{"created":"2023-05-15T14:57:14.691977+00:00","id":77681,"links":{},"metadata":{"_buckets":{"deposit":"7036ef4c-56fa-4570-9bf7-5dc7db89b9ac"},"_deposit":{"created_by":1,"id":"77681","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"77681"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00077681","sets":["1"]},"author_link":["1002063","1002059","1002058","1002060","1002062","1002065","1002061","1002064","1002057","1002066"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2019-03","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"3","bibliographicPageStart":"e0213397","bibliographicVolumeNumber":"14","bibliographic_titles":[{"bibliographic_title":"PLOS ONE"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Background\nAlthough a 3-arm DOTA construct, which has three carboxylic acids, h has been applied for conjugation to many peptides, we investigated if a 4-arm DOTA construct conjugated to peptides improves chemical properties for melanoma imaging of the melanocortin 1 receptor compared to 3-arm DOTA-conjugated peptides.\n\nMethods\nSpecific activities, radiolabeling efficiencies, and partition coefficients were evaluated using 111In-labeled 3-arm and 4-arm DOTA-α-melanocyte-stimulating hormone (MSH). For assessment of MC1-R affinity and accumulation in tumor cells in vitro, B16-F1 melanoma and/or 4T1 breast cancer cells were incubated with 111In-labeled 3-arm and 4-arm DOTA-α-MSH with and without α-MSH as a substrate. The stability was evaluated using mouse liver homogenates and plasma. Biological distribution and whole-body single photon emission computed tomography imaging of 111In-labeled 3-arm and 4-arm DOTA-α-MSH were obtained using B16-F1 melanoma-bearing mice.\n\nResults\nSpecific activities and radiolabeling efficiencies of both radiotracers were about 1.2 MBq/nM and 90–95%, respectively. The partition coefficients were −0.28 ± 0.03 for 111In-labeled 3-arm DOTA-α-MSH and −0.13 ± 0.04 for 111In-labeled 4-arm DOTA-α-MSH. Although accumulation was significantly inhibited by α-MSH in B16-F1 cells, the inhibition rate of 111In-labeled 4-arm DOTA-α-MSH was lower than that of 111In-labeled 3-arm DOTA-α-MSH. 111In-labeled 4-arm DOTA-α-MSH was taken up early into B16-F1 cells and showed higher accumulation than 111In-labeled 3-arm DOTA-α-MSH after 10 min of incubation. Although these stabilities were relatively high, the stability of 111In-labeled 4-arm DOTA-α-MSH was higher than that of 111In-labeled 3-arm DOTA-α-MSH. Regarding biological distribution, 111In-labeled 4-arm DOTA-α-MSH showed significantly lower average renal accumulation (1.38-fold) and significantly higher average melanoma accumulation (1.32-fold) than 111In-labeled 3-arm DOTA-α-MSH at all acquisition times. 111In-labeled 4-arm DOTA-α-MSH showed significantly higher melanoma-to-kidney, melanoma-to-blood, and melanoma-to-muscle ratios than 111In-labeled 3-arm DOTA-α-MSH.\n\nConclusions\nThe 4-arm DOTA construct has better chemical properties for peptide radiotracers than the 3-arm DOTA construct.","subitem_description_type":"Abstract"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1371/journal.pone.0213397","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://journals.plos.org/plosone/article?id=10.1371/journal.pone.0213397","subitem_relation_type_select":"URI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"1932-6203","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":"Kobayashi, Masato"}],"nameIdentifiers":[{"nameIdentifier":"1002057","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kato, Toshitaka"}],"nameIdentifiers":[{"nameIdentifier":"1002058","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Washiyama, Kohshin"}],"nameIdentifiers":[{"nameIdentifier":"1002059","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ihara, Masaaki"}],"nameIdentifiers":[{"nameIdentifier":"1002060","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mizutani, Asuka"}],"nameIdentifiers":[{"nameIdentifier":"1002061","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nishi, Kodai"}],"nameIdentifiers":[{"nameIdentifier":"1002062","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"G. Flores, 2nd, Leo"}],"nameIdentifiers":[{"nameIdentifier":"1002063","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nishii, Ryuichi"}],"nameIdentifiers":[{"nameIdentifier":"1002064","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kawai, Keiichi"}],"nameIdentifiers":[{"nameIdentifier":"1002065","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ryuichi, Nishii","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1002066","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":"The pharmacological properties of 3-arm or 4-arm DOTA constructs for conjugation to α-melanocyte-stimulating hormone analogues for melanoma imaging","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"The pharmacological properties of 3-arm or 4-arm DOTA constructs for conjugation to α-melanocyte-stimulating hormone analogues for melanoma imaging"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2019-11-28"},"publish_date":"2019-11-28","publish_status":"0","recid":"77681","relation_version_is_last":true,"title":["The pharmacological properties of 3-arm or 4-arm DOTA constructs for conjugation to α-melanocyte-stimulating hormone analogues for melanoma imaging"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T19:35:33.726140+00:00"}