{"created":"2023-05-15T14:52:38.474490+00:00","id":71871,"links":{},"metadata":{"_buckets":{"deposit":"18938b12-902e-4a4c-9cc7-bec3577cf14c"},"_deposit":{"created_by":1,"id":"71871","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"71871"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00071871","sets":["10:28"]},"author_link":["707761","707755","707759","707771","707769","707762","707757","707753","707772","707760","707766","707763","707765","707768","707770","707756","707764","707767","707758","707754"],"item_10005_date_7":{"attribute_name":"発表年月日","attribute_value_mlt":[{"subitem_date_issued_datetime":"2015-11-09","subitem_date_issued_type":"Issued"}]},"item_10005_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Objectives:  1-Methyl-tryptophan (1MTrp) is known as a specific inhibitor targeting the immune- checkpoint protein indoleamine-2,3-dioxygenase, in two stereoisomers of levorotary (L) and dextrorotary (D) (1). A long-standing debate exists in immunology and oncology: which stereoisomer has the potential of antitumor immunotherapy (2). As a first step to disentangle the potential and explore the possibility of pharmacokinetic imaging in immunotherapy, we here developed two novel radioprobes, 1-N-[11C]methyl-L- and -D-tryptophan ([11C]L-1MTrp and [11C]D-1-MTrp), without modifying the chemical structures of the two isomers, and delineated their pharmacokinetic imaging in whole body. \nMethods: [11C]L-1MTrp and [11C]D-1MTrp were synthesized by reaction of the corresponding Boc-Trp-OEt with [11C]CH3I at 80 °C for 5 min, followed by deprotection with 2 N HCl at 100 °C for 5 min. The pharmacokinetics of the L and D isomers were tracked using dynamic PET/CT scans and biodistribution study after the radioprobes injection.\nResults: [11C]L-1MTrp and [11C]D-1MTrp were obtained with radiochemical yields of 47 ± 6.3% (decay-corrected, based on [11C]CO2), a radiochemical purity of > 98%, specific activity of 47130 GBq/μmol, and high enantiomeric purity. PET/CT imaging in rats revealed that for [11C]L-1MTrp, the highest distribution of radioactivity was observed in the pancreas, while for [11C]D-1MTrp, it was observed in the kidney (Fig. 1). Ex vivo biodistribution confirmed the PET/CT results, indicating the differences in pharmacokinetics between the two isomers. \nConclusion: Both [11C]L-1MTrp and [11C]D-1MTrp are therefore useful PET probes for delineating the distribution and action of the checkpoint inhibitor 1MTrp in vivo. This study represents the first step toward using whole-body and real-time insight to disentangle the antitumor potential of the two stereoisomers of 1MTrp, and it can facilitate the development of 1MTrp immunotherapy.","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":"Ninth Japan-China Joint Seminar on Radiopharmaceutical Chemistry","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":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"707753","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Jun"}],"nameIdentifiers":[{"nameIdentifier":"707754","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"707755","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yui, Joji"}],"nameIdentifiers":[{"nameIdentifier":"707756","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"707757","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"707758","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"707759","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakizaka, Hidekatsu"}],"nameIdentifiers":[{"nameIdentifier":"707760","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"707761","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"707762","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"謝 琳","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707763","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"前田 純","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707764","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"熊田 勝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707765","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"由井 譲二","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707766","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 一鼎","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707767","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"羽鳥 晶子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707768","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"念垣 信樹","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707769","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"脇坂 秀克","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707770","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤永 雅之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707771","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"707772","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":"Development of 1-N-[11C]-Methyl-L- and -D-Tryptophan for Pharmacokinetic Imaging of the Immune Checkpoint Inhibitor 1-Methyl-Tryptophan","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Development of 1-N-[11C]-Methyl-L- and -D-Tryptophan for Pharmacokinetic Imaging of the Immune Checkpoint Inhibitor 1-Methyl-Tryptophan"}]},"item_type_id":"10005","owner":"1","path":["28"],"pubdate":{"attribute_name":"公開日","attribute_value":"2015-11-25"},"publish_date":"2015-11-25","publish_status":"0","recid":"71871","relation_version_is_last":true,"title":["Development of 1-N-[11C]-Methyl-L- and -D-Tryptophan for Pharmacokinetic Imaging of the Immune Checkpoint Inhibitor 1-Methyl-Tryptophan"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T19:46:26.061053+00:00"}