Plasminogen activator inhibitor 1 is an intracellular inhibitor of furin proprotein convertase.

Furin has the proalbumin substrate specificity and serpin inhibitory properties of an in situ hepatic convertase.

Furin, a KEX2 protease homolog with high RNA expression in the liver is an excellent candidate as a hepatic proprotein convertase. Here we show that purified recombinant furin has the same proalbumin specificity and serpin inhibitory properties as the in situ hepatic convertase. There was rapid cleavage at the -RRD- site of normal human proalbumin but there no significant cleavage of natural un...

Regulation of membrane type-1 matrix metalloproteinase activation by proprotein convertases.

Membrane type-1 matrix metalloproteinase (MT1-MMP) is the prototypical member of a subgroup of membrane-anchored proteinases that belong to the matrix metalloproteinase family. Although synthesized as a zymogen, MT1-MMP plays an essential role in extracellular matrix remodeling after an undefined process that unmasks its catalytic domain. We now report the existence of a proprotein convertase-M...

A Novel Enediynyl Peptide Inhibitor of Furin That Blocks Processing of proPDGF-A, B and proVEGF-C

BACKGROUND Furin represents a crucial member of secretory mammalian subtilase, the Proprotein Convertase (PC) or Proprotein Convertase Subtilisin/Kexin (PCSK) superfamily. It has been linked to cancer, tumorgenesis, viral and bacterial pathogenesis. As a result it is considered a major target for intervention of these diseases. METHODOLOGY/PRINCIPAL FINDINGS Herein, we report, for the first t...

TACE/ADAM-17 maturation and activation of sheddase activity require proprotein convertase activity.

Proprotein convertases (PCs) have been proposed to play a role in tumor necrosis factor-alpha converting enzyme (TACE) processing/activation. Using the furin-deficient LoVo cells, as well as the furin-proficient synoviocytes and HT1080 cells expressing the furin inhibitor alpha(1)-PDX, we demonstrate that furin activity alone is not sufficient for effective maturation and activation of the TACE...

Methyltetrahydrofolate Reductase C677T Mutation and 4G/5G Plasminogen Activator Inhibitor-1 Polymorphism in a Child with Deep Vein Thrombosis