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Published on: June 20, 2019
Elucidation of crucial structures for a catechol-based inhibitor of plasma hyaluronan-binding protein (factor VII
Eisaku Yamamoto1, Yoshikazu Kitano, Keiji Hasumi
1Department of Applied Biological Science, Tokyo University of Agriculture and Technology, Fuchu, Tokyo, Japan.
Abstract:
Plasma hyaluronan-binding protein (PHBP) is a serine protease the activation of which is implicated in inflammation. Previous investigations have suggested the presence of catechol-binding sites in its proenzyme form, pro-PHBP. Here we found that compounds with plural catechol groups conjugated with strong electron-withdrawing groups, such as tyrphostin AG 537 (IC(50)=18 nM), were potent inhibitors of pro-PHBP activation.
