Compound class:
Peptide or derivative
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.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Epinette C, Croix C, Jaquillard L, Marchand-Adam S, Kellenberger C, Lalmanach G, Cadene M, Viaud-Massuard MC, Gauthier F, Korkmaz B. (2012)
A selective reversible azapeptide inhibitor of human neutrophil proteinase 3 derived from a high affinity FRET substrate. Biochem Pharmacol, 83 (6): 788-96. [PMID:22209715] |
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2. Korkmaz B, Lesner A, Guarino C, Wysocka M, Kellenberger C, Watier H, Specks U, Gauthier F, Jenne DE. (2016)
Inhibitors and Antibody Fragments as Potential Anti-Inflammatory Therapeutics Targeting Neutrophil Proteinase 3 in Human Disease. Pharmacol Rev, 68 (3): 603-30. [PMID:27329045] |
