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Furin is a proprotein convertase, converting precursor proteins to functional proteins within the Golgi/trans-Golgi secretory pathway. Furin inhibitor I is a selective, irreversible, and cell-permeable competitive inhibitor of proprotein convertases, including furin/SPC1 (Ki = ~1 nM), SPC2/PC2 (Ki = 0.36 nM), SPC3/PC1/PC3 (Ki = 2.0 nM), SPC4/PACE4 (Ki = 3.6 nM), SPC6/PC5/PC6, and SPC7/LPC/PC7/PC8 (Ki = 0.12 nM).[1],[2] Because furin activates viral glycoproteins, this inhibitor is a useful antiviral agent.[3] In addition, it inhibits furin-dependent pro-MMP-2 activation in mononuclear inflammatory cells.[4]

Reference:

[1]. Angliker, H., Wikstrom, P., Shaw, E., et al. The synthesis of inhibitors for processing proteinases and their action on the Kex2 proteinase of yeast. Biochemistry Journal 293(1), 75-81 (1993).

[2]. Fugère, M., Limperis, P.C., Beaulieu-Audy, V., et al. Inhibitory potency and specificity of subtilase-like Pro-protein convertase (SPC) prodomains. The Journal of Biological Chemisty 277(10), 7648-7656 (2002).

[3]. Wanyiri, J.W., O'Connor, R., Allison, G., et al. Proteolytic processing of the Cryptosporidium glycoprotein gp40/15 by human furin and by a parasite-derived furin-like protease activity. Infection and Immunity 75(1), 184-192 (2007).

[4]. Stawowy, P., Meyborg, H., Stibenz, D., et al. Furin-like proprotein convertases are central regulators of the membrane type matrix metalloproteinase-pro-matrix metalloproteinase-2 proteolytic cascade in atherosclerosis. Circulation 111(21), 2820-2827 (2005).

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