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

Inhibition of Human Chymase by Suramin

Kazumasa Takao1,2, Shinji Takai1, Takafumi Ishihara2, Shiro Mita2 and Mizuo Miyazaki1,*

1Department of Pharmacology, Osaka Medical College, Takatsuki, Osaka 569 - 8686, Japan
2Discovery Research Division, Santen Pharmaceutical Co., Ltd., Ikoma, Nara 630 - 0101, Japan
* To whom correspondence should be addressed.

Abstract: 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.

Keywords: Chymase, Suramin, Heparin

Copyrightę The Japanese Pharmacological Society 1999

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