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Inhibition of furin by serpin Spn4A from Drosophila melanogaster.

FEBS letters (2004-11-06)
Mareke Oley, Matthias C Letzel, Hermann Ragg
ABSTRACT

The serpin gene Spn4 from Drosophila melanogaster encodes multiple isoforms with alternative reactive site loops (RSL). Here, we show that isoform Spn4A inhibits human furin with an apparent kassoc of 5.5 x 10(6) M(-1) s(-1). The serpin forms SDS-stable complexes with the enzyme and the RSL of Spn4A is cleaved C-terminally to the sequence -Arg-Arg-Lys-Arg/ in accord with the recognition/cleavage site of furin. Immunofluorescence studies show that Spn4A is localized in the endoplasmic reticulum (ER), suggesting that the inhibitor is an interesting tool for investigating the cellular mechanisms regulating furin and for the design of agents controlling prohormone convertases.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Protease Inhibitor Cocktail, for use in purification of Histidine-tagged proteins, DMSO solution
Sigma-Aldrich
Anti-Rabbit IgG (whole molecule), F(ab′)2 fragment–FITC antibody produced in goat, affinity isolated antibody, buffered aqueous solution