{"created":"2023-05-15T15:02:43.240284+00:00","id":85037,"links":{},"metadata":{"_buckets":{"deposit":"f9b8dffd-42f8-444e-9d83-99c11b62a15c"},"_deposit":{"created_by":1,"id":"85037","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"85037"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00085037","sets":["1"]},"author_link":["1025489","1025481","1025485","1025491","1025483","1025488","1025493","1025484","1025494","1025495","1025492","1025486","1025482","1025487","1025490"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2022-01","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"3","bibliographicPageEnd":"1847","bibliographicPageStart":"1835","bibliographicVolumeNumber":"65","bibliographic_titles":[{"bibliographic_title":"Journal of medicinal chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor approved for treating non-small-cell lung cancer (NSCLC) with EGFR mutations. Genetic testing is required to detect the mutation for selecting patients who can use osimertinib. Here, we report an attempt to develop nuclear imaging probes that detect the EGFR mutations. We designed and synthesized I-osimertinib and Br-osimertinib with a radioactive or nonradioactive halogen atom at an indole ring in osimertinib and evaluated them.  assays suggested that both I-osimertinib and Br-osimertinib exhibit a specifically high activity toward NSCLC with EGFR L858R/T790M mutations. In biodistribution experiments, the accumulation of both [I]I-osimertinib and [Br]Br-osimertinib in tumors with mutations was significantly higher than that in blood and muscle. However, these osimertinib derivatives showed a significantly higher accumulation in lungs than in tumors. Therefore, for detecting the mutations in lung cancer, further structural modifications of the probes are required.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"American Chemical Society"}]},"item_8_relation_13":{"attribute_name":"PubMed番号","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"35015529","subitem_relation_type_select":"PMID"}}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1021/acs.jmedchem.1c01211","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":"https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01211","subitem_relation_type_select":"URI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0022-2623","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":"Mishiro, Kenji"}],"nameIdentifiers":[{"nameIdentifier":"1025481","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nishii, Ryuichi"}],"nameIdentifiers":[{"nameIdentifier":"1025482","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sawazaki, Izumi"}],"nameIdentifiers":[{"nameIdentifier":"1025483","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sofuku, Tomoki"}],"nameIdentifiers":[{"nameIdentifier":"1025484","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fuchigami, Takeshi"}],"nameIdentifiers":[{"nameIdentifier":"1025485","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sudo, Hitomi"}],"nameIdentifiers":[{"nameIdentifier":"1025486","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Effendi, Nurmaya"}],"nameIdentifiers":[{"nameIdentifier":"1025487","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Makino, Akira"}],"nameIdentifiers":[{"nameIdentifier":"1025488","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kiyono, Yasushi"}],"nameIdentifiers":[{"nameIdentifier":"1025489","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shiba, Kazuhiro"}],"nameIdentifiers":[{"nameIdentifier":"1025490","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Taki, Junichi"}],"nameIdentifiers":[{"nameIdentifier":"1025491","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kinuya, Seigo"}],"nameIdentifiers":[{"nameIdentifier":"1025492","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Kazuma"}],"nameIdentifiers":[{"nameIdentifier":"1025493","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ryuichi, Nishii","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1025494","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hitomi, Sudo","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1025495","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":"Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of Osimertinib","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of Osimertinib"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2022-01-14"},"publish_date":"2022-01-14","publish_status":"0","recid":"85037","relation_version_is_last":true,"title":["Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of Osimertinib"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T18:02:37.793283+00:00"}