA receptors using ligand-directed chemistry
https://repo.qst.go.jp/records/66729
https://repo.qst.go.jp/records/667299fb87fbc-831c-4c76-90e5-851e964b51cd
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-03-27 | |||||
| タイトル | ||||||
| タイトル | An efficient and rational method for selecting allosteric modulators to GABAA receptors using ligand-directed chemistry | |||||
| 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 |
Yamaura, Kei
× Yamaura, Kei× Kiyonaka, Shigeki× Sakamoto, Seiji× Hamachi, Itaru× 山浦 圭 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Allosteric modulators have drawn intense attention because of their high specificity and low toxicity relative to traditional compounds which bind to the orthosteric site of a target protein. However, it is hard to discover such allosteric modulators acting on membrane-proteins, important drug targets. As a result, development of these modulators has been stagnant in recent years. For example, benzodiazepines, allosteric modulators acting on GABAA receptors, are widely and clinically utilized as anxiolytic and sleep-inducing agents in spite of their drug resistance and addiction. Here, we developed a new method termed BFQRAP (Bimolecular Fluorescence Quenching and Recovery with Assistance of Positive allosteric modulator) using GABAAR-based semisynthetic fluorescent biosensors constructed by ligand-directed chemistry, which enables to rationally detect and select positive allosteric modulators that is bound to various allosteric sites of GABAAR. This method was applied to the high-throughput screening of a chemical library, leading to the discovery of new positive allosteric modulators functioning on GABAARs. |
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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 | 日本化学会 第98春季年会 (2018) | |||||
| 発表年月日 | ||||||
| 日付 | 2018-03-22 | |||||
| 日付タイプ | Issued | |||||
