Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
Thrombin enzyme (Factor IIa) is an important clotting factor that controls the transformation of soluble fibrinogen to insoluble active fibrin strands. Thrombin is a serine protease (EC 220.127.116.11) that catalyzes many coagulation-related reactions. Thrombin inhibitors are used as anticoagulants to prevent arterial and venous thrombosis. Some of these inhibitors are currently in clinical use while others are in clinical development. Biovision’s Thrombin Inhibitor Screening Kit utilizes the ability of Thrombin to cleave a synthetic AMC-based peptide substrate to release AMC, which can be detected by measuring its fluorescence at Ex/Em = 350/450 nm. In the presence of Thrombin specific inhibitors, the extent of cleavage reaction is reduced or completely abolished. The loss in the fluorescence intensity can be correlated to the amount of inhibitor present in the assay solution. The kit provides a simple and rapid method to screen potential inhibitors of Thrombin.