{"created":"2021-03-01T06:34:18.374144+00:00","id":26381,"links":{},"metadata":{"_buckets":{"deposit":"6610bb3c-c36b-4158-95cd-938063848f1f"},"_deposit":{"id":"26381","owners":[],"pid":{"revision_id":0,"type":"depid","value":"26381"},"status":"published"},"_oai":{"id":"oai:nagoya.repo.nii.ac.jp:00026381","sets":["643:666:667"]},"author_link":["85382","85383","85384","85385","85386","85387","85388","85389","85390","85391","85392","85393"],"item_10_biblio_info_6":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2017-05","bibliographicIssueDateType":"Issued"},"bibliographicPageEnd":"7","bibliographicPageStart":"1","bibliographicVolumeNumber":"138","bibliographic_titles":[{"bibliographic_title":"Pesticide Biochemistry and Physiology","bibliographic_titleLang":"en"}]}]},"item_10_description_4":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Trichothecene mycotoxins often accumulate in apparently normal grains of cereal crops. In an effort to develop an agricultural chemical to reduce trichothecene contamination, we screened trichothecene production inhibitors from the compounds on the chemical arrays. By using the trichodiene (TDN) synthase tagged with hexahistidine (rTRI5) as a target protein, 32 hit compounds were obtained from chemical library of the RIKEN Natural Product Depository (NPDepo) by chemical array screening. At 10 μg mL^− 1, none of the 32 chemicals inhibited trichothecene production by Fusarium graminearum in liquid culture. Against the purified rTRI5 enzyme, however, NPD10133 [progesterone 3-(O-carboxymethyl)oxime amide-bonded to phenylalanine] showed weak inhibitory activity at 10 μg mL^− 1 (18.7 μM). For the screening of chemicals inhibiting trichothecene accumulation in liquid culture, 20 analogs of NPD10133 selected from the NPDepo chemical library were assayed. At 10 μM, only NPD352 [testosterone 3-(O-carboxymethyl)oxime amide-bonded to phenylalanine methyl ester] inhibited rTRI5 activity and trichothecene production. Kinetic analysis suggested that the enzyme inhibition was of a mixed-type. The identification of NPD352 as a TDN synthase inhibitor lays the foundation for the development of a more potent inhibitor via systematic introduction of wide structural diversity on the gonane skeleton and amino acid residues.","subitem_description_language":"en","subitem_description_type":"Abstract"}]},"item_10_publisher_32":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Elsevier","subitem_publisher_language":"en"}]},"item_10_relation_11":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type":"isVersionOf","subitem_relation_type_id":{"subitem_relation_type_id_text":"https://doi.org/10.1016/j.pestbp.2017.03.006","subitem_relation_type_select":"DOI"}}]},"item_10_rights_12":{"attribute_name":"権利","attribute_value_mlt":[{"subitem_rights":"© 2017. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/","subitem_rights_language":"en"}]},"item_10_select_15":{"attribute_name":"著者版フラグ","attribute_value_mlt":[{"subitem_select_item":"author"}]},"item_10_source_id_61":{"attribute_name":"ISSN（print）","attribute_value_mlt":[{"subitem_source_identifier":"0048-3575","subitem_source_identifier_type":"PISSN"}]},"item_1615787544753":{"attribute_name":"出版タイプ","attribute_value_mlt":[{"subitem_version_resource":"http://purl.org/coar/version/c_ab4af688f83e57aa","subitem_version_type":"AM"}]},"item_access_right":{"attribute_name":"アクセス権","attribute_value_mlt":[{"subitem_access_right":"open access","subitem_access_right_uri":"http://purl.org/coar/access_right/c_abf2"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"Maeda, Kazuyuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85382","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nakajima, Yuichi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85383","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Motoyama, Takayuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85384","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kondoh, Yasumitsu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85385","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kawamura, Tatsuro","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85386","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kanamaru, Kyoko","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85387","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ohsato, Shuichi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85388","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nishiuchi, Takumi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85389","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yoshida, Minoru","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85390","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Osada, Hiroyuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85391","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kobayashi, Tetsuo","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85392","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kimura, Makoto","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"85393","nameIdentifierScheme":"WEKO"}]}]},"item_files":{"attribute_name":"ファイル情報","attribute_type":"file","attribute_value_mlt":[{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2018-09-27"}],"displaytype":"detail","filename":"Identification_of_a_trichothecene_production_inhibitor.pdf","filesize":[{"value":"1.6 MB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"Identification_of_a_trichothecene_production_inhibitor","objectType":"fulltext","url":"https://nagoya.repo.nii.ac.jp/record/26381/files/Identification_of_a_trichothecene_production_inhibitor.pdf"},"version_id":"ebd92455-3660-427b-9a4a-a427e1cf44b9"}]},"item_keyword":{"attribute_name":"キーワード","attribute_value_mlt":[{"subitem_subject":"Chemical array","subitem_subject_scheme":"Other"},{"subitem_subject":"Fusarium graminearum","subitem_subject_scheme":"Other"},{"subitem_subject":"Gonane skeleton","subitem_subject_scheme":"Other"},{"subitem_subject":"Mixed-type inhibition","subitem_subject_scheme":"Other"},{"subitem_subject":"Trichodiene synthase","subitem_subject_scheme":"Other"},{"subitem_subject":"Trichothecene production inhibitor","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":"Identification of a trichothecene production inhibitor by chemical array and library screening using trichodiene synthase as a target protein","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Identification of a trichothecene production inhibitor by chemical array and library screening using trichodiene synthase as a target protein","subitem_title_language":"en"}]},"item_type_id":"10","owner":"1","path":["667"],"pubdate":{"attribute_name":"PubDate","attribute_value":"2018-09-27"},"publish_date":"2018-09-27","publish_status":"0","recid":"26381","relation_version_is_last":true,"title":["Identification of a trichothecene production inhibitor by chemical array and library screening using trichodiene synthase as a target protein"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-01-16T04:16:56.186929+00:00"}