azapro-3   Click here for help

GtoPdb Ligand ID: 9221

Immunopharmacology Ligand
Comment: Azapro-3 is a synthetic, selective and reversible peptide inhibitor of proteinase 3 [1-2]. Competes competitively with enzyme substrate and is proteolytically stable. It does not inhibit neutrophil elastase, cathepsin G, chymotrypsin or granzyme B.
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Bioactivity Comments
Azapro-3, inhibits free PR3 in solution, PR3 bound to neutrophil membranes, and PR3 in crude lung secretions from patients with chronic inflammatory pulmonary diseases [1].
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
proteinase 3 Hs Inhibitor Inhibition 5.8 pKi - 1
pKi 5.8 (Ki 1.5x10-6 M) [1]