proteinase 3 | S1: Chymotrypsin | IUPHAR Guide to IMMUNOPHARMACOLOGY

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proteinase 3

Target id: 2401

Nomenclature: proteinase 3

Family: S1: Chymotrypsin

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: ON :     proteinase 3 has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 256 19p13.3 PRTN3 proteinase 3
Mouse - 254 10 C1 Prtn3 proteinase 3
Rat - 254 7q11 Prtn3 proteinase 3
Previous and Unofficial Names
ACPA | AGP7 | Wegener granulomatosis autoantigen | C-ANCA | MBT | myeloblastin | PR3
Database Links
Specialist databases
MEROPS S01.134 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  X-ray crystal structure of human proteinase 3 (PR3).
Resolution:  2.2Å
Species:  Human
References:  2
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 11 [PMID: 29442501] Hs Inhibition 8.3 pKi 3
pKi 8.3 (Ki 5.4x10-9 M) [3]
Description: Inhibition of human PR3 in vitro.
azapro-3 Hs Inhibition 5.8 pKi 1
pKi 5.8 (Ki 1.5x10-6 M) [1]
compound 4g [PMID: 22595175] Hs Inhibition 5.8 pIC50 5
pIC50 5.8 (IC50 1.4x10-6 M) [5]
Clinically-Relevant Mutations and Pathophysiology
Disease:  Wegener granulomatosis
Synonyms: Wegener's granulomatosis [Disease Ontology: DOID:12132]
Disease Ontology: DOID:12132
OMIM: 608710
Orphanet: ORPHA900


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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]

2. Fujinaga M, Chernaia MM, Halenbeck R, Koths K, James MN. (1996) The crystal structure of PR3, a neutrophil serine proteinase antigen of Wegener's granulomatosis antibodies. J. Mol. Biol., 261 (2): 267-78. [PMID:8757293]

3. Guarino C, Gruba N, Grzywa R, Dyguda-Kazimierowicz E, Hamon Y, Łȩgowska M, Skoreński M, Dallet-Choisy S, Marchand-Adam S, Kellenberger C et al.. (2018) Exploiting the S4-S5 Specificity of Human Neutrophil Proteinase 3 to Improve the Potency of Peptidyl Di(chlorophenyl)-phosphonate Ester Inhibitors: A Kinetic and Molecular Modeling Analysis. J. Med. Chem., 61 (5): 1858-1870. [PMID:29442501]

4. 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]

5. Santana AB, Lucas SD, Gonçalves LM, Correia HF, Cardote TA, Guedes RC, Iley J, Moreira R. (2012) N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases. Bioorg. Med. Chem. Lett., 22 (12): 3993-7. [PMID:22595175]

How to cite this page

S1: Chymotrypsin: proteinase 3. Last modified on 27/02/2018. Accessed on 16/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY,