2. Academic Validation
  3. Elucidation of crucial structures for a catechol-based inhibitor of plasma hyaluronan-binding protein (factor VII activating protease) autoactivation

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

  • Biosci Biotechnol Biochem. 2011;75(10):2070-2. doi: 10.1271/bbb.110515.
Eisaku Yamamoto 1,  Yoshikazu Kitano,  Keiji Hasumi
Affiliations

Affiliation

  • 1 Department of Applied Biological Science, Tokyo University of Agriculture and Technology, Fuchu, Tokyo, Japan.
PMID: 21979097 DOI: 10.1271/bbb.110515
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.

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