{"created":"2023-05-15T15:02:00.363804+00:00","id":84101,"links":{},"metadata":{"_buckets":{"deposit":"14c31585-6aee-446c-9506-7fec76879fa0"},"_deposit":{"created_by":1,"id":"84101","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"84101"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00084101","sets":["10:28"]},"author_link":["1016565","1016578","1016576","1016572","1016577","1016575","1016564","1016573","1016570","1016583","1016574","1016566","1016582","1016568","1016561","1016580","1016569","1016579","1016563","1016567","1016562","1016581","1016571"],"item_10005_date_7":{"attribute_name":"発表年月日","attribute_value_mlt":[{"subitem_date_issued_datetime":"2021-11-29","subitem_date_issued_type":"Issued"}]},"item_10005_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Diacylglycerol kinase gamma (DGKγ) is a subtype of DGK enzyme which catalyzes ATP-dependent \nconversion of diacylglycerol to phosphatidic acid. DGKγ, localized in brain, plays some important role in \ncentral nervous system. However, its function has not been widely investigated. Positron emission tomography \n(PET) imaging of DGKγ validates target engagement of therapeutic DGKγ inhibitors and investigates DGKγ\nlevels under normal and disease conditions. In this study, we designed and synthesized a series of 3-acetyl \nindole derivatives as candidates for PET imaging agents for DGKγ. Among the synthesized compounds, 2-\n((3-acetyl-1-(6-methoxypyridin-3-yl)-2-methyl-1H-indol-5-yl)oxy)-N-methylacetamide (9) exhibited potent \ninhibitory activity (IC50 = 30 nM) against DGKγ and desirable physicochemical properties allowing efficient \nblood-brain barrier penetration and low levels of undesirable non-specific binding. The radio-labeling of 9\nfollowed by PET imaging of wild-type and DGKγ-deficient mice and rats indicated that [11C]9 ([11C]T-278) \nspecifically binds to DGKγ and yields a high signal-noise ratio for DGKγ in rodent brains.","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":"AIMECS 2021","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":"Hattori, Yasushi"}],"nameIdentifiers":[{"nameIdentifier":"1016561","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Tomoteru, Yamasaki"}],"nameIdentifiers":[{"nameIdentifier":"1016562","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ohashi, Tomohiro"}],"nameIdentifiers":[{"nameIdentifier":"1016563","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Miyanohana, Yuhei"}],"nameIdentifiers":[{"nameIdentifier":"1016564","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kusumoto, Tomokazu"}],"nameIdentifiers":[{"nameIdentifier":"1016565","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Ryouta"}],"nameIdentifiers":[{"nameIdentifier":"1016566","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Miyamoto, Maki"}],"nameIdentifiers":[{"nameIdentifier":"1016567","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Debori, Yasuyuki"}],"nameIdentifiers":[{"nameIdentifier":"1016568","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hata, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"1016569","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"1016570","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hidekatsu, Wakizaka"}],"nameIdentifiers":[{"nameIdentifier":"1016571","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Takeshi, Wakabayashi"}],"nameIdentifiers":[{"nameIdentifier":"1016572","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga"}],"nameIdentifiers":[{"nameIdentifier":"1016573","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamashita, Ryo"}],"nameIdentifiers":[{"nameIdentifier":"1016574","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"1016575","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Koike, Tatsuki"}],"nameIdentifiers":[{"nameIdentifier":"1016576","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hattori, Yasushi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1016577","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Tomoteru, Yamasaki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1016578","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1016579","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hidekatsu, Wakizaka","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1016580","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Takeshi, Wakabayashi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1016581","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1016582","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1016583","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":"Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetyl-indole 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-Acetyl-indole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain"}]},"item_type_id":"10005","owner":"1","path":["28"],"pubdate":{"attribute_name":"公開日","attribute_value":"2021-08-13"},"publish_date":"2021-08-13","publish_status":"0","recid":"84101","relation_version_is_last":true,"title":["Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetyl-indole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T18:39:48.949908+00:00"}