Inhibition of Human Chymase by Suramin.

  • Takao Kazumasa
    Department of Pharmacology, Osaka Medical College Discovery Research Division, Santen Pharmaceutical Co., Ltd.
  • Takai Shinji
    Department of Pharmacology, Osaka Medical College
  • Ishihara Takafumi
    Discovery Research Division, Santen Pharmaceutical Co., Ltd.
  • Mita Shiro
    Discovery Research Division, Santen Pharmaceutical Co., Ltd.
  • Miyazaki Mizuo
    Department of Pharmacology, Osaka Medical College

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抄録

Chymase is a chymotrypsin-like protease localized in mast cells in complexes with heparin. In the present study, we demonstrated that suramin, a hexasulfonated naphthylurea used as an anti-cancer drug, inhibits the activity of purified human chymase in vitro. The inhibition was ionic-strength-dependent. It was observed that suramin competed with heparin-Sepharose gel for binding to chymase and the inhibition of chymase activity by suramin was partially impaired by heparin. Our results show that suramin may become a prototype of a new type of chymase inhibitor because of its unique character.

収録刊行物

  • Jpn.J.Pharmacol.

    Jpn.J.Pharmacol. 81 (4), 404-407, 1999

    公益社団法人 日本薬理学会

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