{"created":"2023-05-15T15:03:50.430887+00:00","id":86391,"links":{},"metadata":{"_buckets":{"deposit":"31e869a9-8ba9-4d58-8309-a1473efd3192"},"_deposit":{"created_by":1,"id":"86391","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"86391"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00086391","sets":["10:28"]},"author_link":["1054239","1054232","1054234","1054235","1054237","1054242","1054246","1054244","1054248","1054238","1054249","1054236","1054241","1054245","1054233","1054247","1054250","1054240","1054243"],"item_10005_date_7":{"attribute_name":"発表年月日","attribute_value_mlt":[{"subitem_date_issued_datetime":"2022-09-07","subitem_date_issued_type":"Issued"}]},"item_10005_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Background/Aims: Metabotropic glutamate receptor 1 (mGluR1), a key mediator of glutamatergic signaling, is frequently expressed as an oncoprotein and has been an attractive target to overcome most solid tumors, such as melanoma (1). Here, a novel small-molecular radiopharmaceutical pair, 3-iodo-N-[4-[6-(methylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-[11C]methylbenzamide ([11C]1) and 3-211At-astato-N-[4-[6-(methylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([211At]1), was designed and developed to target the mGluR1 for theranostics of melanomas. \nMethods: [ 11C]1 was synthesized by reacting a N-desmethyl precursor with [11C]CH3OTf in the presence of NaOH at room temperature for 5 min. Radiolabeling with [211At]1 was performed by reaction of aryl tin precursor with NCS-containing 211At/MeOH solution according to the method reported by our laboratory (2). The theranostic potentials of the radiopharmaceutical pair were explored for PET imaging and radiotherapy in mGluR1-positive B16F10 melanoma-bearing mice.\nResults: [ 11C]1 and [211At]1 were obtained with a radiochemical purity of greater than 99% and radiochemical yields of 19 ± 8 % and 46 ± 3%, respectively, based on the total radioactivity of used radionuclides. In vivo PET imaging of [ 11C]1 clearly visualized the targeted melanomas with a good tumor-to-background contrast. Ex vivo biodistribution study verified the persistent increase of [ 11C]1, which reached 12.29 ± 2.44 %ID/g tissue at 90 min in the targeted melanomas, and rapidly cleared from nontarget organs after intravenous injection. In the therapeutic studies, [211At]1 exhibited unequivocal and durable antitumor efficacy with only a single treatment (2.96 MBq) in the melanoma model, compared to the controls (0.31 ± 0.08 cm3 vs. 10.44 ± 1.61 cm3 at 16 days post-therapy). No decrease in body weight and no liver and kidney damage were observed through the examination period in melanoma mice injected with 2.96 MBq of [211At]1.\nConclusions: The novel small-molecular radiopharmaceutical pair successfully visualized the mGluR1-positive melanomas by [ 11C]1 with high contrast PET images, and further treated the melanoma by [211At]1 without significant toxicity. The results highlight the good potential of using [ 11C]1 and [211At]1 as theranostic agents for the management of mGluR1-positive tumors and should be further investigated in the theranostic field of oncology in the clinic.\n","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":"第13回世界核医学会（13th orld Federation of Nuclear Medicine and Biology)","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":"Lin, Xie"}],"nameIdentifiers":[{"nameIdentifier":"1054232","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Hanyu"}],"nameIdentifiers":[{"nameIdentifier":"1054233","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga"}],"nameIdentifiers":[{"nameIdentifier":"1054234","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Lulu"}],"nameIdentifiers":[{"nameIdentifier":"1054235","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"1054236","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakana, Mori"}],"nameIdentifiers":[{"nameIdentifier":"1054237","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu"}],"nameIdentifiers":[{"nameIdentifier":"1054238","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsuyuki, Minegishi"}],"nameIdentifiers":[{"nameIdentifier":"1054239","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kotaro, Nagatsu"}],"nameIdentifiers":[{"nameIdentifier":"1054240","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"1054241","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Lin, Xie","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054242","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Hanyu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054243","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054244","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054245","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakana, Mori","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054246","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054247","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsuyuki, Minegishi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054248","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kotaro, Nagatsu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054249","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054250","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 metabotropic glutamate receptor 1-targeted radiopharmaceuticals for theranostics of melanoma","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Development of metabotropic glutamate receptor 1-targeted radiopharmaceuticals for theranostics of melanoma"}]},"item_type_id":"10005","owner":"1","path":["28"],"pubdate":{"attribute_name":"公開日","attribute_value":"2022-06-27"},"publish_date":"2022-06-27","publish_status":"0","recid":"86391","relation_version_is_last":true,"title":["Development of metabotropic glutamate receptor 1-targeted radiopharmaceuticals for theranostics of melanoma"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T16:59:59.224868+00:00"}