Matrix metalloproteinase-12 (MMP-12) fluorometric drug discovery kit, GREEN

The MMP-12 Fluorometric (also known as fluorimetric) Drug Discovery Kit, GREEN is a complete assay system designed to screen MMP-12 inhibitors using a quenched fluorogenic OMNIMMP^® Green  substrate: 5-FAM-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(TQ2W)-NH₂ [5-FAM = 5-carboxyfluorescein; Nva=norvaline; TQ2W=quencher]. FAM fluorescence is thoroughly quenched by the TQ2W group until cleavage by MMPs separates the two moieties.

The assays are performed in a convenient 96-well microplate format. The kit is useful to screen inhibitors of MMP-12, a potential therapeutic target. The compound NNGH is also included as a prototypic control inhibitor.

Matrix metalloproteinase-12 (MMP-12, metalloelastase, macrophage elastase, commonly confused with neutrophil elastase) is a member of the MMP family of extracellular proteases. These enzymes play a role in many normal and disease states by virtue of their broad substrate specificities. Targets of MMP-12 include elastin, fibronectin, laminin, plasminogen, u-PAR, and tissue factor pathway inhibitor. MMP-12 is secreted as a 53kDa proenzyme (as measured by SDS-PAGE), and activated by cleavage to forms of 45-22kDa.  MMP-12 is an important target for inhibitor screening due to its involvement in diseases such as cancer, allergy and emphysema.