Elucidation of Crucial Structures for a Catechol-Based Inhibitor of Plasma Hyaluronan-Binding Protein (Factor VII Activating Protease) Autoactivation

抄録

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 (IC₅₀=18 nM), were potent inhibitors of pro-PHBP activation.