{"created":"2023-05-15T15:03:52.187868+00:00","id":86417,"links":{},"metadata":{"_buckets":{"deposit":"f5b6c924-1901-42fc-8834-dc82e6fb9df4"},"_deposit":{"created_by":1,"id":"86417","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"86417"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00086417","sets":["10:29"]},"author_link":["1054637","1054656","1054646","1054648","1054650","1054657","1054651","1054641","1054654","1054642","1054647","1054649","1054645","1054655","1054639","1054640","1054653","1054644","1054643","1054652","1054638"],"item_10005_date_7":{"attribute_name":"発表年月日","attribute_value_mlt":[{"subitem_date_issued_datetime":"2022-06-14","subitem_date_issued_type":"Issued"}]},"item_10005_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Objectives: Metabotropic glutamate receptor 1 (GRM1) is aberrantly overexpressed in a wide variety of human solid tumors, such as melanoma，but not in normal peripheral organs (1). Therefore, GRM1 can be a widely–applicable target for the theranostics in oncology. 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 GRM1 for the theranostics in melanomas (Fig.1).  \n\nMethod: [ 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 of [211At]1 was performed by reaction of aryl tin precursor with NCS-containing 211At/MeOH solution. The theranostic potentials of the radiopharmaceutical pair were explored for PET imaging and radiotherapy in GRM1-positive B16F10 melanoma-bearing mice.  \n\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 (Fig. 1A). 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 (0.38 ± 0.02 cm3 vs. 7.88 ± 1.28 cm3 at 13 days post-therapy) (Fig. 1B). 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. \n\nConclusion: The novel small-molecular radiopharmaceutical pair successfully visualized the GRM1-positive melanomas by [ 11C]1 with high contrast PET images, and further treated 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 GRM1-positive tumors and should be further investigated in the theranostic field of oncology in the clinic. ","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":"SNMMI2022","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":"1054637","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Hanyu"}],"nameIdentifiers":[{"nameIdentifier":"1054638","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga"}],"nameIdentifiers":[{"nameIdentifier":"1054639","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Lulu"}],"nameIdentifiers":[{"nameIdentifier":"1054640","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"1054641","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakana, Mori"}],"nameIdentifiers":[{"nameIdentifier":"1054642","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu"}],"nameIdentifiers":[{"nameIdentifier":"1054643","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsuyuki, Minegishi"}],"nameIdentifiers":[{"nameIdentifier":"1054644","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kotaro, Nagatsu"}],"nameIdentifiers":[{"nameIdentifier":"1054645","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kazunori, Kawamura"}],"nameIdentifiers":[{"nameIdentifier":"1054646","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"1054647","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Lin, Xie","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054648","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Hanyu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054649","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054650","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054651","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakana, Mori","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054652","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054653","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsuyuki, Minegishi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054654","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kotaro, Nagatsu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054655","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kazunori, Kawamura","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054656","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1054657","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":"Theranostics of melanoma targeting metabotropic glutamate receptor 1 with a novel small-molecular radiopharmaceutical pair ","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Theranostics of melanoma targeting metabotropic glutamate receptor 1 with a novel small-molecular radiopharmaceutical pair "}]},"item_type_id":"10005","owner":"1","path":["29"],"pubdate":{"attribute_name":"公開日","attribute_value":"2022-05-02"},"publish_date":"2022-05-02","publish_status":"0","recid":"86417","relation_version_is_last":true,"title":["Theranostics of melanoma targeting metabotropic glutamate receptor 1 with a novel small-molecular radiopharmaceutical pair "],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T16:59:22.333721+00:00"}