Matrix metalloproteinase-3 (MMP-3) fluorometric drug discovery kit, GREEN

The MMP-3 Fluorometric (also known as fluorimetric)Drug Discovery Kit, GREEN is a complete assay system designed to screen MMP-3 inhibitors using a quenched fluorogenic MMP-3 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-3, a potential therapeutic target. The compound NNGH is also included as a prototypic control inhibitor.

Matrix metalloproteinase-3 (MMP-3, stromelysin-1, transin-1) 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-3 include collagens, fibronectin, and laminin, plasminogen, HB-EGF, E-cadherin, and other MMPs. MMP-3 is secreted as a 55-59kDa glycosylated proenzyme (measured by SDS-PAGE), and activated by cleavage to forms of 21-48kDa. It is unique from other MMPs in that its pH optimum is 5.9, rather than around 7.0.