{"created":"2023-05-15T14:57:33.975530+00:00","id":78127,"links":{},"metadata":{"_buckets":{"deposit":"a9e59c37-f750-400d-b680-0224c02f75f8"},"_deposit":{"created_by":1,"id":"78127","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"78127"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00078127","sets":["1"]},"author_link":["1000015","1000021","1000012","1000008","1000016","1000020","1000017","1000006","1000013","1000022","1000023","1000011","1000010","1000014","1000027","1000007","1000004","1000024","1000025","1000019","1000026","1000028","1000005","1000018","1000009"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2019-08","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"2","bibliographicPageEnd":"248","bibliographicPageStart":"242","bibliographicVolumeNumber":"61","bibliographic_titles":[{"bibliographic_title":"The Journal of Nuclear Medicine"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Targeted radionuclide therapy (TRT) targeting oncoproteins facilitates the delivery of therapeutic radionuclides to tumor tissues with high precision. Herein, we developed two new radiopharmaceuticals, 4-131I-iodo- and 4-211At-astato-N-[4-(6-(isopropylamino)pyridine-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide (131I-IITM and 211At-AITM), targeting the ectopic metabotropic glutamate receptor 1 (mGluR1) in melanomas for TRT studies. Methods: 131I-IITM and 211At-AITM were synthesized by reacting a stannyl precursor with 131I-NaI and 211At in the presence of an oxidizing agent. The therapeutic efficacy and safety of the two radiopharmaceuticals were investigated using mGluR1-expressing B16F10 melanoma cells and melanoma-bearing mice. Results: 131I-IITM and 211At-AITM were obtained with radiochemical purity of >99% and radiochemical yields of 42.7% ± 10.4% and 28.9% ± 9.9%, respectively, based on the total radioactivity of used radionuclides. 131I-IITM and 211At-AITM exhibited maximum uptakes of 4.66% ± 0.70% ID/g and 7.68% ± 0.71% ID/g in the targeted melanomas, respectively, and were rapidly cleared from non-target organs after intravenous injection. Both agents markedly inhibited melanoma growth compared with the controls (61.00% and 95.68%, respectively). In the melanoma model, considerably greater therapeutic efficacy with negligible toxicity was observed using 211At-AITM. Conclusion: The non-toxic radiopharmaceuticals 131I-IITM and 211At-AITM are useful high-precision TRT agents that can be used to target the oncoprotein mGluR1 for melanoma therapy. ","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Society of Nuclear Medicine and Molecular Imaging"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.2967/jnumed.119.230946","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":"http://jnm.snmjournals.org/content/61/2/242.long","subitem_relation_type_select":"URI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0161-5505","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":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"1000004","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hanyu, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"1000005","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"1000006","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"1000007","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu"}],"nameIdentifiers":[{"nameIdentifier":"1000008","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Minegishi, Katsuyuki"}],"nameIdentifiers":[{"nameIdentifier":"1000009","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Jiang, Cuiping"}],"nameIdentifiers":[{"nameIdentifier":"1000010","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kurosawa, Fuki"}],"nameIdentifiers":[{"nameIdentifier":"1000011","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Morokoshi, Yukie"}],"nameIdentifiers":[{"nameIdentifier":"1000012","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Li, Huizi"}],"nameIdentifiers":[{"nameIdentifier":"1000013","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hasegawa, Sumitaka"}],"nameIdentifiers":[{"nameIdentifier":"1000014","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nagatsu, Kotaro"}],"nameIdentifiers":[{"nameIdentifier":"1000015","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ming-Rong, Zhang"}],"nameIdentifiers":[{"nameIdentifier":"1000016","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Lin, Xie","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000017","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Hanyu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000018","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000019","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000020","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000021","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsuyuki, Minegishi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000022","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fuki, Kurosawa","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000023","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yukie, Morokoshi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000024","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Li, Huizi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000025","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sumitaka, Hasegawa","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000026","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kotaro, Nagatsu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000027","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1000028","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":"131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1 ","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1 "}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2019-12-20"},"publish_date":"2019-12-20","publish_status":"0","recid":"78127","relation_version_is_last":true,"title":["131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1 "],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T19:42:53.028267+00:00"}