Matrix metalloproteinase-2 (MMP-2) fluorometric drug discovery kit, RED

The MMP-2 Fluorometric (also known as fluorimetric) Drug Discovery Kit, RED is a complete assay system designed to screen MMP-2 inhibitors using a quenched fluorogenic substrate OMNIMMP^® RED: TQ3-GABA-Pro-Cha-Abu-Smc-His-Ala-Dab(6-TAMRA)-Ala-Lys-NH₂ [TQ3=quencher; GABA=4-aminobutyric acid; Cha=L-cyclohexylalanine; Abu=2-aminobutyric acid; Smc=S-methyl-L-cysteine; Dab=2,4-diaminobutyric acid; 6-TAMRA=6-tetramethylrhodamine]. TAMRA fluorescence is thoroughly quenched by the TQ3 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-2, a potential therapeutic target. The compound NNGH is also included as a prototypic control inhibitor.

Matrix metalloproteinase-2 (MMP-2, gelatinase A, 72kDa type IV collagenase) 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-2 include native and denatured collagens, fibronectin, elastin, laminin-5, pro-TNF-α, and neurocan. MMP-2 is secreted as a 72kDa proenzyme (as measured by SDS-PAGE), and activated by cleavage to 62 and 59kDa. MMP-2 is an important target for inhibitor screening due to its involvement in diseases such as atherosclerosis, and cancer growth, angiogenesis, and metastasis.