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

Eisaku YAMAMOTO; Yoshikazu KITANO; Keiji HASUMI

doi:10.1271/bbb.110515

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

Eisaku YAMAMOTO, Yoshikazu KITANO, Keiji HASUMI

著者情報

キーワード: plasma hyaluronan-binding protein, factor VII activating protease, autoactivation, inhibitor, proteolysis

ジャーナルフリー早期公開

論文ID: 110515

DOI https://doi.org/10.1271/bbb.110515

この記事には本公開記事があります。

The final version of this article is now available: Vol. 75 (2011) , No. 10 p.2070

詳細

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.

責任著者(Corresponding author)

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