Elastases

Elastase inhibitors block serine proteases that degrade elastin and other extracellular matrix proteins. Neutrophil elastase, the main target here, is stored in azurophil granules of neutrophils together with proteinase 3 and cathepsin G. After release it cleaves elastin and collagens, and it processes cytokines and cell surface receptors at sites of inflammation. During the formation of neutrophil extracellular traps (NETs), the enzyme moves to the nucleus and helps to decondense chromatin. Inhibitors are used in models of acute lung injury, cystic fibrosis and chronic obstructive pulmonary disease (COPD). Sivelestat, BAY-678 and DMP 777 are inhibitors of human neutrophil elastase. Related enzymes of the same class are listed under Serine Protease.