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

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  • YAMAMOTO Eisaku
    Department of Applied Biological Science, Tokyo University of Agriculture and Technology
  • KITANO Yoshikazu
    Department of Applied Biological Science, Tokyo University of Agriculture and Technology
  • HASUMI Keiji
    Department of Applied Biological Science, Tokyo University of Agriculture and Technology

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  • Elucidation of crucial structures for a catechol-based inhibitor of plasma hyaluronan-binding protein (factor 7 activating protease) autoactivation

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

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