{"created":"2023-05-15T16:49:03.531569+00:00","id":26337,"links":{},"metadata":{"_buckets":{"deposit":"2fbbcd31-d7aa-40ea-8d1e-8756266e806c"},"_deposit":{"created_by":6,"id":"26337","owners":[6],"pid":{"revision_id":0,"type":"depid","value":"26337"},"status":"published"},"_oai":{"id":"oai:nagasaki-u.repo.nii.ac.jp:00026337","sets":["1980:1981"]},"author_link":["117291","117290","117295","117296","117294","117292","117289","117288","117293","117287"],"item_2_biblio_info_6":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2021-01-23","bibliographicIssueDateType":"Issued"},"bibliographicPageStart":"116039","bibliographicVolumeNumber":"34","bibliographic_titles":[{"bibliographic_title":"Bioorganic & Medicinal Chemistry"}]}]},"item_2_description_4":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Azalamellarin N, a synthetic lactam congener of the marine natural product lamellarin N, and its A-ring-modified analogues were synthesized and evaluated as potent and non-covalent inhibitors of the drug-resistant epidermal growth factor receptor T790M/L858R mutant. An in vitro tyrosine kinase assay indicated that the inhibitory activities of the synthetic azalamellarin analogues were higher than those of the corresponding lamellarins.The azalamellarin analogue bearing two 3-(dimethylamino)propoxy groups at C20- and C21-positions exhibited the highest activity and selectivity against the mutant kinase [IC50 (T790M/L858R) = 1.7 nM; IC50 (WT) = 4.6 nM]. The inhibitory activity was attributed to the hydrogen bonding interaction between the lactam NH group of the B-ring and carbonyl group of a methionine residue.","subitem_description_type":"Abstract"}]},"item_2_description_63":{"attribute_name":"引用","attribute_value_mlt":[{"subitem_description":"Bioorganic and Medicinal Chemistry, 34, art.no.116039; 2021","subitem_description_type":"Other"}]},"item_2_publisher_33":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Elevier Ltd"}]},"item_2_relation_12":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type":"isVersionOf","subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1016/j.bmc.2021.116039","subitem_relation_type_select":"DOI"}}]},"item_2_rights_13":{"attribute_name":"権利","attribute_value_mlt":[{"subitem_rights":"© 2021 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/"}]},"item_2_source_id_7":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"09680896","subitem_source_identifier_type":"ISSN"}]},"item_2_version_type_16":{"attribute_name":"著者版フラグ","attribute_value_mlt":[{"subitem_version_resource":"http://purl.org/coar/version/c_ab4af688f83e57aa","subitem_version_type":"AM"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"Fukuda, Tsutomu"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Anzai, Mizuho"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Nakahara, Akane"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Yamashita, Kentaro"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Matsukura, Kazuaki"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Ishibashi, Fumito"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Oku, Yusuke"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Nishiya, Naoyuki"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Uehara, Yoshimasa"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Iwao, Masatomo"}],"nameIdentifiers":[{}]}]},"item_files":{"attribute_name":"ファイル情報","attribute_type":"file","attribute_value_mlt":[{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2023-01-23"}],"displaytype":"detail","filename":"BMChem34_116039.pdf","filesize":[{"value":"7.0 MB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"BMChem34_116039.pdf ","url":"https://nagasaki-u.repo.nii.ac.jp/record/26337/files/BMChem34_116039.pdf"},"version_id":"2df5b7b0-65d6-431d-a758-f2e354700fb8"},{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2023-01-23"}],"displaytype":"detail","filename":"supplementary data.pdf","filesize":[{"value":"6.7 MB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"supplementary data.pdf","url":"https://nagasaki-u.repo.nii.ac.jp/record/26337/files/supplementary data.pdf"},"version_id":"a4514eac-e770-4e1e-a8cc-1663e5d29df7"}]},"item_keyword":{"attribute_name":"キーワード","attribute_value_mlt":[{"subitem_subject":"A-ring-modified azalamellarin analogues","subitem_subject_scheme":"Other"},{"subitem_subject":"Azalamellarin N","subitem_subject_scheme":"Other"},{"subitem_subject":"EGFR T790M/L858R mutant","subitem_subject_scheme":"Other"},{"subitem_subject":"EGFR tyrosine kinase inhibitors (EGFR-TKIs)","subitem_subject_scheme":"Other"}]},"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":"Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant"}]},"item_type_id":"2","owner":"6","path":["1981"],"pubdate":{"attribute_name":"公開日","attribute_value":"2021-01-23"},"publish_date":"2021-01-23","publish_status":"0","recid":"26337","relation_version_is_last":true,"title":["Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant"],"weko_creator_id":"6","weko_shared_id":-1},"updated":"2023-05-15T20:28:18.128666+00:00"}