{"created":"2023-05-15T16:30:30.511355+00:00","id":1663,"links":{},"metadata":{"_buckets":{"deposit":"4191ffb2-8121-419c-bf03-20f931599a8a"},"_deposit":{"created_by":2,"id":"1663","owners":[2],"pid":{"revision_id":0,"type":"depid","value":"1663"},"status":"published"},"_oai":{"id":"oai:nagasaki-u.repo.nii.ac.jp:00001663","sets":["14:21"]},"author_link":["8003","8010","8005","8002","8007","8008","8011","8004","8009","8006"],"item_2_biblio_info_6":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2017-12-15","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"24","bibliographicPageEnd":"6580","bibliographicPageStart":"6563","bibliographicVolumeNumber":"25","bibliographic_titles":[{"bibliographic_title":"Bioorganic & Medicinal Chemistry"}]}]},"item_2_description_4":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"A series of A-ring-modified lamellarin N analogues were designed, synthesized, and evaluated as potential noncovalent inhibitors of the EGFR T790M/L858R mutant, a causal factor in the drug-resistant non-small cell lung cancer. Several water-soluble ammonium- or guanidinium-tethered analogues exhibited good kinase inhibitory activities. The most promising analogue, 14f, displayed an excellent inhibitory profile against the T790M/L858R mutant [IC50 (WT)?=?31.8?nM; IC50 (T790M/L858R)?=?8.9?nM]. The effects of A-ring-substituents on activity were rationalized by docking studies.","subitem_description_type":"Abstract"}]},"item_2_description_63":{"attribute_name":"引用","attribute_value_mlt":[{"subitem_description":"Bioorganic & Medicinal Chemistry, 25(24), pp.6563-6580; 2017","subitem_description_type":"Other"}]},"item_2_publisher_33":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Elsevier 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.2017.10.030","subitem_relation_type_select":"DOI"}}]},"item_2_rights_13":{"attribute_name":"権利","attribute_value_mlt":[{"subitem_rights":"c2017, Elsevier. 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":"Umeki, Teppei"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Tokushima, Keiji"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Xiang, Gao"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Yoshida, Yuki"}],"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":"2020-12-18"}],"displaytype":"detail","filename":"Supplementary_data.pdf","filesize":[{"value":"17.3 MB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"Supplementary_data.pdf","url":"https://nagasaki-u.repo.nii.ac.jp/record/1663/files/Supplementary_data.pdf"},"version_id":"1350f420-668d-40ab-a246-0479bb21e6dd"},{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2020-12-18"}],"displaytype":"detail","filename":"BMC25_6563.pdf","filesize":[{"value":"1.7 MB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"BMC25_6563.pdf","url":"https://nagasaki-u.repo.nii.ac.jp/record/1663/files/BMC25_6563.pdf"},"version_id":"05915b55-a332-4d56-994d-d0ce5d49f72d"}]},"item_keyword":{"attribute_name":"キーワード","attribute_value_mlt":[{"subitem_subject":"EGFR tyrosine kinase inhibitors (EGFR-TKI)","subitem_subject_scheme":"Other"},{"subitem_subject":"EGFR T790M/L858R mutant","subitem_subject_scheme":"Other"},{"subitem_subject":"Structure-based drug design (SBDD)","subitem_subject_scheme":"Other"},{"subitem_subject":"Lamellarin N","subitem_subject_scheme":"Other"},{"subitem_subject":"Water-soluble analogues","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":"Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant"}]},"item_type_id":"2","owner":"2","path":["21"],"pubdate":{"attribute_name":"公開日","attribute_value":"2019-12-15"},"publish_date":"2019-12-15","publish_status":"0","recid":"1663","relation_version_is_last":true,"title":["Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant"],"weko_creator_id":"2","weko_shared_id":-1},"updated":"2023-05-16T03:58:30.834342+00:00"}