Development of Active Center-Directed Inhibitors against Plasmin

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概要

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• Active center-directed inhibitors of plasmin were designed based on the structure of specific substrates of plasmin and then synthesized. Their effects on plasmin were examined and the structure-inhibitory activity relationship was studied. N^α-trans-4-Aminomethylcyclohexanecarbonyllysine 4-benzoylanilide (Tra-Lys-BZA) inhibited plasmin activities toward S-2251 and fibrin with IC_<50> values of 15 and 6.1 μM, respectively and N^α-trans-4-aminomethylcyclohexanecarbonyllysine 4-benzylpiperidine amide (Tra-Lys-BPP) did not show any detectable inhibitory activity. Moreover, it was revealed that Tra-Lys-4-methoxycarbonylanilide inhibited plasma kallikrein more potently than plasmin.

• 社団法人日本薬学会の論文
• 1991-09-25

著者

• 岡田 芳男

  Faculty of Pharmaceutical Sciences Kobe-Gakuin University

• 津田 裕子

  Faculty of Pharmaceutical Sciences

• 手納 直規

  Faculty of Pharmaceutical Sciences

• 津田 裕子

  神戸学院大学薬学部薬品化学

• 岡田 芳男

  神戸学院大学 薬学部

• 和中 敬子

  Kobe Research Projects on Thrombosis and Haemostasis

• 岡本 歌子

  Kobe Research Projects on Thrombosis and Haemostasis

• 岡本 彰祐

  Kobe Research Projects on Thrombosis and Haemostasis

• 土方-奥宮 明子

  School of Allied Medical Sciences, Kobe University

• 内藤 威敏

  Life Science Research Lab., Showa Denko Co., Ltd.,

• 手納 直規

  Faculty Of Pharmaceutical Sciences Kobe-gakuin University

• 内藤 威敏

  Kobe Research Projects On Thrombosis And Haemostasis Saiseikai Hyogo Hospital

• 土方-奥宮 明子

  School Of Allied Medical Sciences Kobe University

• 岡本 歌子

  血栓止血研究神戸プロジェクト

• 岡本 彰祐

  血栓止血研究神戸プロジェクト

関連論文

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