{"created":"2023-05-15T15:02:51.902277+00:00","id":85193,"links":{},"metadata":{"_buckets":{"deposit":"a5c34ed0-8f97-42f5-961f-2b40cff5b038"},"_deposit":{"created_by":1,"id":"85193","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"85193"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00085193","sets":["1"]},"author_link":["1027005","1027009","1027008","1027013","1026995","1027007","1027014","1026998","1027017","1026999","1027006","1027016","1027002","1027012","1026997","1027001","1027011","1027010","1027015","1027003","1026996","1027000","1027004"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2021-08","bibliographicIssueDateType":"Issued"},"bibliographicPageEnd":"12002","bibliographicPageStart":"11990","bibliographicVolumeNumber":"64","bibliographic_titles":[{"bibliographic_title":"Journal of Medicinal Chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Diacylglycerol kinase gamma (DGKγ) is a subtype of DGK enzyme which catalyzes ATPdependent conversion of diacylglycerol to phosphatidic acid. DGKγ, localized in brain, plays some important role in central nervous system. However, its function has not been widely investigated. Positron emission tomography (PET) imaging of DGKγ validates target engagement of therapeutic DGKγ inhibitors and investigates DGKγ levels under normal and disease conditions. In this study, we designed and synthesized a series of 3-acetyl indole\nderivatives as candidates for PET imaging agents for DGKγ. Among the synthesized compounds, 2-((3-acetyl-1-(6-methoxypyridin-3-yl)-2-methyl-1H-indol-5-yl)oxy)-N-methylacetamide (9) exhibited potent inhibitory activity (IC50 = 30 nM) against DGKγ and desirable physicochemical properties allowing efficient blood-brain barrier penetration and low levels of undesirable nonspecific\nbinding. The radio-labeling of 9 followed by PET imaging of wild-type and DGKγ-\ndeficient mice and rats indicated that [11C]9 ([11C]T-278) specifically binds to DGKγ and yields a high signal-noise ratio for DGKγ in rodent brains.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"ACS"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1021/acs.jmedchem.1c00584","subitem_relation_type_select":"DOI"}}]},"item_8_relation_17":{"attribute_name":"関連サイト","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c00584","subitem_relation_type_select":"URI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0022-2623","subitem_source_identifier_type":"ISSN"}]},"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":"Hattori, Yasushi"}],"nameIdentifiers":[{"nameIdentifier":"1026995","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Tomoteru, Yamasaki"}],"nameIdentifiers":[{"nameIdentifier":"1026996","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ohashi, Tomohiro"}],"nameIdentifiers":[{"nameIdentifier":"1026997","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Miyanohana, Yuhei"}],"nameIdentifiers":[{"nameIdentifier":"1026998","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kusumoto, Tomokazu"}],"nameIdentifiers":[{"nameIdentifier":"1026999","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Ryouta"}],"nameIdentifiers":[{"nameIdentifier":"1027000","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Miyamoto, Maki"}],"nameIdentifiers":[{"nameIdentifier":"1027001","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Debori, Yasuyuki"}],"nameIdentifiers":[{"nameIdentifier":"1027002","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hata, Akito"}],"nameIdentifiers":[{"nameIdentifier":"1027003","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"1027004","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hidekatsu, Wakizaka"}],"nameIdentifiers":[{"nameIdentifier":"1027005","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Takeshi, Wakabayashi"}],"nameIdentifiers":[{"nameIdentifier":"1027006","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga"}],"nameIdentifiers":[{"nameIdentifier":"1027007","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamashita, Ryo"}],"nameIdentifiers":[{"nameIdentifier":"1027008","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"1027009","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Koike, Tatsuki"}],"nameIdentifiers":[{"nameIdentifier":"1027010","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hattori, Yasushi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027011","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Tomoteru, Yamasaki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027012","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027013","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hidekatsu, Wakizaka","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027014","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Takeshi, Wakabayashi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027015","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027016","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027017","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":"journal article","resourceuri":"http://purl.org/coar/resource_type/c_6501"}]},"item_title":"Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetylindole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetylindole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2021-07-26"},"publish_date":"2021-07-26","publish_status":"0","recid":"85193","relation_version_is_last":true,"title":["Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetylindole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T17:56:59.109716+00:00"}