Synthesis of Active Center-Directed Prptide Inhibitors of Plasmin

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概要

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• Active center-directed peptide inhibitors of plasmin were designed based on the structure of specific substrates of plasmin and synthesized by a conventional solution method. Their effects on plasmin were examined and the structure-activity relationship was studied. D-Ile-Phe-Lys-BZA (4-benzoylanilide) inhibited plasmin activities toward S-2251 and fibrin (IC_<50> : 0.069mM and 0.18mM respectively) but D-Ile-Phe-Lys-BPP (4-benzylpiperidine amide) was not inhibitory. However D-Ile-Phe-Lys-BZA was cleaved by plasmin to release benzoylaniline, indicating that this type of peptide inhibitor is not stable to plasmin. It was found that Tos-Lys-pNA was not cleaved by palsmin and inhibited plasmin activity toward not only fibrin but also amall peptide substrates and fibrinogen by blocking the active center of plasmin with some selectivity. In order to obtain potent and stable inhibitors of plasmin, it is recommended to design them with reference to the structures of Tos-Lys-pNA and the specific substrate, D-Ile-Phe-Lys-pNA.

• 社団法人日本薬学会の論文
• 1988-04-25

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 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

• 坊垣 美也子

  Kobe Research Projects on Thrombosis and Haemostasis, Saiseikai Hospital

• 土方-奥宮 明子

  Shcool of Alied Medical Sciences, Kobe University

• 岡本 彰祐

  血栓止血研究神戸プロジェクト

• 坊垣 美也子

  Kobe Research Projects On Thrombosis And Haemostasis Saiseikai Hospital

関連論文

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