Furin is a proprotein convertase, converting precursor proteins to functional proteins within the Golgi/trans-Golgi secretory pathway.
Naphthofluorescein is a cell-permeable inhibitor of furin (IC50 = 12 μM).1 It inhibits furin-mediated cleavage of the pro-form of membrane type-1 matrix metalloproteinase MT1-MMP, resulting in decreased levels of active MT1-MMP.1 This, in turn, suppresses MMP-2 activation and reduces cell motility in CHO cells expressing proMT1-MMP.1 Napthofluorescein significantly inhibits the invasion of Matrigel by the human fibrosarcoma cell line, HT1080.1 The effects of this furin inhibitor on other furin-mediated processes, in vivo or in vitro, remain to be determined
1
Coppola, J.M., Bhojani, M.S., Ross, B.D., et al. A small-molecule furin inhibitor inhibits cancer cell motility and invasiveness. Neoplasia10(4)363-370(2008).
Coppola, J.M., Bhojani, M.S., Ross, B.D., et al. A small-molecule furin inhibitor inhibits cancer cell motility and invasiveness. Neoplasia10(4)363-370(2008).
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