{"created":"2023-05-15T14:38:09.540532+00:00","id":49236,"links":{},"metadata":{"_buckets":{"deposit":"e0d0f137-c992-4658-9a53-d0e5d2638be7"},"_deposit":{"created_by":1,"id":"49236","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"49236"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00049236","sets":["1"]},"author_link":["734458","734456","734462","734454","734463","734459","734455","734453","734457","734461","734464","734460","734465"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2018-11","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"12","bibliographicPageEnd":"5153","bibliographicPageStart":"5138","bibliographicVolumeNumber":"61","bibliographic_titles":[{"bibliographic_title":"Journal of Medicinal Chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"The emergence of drug-resistant HIV from a wide spreading anti-viral chemotherapy targeting the HIV protease in the past decades is unavoidable and provides a challenge to develop alternative inhibitors. We synthesized a series of allophenylnorstatine-based peptidomimetics with various P3, P2 and P2´ moieties. The derivatives with P2 tetrahydrofuranylglycine (Thfg) were found to be potent against wild type HIV-1 protease and the virus, identifying a highly potent compound 21f (KNI-1657) against lopinavir/ritonavir- or darunavir-resistant strains. Co-crystal structures of 21f and the wild-type protease revealed numerous key hydrogen bonding interactions with the Thfg. These results suggest that the strategy to design allophenylnorstatine-based peptidomimetics combined with Thfg residue would be promising for generating candidates to overcome multi-drug resistance.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"ELSEVIER"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1021/acs.jmedchem.7b01709","subitem_relation_type_select":"DOI"}}]},"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":"Hidaka, Koushi"}],"nameIdentifiers":[{"nameIdentifier":"734453","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kimura, Tooru"}],"nameIdentifiers":[{"nameIdentifier":"734454","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sankaranarayanan, Rajesh"}],"nameIdentifiers":[{"nameIdentifier":"734455","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wang, Jun"}],"nameIdentifiers":[{"nameIdentifier":"734456","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"F. McDaniel, Keith"}],"nameIdentifiers":[{"nameIdentifier":"734457","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"J. Kempf, Dale"}],"nameIdentifiers":[{"nameIdentifier":"734458","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kameoka, Masanori"}],"nameIdentifiers":[{"nameIdentifier":"734459","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Adachi, Motoyasu"}],"nameIdentifiers":[{"nameIdentifier":"734460","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuroki, Ryota"}],"nameIdentifiers":[{"nameIdentifier":"734461","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Jeffrey-Tri, Nguyen"}],"nameIdentifiers":[{"nameIdentifier":"734462","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hayashi, Yoshio"}],"nameIdentifiers":[{"nameIdentifier":"734463","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kiso, Yoshiaki"}],"nameIdentifiers":[{"nameIdentifier":"734464","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Adachi, Motoyasu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"734465","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":"Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2018-10-29"},"publish_date":"2018-10-29","publish_status":"0","recid":"49236","relation_version_is_last":true,"title":["Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-16T07:55:30.926392+00:00"}