An essential tool for the efficient screening of your furin inhibitors, as potential antiviral, or other drug candidates
High sensitivity fluorimetric detection of furin activity (0.02ng/uL of furin)
Compatible with HTS for drug discovery applications
One-step homogeneous mix-and-read format
Custom services available
Expert Assay Support (firstname.lastname@example.org or 1-800-452-5530 x1)
The SensoLyte®Rh110 human Furin Activity Assay Kit employs a fluorescent peptide substrate for the detection of human furin activity. This substrate contains the rhodamine 110 fluorophore (Rh110).
When Furin cleaves this Rh110 substrate, it results in the release of a bright green fluorescence that can be detected at excitation/emission = 496nm/520 nm. In the presence of inhibitor, Furin cannot cleave the substrate and no signal is recorded. The longer wavelength spectra and higher extinction coefficient of Rh110 provide greater sensitivity and less background interference from other reaction components.
This assay can detect as low as 0.02ng/uL of active human furin including enzyme activity detection, and it can also be applied for screening inhibitors. Furin inhibitors present as potent therapeutic candidates for chronic infections caused by HIV or HBV.
Furin, a proprotein convertase is expressed in all mammalian cell types, and processes a variety of precursor molecules into their active forms, including hormones, enzymes, growth factors, receptors, plasma proteins, bacterial toxins, viral envelope proteins, etc.
Furin has specifically been identified as an anti-viral drug target for HIV or HBV infections.
Furin is essential to the maturation and viral infectivity of HIV. It is one of the proteases responsible for the cleavage of the HIV precursor envelope protein glycoprotein 160 (gp160), into the gp120 and gp41 moieties.
The gp120 envelop moiety is responsible for virion-specific binding to the cell surface CD4, while gp41 is the transmembrane component that mediates virus-to-cell membrane fusion thereby causing viral nucleocapsid to penetrate into the cytosol.
Drugs/inhibitors that inhibit gp160 processing into gp120 and gp41 have been studied to prevent viral propagation.
1. Artenstein A and Opal S. Proprotein convertases in health and disease. NEJM 365, 2507-2518 (2011).
2. Stein B and Engelman EG. Intracellular processing of the gp160 HIV-1 envelope precursor. JBC 265(5), 2640-2649 (1990).
3. Moulard M and Decroly. Maturation of HIV envelope glycoprotein precursors by cellular endoproteases. BBA 1469, 121-132 (2000).