{"created":"2023-05-15T14:48:42.641295+00:00","id":66729,"links":{},"metadata":{"_buckets":{"deposit":"b5cd0932-596d-43f7-b49c-15d0b82412f8"},"_deposit":{"created_by":1,"id":"66729","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"66729"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00066729","sets":["10:29"]},"author_link":["656194","656191","656195","656193","656192"],"item_10005_date_7":{"attribute_name":"発表年月日","attribute_value_mlt":[{"subitem_date_issued_datetime":"2018-03-22","subitem_date_issued_type":"Issued"}]},"item_10005_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"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.\n     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.","subitem_description_type":"Abstract"}]},"item_10005_description_6":{"attribute_name":"会議概要（会議名, 開催地, 会期, 主催者等）","attribute_value_mlt":[{"subitem_description":"日本化学会 第98春季年会 (2018)","subitem_description_type":"Other"}]},"item_access_right":{"attribute_name":"アクセス権","attribute_value_mlt":[{"subitem_access_right":"metadata only access","subitem_access_right_uri":"http://purl.org/coar/access_right/c_14cb"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"Yamaura, Kei"}],"nameIdentifiers":[{"nameIdentifier":"656191","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kiyonaka, Shigeki"}],"nameIdentifiers":[{"nameIdentifier":"656192","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sakamoto, Seiji"}],"nameIdentifiers":[{"nameIdentifier":"656193","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hamachi, Itaru"}],"nameIdentifiers":[{"nameIdentifier":"656194","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山浦 圭","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"656195","nameIdentifierScheme":"WEKO"}]}]},"item_language":{"attribute_name":"言語","attribute_value_mlt":[{"subitem_language":"eng"}]},"item_resource_type":{"attribute_name":"資源タイプ","attribute_value_mlt":[{"resourcetype":"conference object","resourceuri":"http://purl.org/coar/resource_type/c_c94f"}]},"item_title":"An efficient and rational method for selecting allosteric modulators to GABAA receptors using ligand-directed chemistry","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"An efficient and rational method for selecting allosteric modulators to GABAA receptors using ligand-directed chemistry"}]},"item_type_id":"10005","owner":"1","path":["29"],"pubdate":{"attribute_name":"公開日","attribute_value":"2018-03-27"},"publish_date":"2018-03-27","publish_status":"0","recid":"66729","relation_version_is_last":true,"title":["An efficient and rational method for selecting allosteric modulators to GABAA receptors using ligand-directed chemistry"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T20:45:37.877578+00:00"}