DPPIV drug discovery kit

• Measures DPPIV activity in plasma, serum, urine, and saliva
• Allows correlation of DPPIV activity levels with disease states or drug treatments
• Allows determination of efficacy of DPPIV inhibitors

The DPPIV Drug Discovery Kit is a complete assay system designed to screen DPPIV inhibitors, providing enough material to perform at least 96 assays. DPPIV (DPP4, CD26) is a member of the class of proteases known as prolyl peptidases, which cleave proteins after proline residues and is thought to play roles in diabetes, cancer, and autoimmune diseases, making it a target for drug discovery.

The kit contains both a chromogenic substrate (H-Gly-Pro-pNA; K_m=114 µM) and a fluorogenic substrate (H-Gly-Pro-AMC; K_m=50 µM).

Cleavage of the p-nitroaniline (pNA) from the colorimetric substrate increases absorbance at 405 nm. The fluorimetric assay is based on the cleavage of 7-amino-4-methylcoumarin (AMC) moiety from the C-terminus of the peptide substrate, which increases its fluorescence intensity at 460 nm. The kit is useful to screen inhibitors of DPPIV, a potential therapeutic target. A DPPIV inhibitor, P32/98 (K_I=130 nM12), is included for use as a control. Other DPP enzymes are available for specificity profiling.