『徳島大学 教育・研究者情報データベース (EDB)』---[学外] /
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登録内容 (EID=338497)

EID=338497EID:338497, Map:0, LastModified:2018年7月2日(月) 14:15:10, Operator:[大家 隆弘], Avail:TRUE, Censor:0, Owner:[宇都 義浩], Read:継承, Write:継承, Delete:継承.
種別 (必須): 学術論文 (審査論文) [継承]
言語 (必須): 英語 [継承]
招待 (推奨):
審査 (推奨): Peer Review [継承]
カテゴリ (推奨): 研究 [継承]
共著種別 (推奨): 国内共著 (徳島大学内研究者と国内(学外)研究者との共同研究 (国外研究者を含まない)) [継承]
学究種別 (推奨):
組織 (推奨): 1.徳島大学.大学院社会産業理工学研究部.生物資源産業学域 (2017年4月1日〜) [継承]
著者 (必須): 1. (英) Ohkura Kazuto (日) (読)
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[継承]
2. (英) Tatematsu Y (日) (読)
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[継承]
3. (英) Kawaguchi Y (日) (読)
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[継承]
4.宇都 義浩 ([徳島大学.大学院社会産業理工学研究部.生物資源産業学域.応用生命系.応用生物資源学分野]/[徳島大学.生物資源産業学部.生物資源産業学科.応用生命講座])
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学籍番号 (推奨):
[継承]
5.堀 均
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学籍番号 (推奨):
[継承]
題名 (必須): (英) Interactive Analysis of TX-1123 with Cyclo-oxygenase: Design of COX2 Selective TX Analogs.  (日)    [継承]
副題 (任意):
要約 (任意): (英) To date, two cyclo-oxygenase (COX) isoforms, COX1 and COX2, have been identified. In the present study, the COX-inhibitory activities of TX-1123 derivatives with the 2-hydroxyarylidene-4-cyclopentene-1,3-dione structure were examined, and the binding profiles of TX-1123 to COXs were analyzed using docking simulations. X-Ray data on COX1 [protein data bank (PDB) ID=1PGG] and COX2 (PDB ID=3LN1) were used for molecular interactive simulations. The interactive profiles of TX-1123 derivatives with COXs were examined using a molecular simulation technique with Molegro Virtual Docker (CLC bio, Aarhus, Denmark). TX-1123 exhibited COX1-inhibitory activity [half-maximal-inhibitory concentration (IC)=1.57×10 M]. The COX2 inhibitory activity of TX-1123 was potent (IC=1.16×10 M), and the ratio of COX1/COX2 inhibition was 13.5. TX-1123 bound to the COX2 molecule, and the oxygen atom of the 4-cyclopentene-1,3-dione region of TX-1123 interacted with Cys and Gln of COX2. The TX-1123-binding pocket of COX2 differs from that of the COX2-selective celecoxib-binding pocket. TX-1123 exhibited a different COX2-interactive mechanism from that of celecoxib.  (日)    [継承]
キーワード (推奨): 1. (英) Protein kinase (日) (読) [継承]
2. (英) cyclo-oxygenase (日) (読) [継承]
3. (英) kinase inhibitor (日) (読) [継承]
発行所 (推奨):
誌名 (必須): Anticancer Research (International Institute of Anticancer Research(IIAR))
(pISSN: 0250-7005, eISSN: 1791-7530)

ISSN (任意): 1791-7530
ISSN: 0250-7005 (pISSN: 0250-7005, eISSN: 1791-7530)
Title: Anticancer research
Title(ISO): Anticancer Res.
Publisher: International Institute of Anticancer Research
 (NLM Catalog  (Scopus  (CrossRef (Scopus information is found. [need login])
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(必須): 37 [継承]
(必須): 7 [継承]
(必須): 3849 3854 [継承]
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年月日 (必須): 西暦 2017年 7月 初日 (平成 29年 7月 初日) [継承]
URL (任意):
DOI (任意): 10.21873/anticanres.11764    (→Scopusで検索) [継承]
PMID (任意): 28668885    (→Scopusで検索) [継承]
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Scopus (任意): 2-s2.0-85021744282 [継承]
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備考 (任意): 1.(英) Article.PublicationTypeList.PublicationType: Journal Article  (日)    [継承]
2.(英) KeywordList.Keyword: Protein kinase  (日)    [継承]
3.(英) KeywordList.Keyword: cyclo-oxygenase  (日)    [継承]
4.(英) KeywordList.Keyword: kinase inhibitor  (日)    [継承]

標準的な表示

和文冊子 ● Kazuto Ohkura, Y Tatematsu, Y Kawaguchi, Yoshihiro Uto and Hitoshi Hori : Interactive Analysis of TX-1123 with Cyclo-oxygenase: Design of COX2 Selective TX Analogs., Anticancer Research, Vol.37, No.7, 3849-3854, 2017.
欧文冊子 ● Kazuto Ohkura, Y Tatematsu, Y Kawaguchi, Yoshihiro Uto and Hitoshi Hori : Interactive Analysis of TX-1123 with Cyclo-oxygenase: Design of COX2 Selective TX Analogs., Anticancer Research, Vol.37, No.7, 3849-3854, 2017.

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