elastase
Elastase is an enzyme from the class of proteases (peptidases) that break down proteins.Elastase breaks down elastin, an elastic fibre that, together with collagen, determines the mechanical properties of connective tissue. The neutrophil form breaks down the Outer membrane protein A (OmpA) of E. coli and other Gram-negative bacteria. Elastase also has the important immunological role of breaking down Shigella virulence factors. This is accomplished through the cleavage of peptide bonds in the target proteins. The specific peptide bonds cleaved are those on the carboxyl side of small, hydrophobic amino acids such as glycine, alanine, and valine. Elastase has been shown to disrupt tight junctions, cause proteolytic damage to tissue, break down cytokines and alpha proteinase inhibitor, cleave immunoglobulin A and G (IgA, IgG), and cleave both C3bi, a component of the complement system, and CR1, a receptor on neutrophils for another complement molecule involved in phagocytosis. The cleavage of IgA, IgG, C3bi, and CR1 contributes to a decrease of the ability of neutrophils to kill bacteria by phagocytosis.
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Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases.
Phase 2.
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Sivelestat sodium salt是选择性 leukocyte elastase 抑制剂。
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ONO 6818是高亲和性，选择性 人 neutraphil elastase 1 (HNE1) 抑制剂， 口服 active。
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Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases.
Phase 2.
More
-
Sivelestat sodium salt是选择性 leukocyte elastase 抑制剂。
More
-
ONO 6818是高亲和性，选择性 人 neutraphil elastase 1 (HNE1) 抑制剂， 口服 active。
More
