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

作者：Yamamoto Eisaku; Kitano Yoshikazu; Hasumi Keiji^*

来源：Bioscience Biotechnology and Biochemistry, 2011, 75(10): 2070-2072.

DOI：10.1271/bbb.110515

• plasma hyaluronan-binding protein
• factor VII activating protease
• autoactivation
• inhibitor
• proteolysis

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.

• 出版日期2011-10