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Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | 267 | 19p13.3 | ELANE | elastase, neutrophil expressed | |
| Mouse | - | 265 | 10 39.72 cM | Elane | elastase, neutrophil expressed | |
| Rat | - | 265 | 7q11 | Elane | elastase, neutrophil expressed | |
| Previous and Unofficial Names |
| medullasin | HNE | Ela2 | elastase-2 | HLE | leukocyte elastase | NE | neutrophil elastase | elastase |
| Database Links |
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| Specialist databases | |
| MEROPS | S01.131 (Hs) |
| Other databases | |
| Alphafold | P08246 (Hs), Q3UP87 (Mm) |
| BRENDA | 3.4.21.37 |
| ChEMBL Target | CHEMBL248 (Hs), CHEMBL5156 (Mm) |
| DrugBank Target | P08246 (Hs) |
| Ensembl Gene | ENSG00000197561 (Hs), ENSMUSG00000020125 (Mm), ENSRNOG00000033685 (Rn) |
| Entrez Gene | 1991 (Hs), 50701 (Mm), 299606 (Rn) |
| Human Protein Atlas | ENSG00000197561 (Hs) |
| KEGG Enzyme | 3.4.21.37 |
| KEGG Gene | hsa:1991 (Hs), mmu:50701 (Mm), rno:299606 (Rn) |
| OMIM | 130130 (Hs) |
| Orphanet | ORPHA121511 (Hs) |
| Pharos | P08246 (Hs) |
| RefSeq Nucleotide | NM_001972 (Hs), NM_015779 (Mm), NM_001106767 (Rn) |
| RefSeq Protein | NP_001963 (Hs), NP_056594 (Mm), NP_001100237 (Rn) |
| UniProtKB | P08246 (Hs), Q3UP87 (Mm) |
| Wikipedia | ELANE (Hs) |
| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Immunopharmacology Comments |
| Neutrophil elastase (NE) is a serine proteinase with broad substrate specificity. It is stored in azurophil granules within neutrophils and is involved primarily in host defence. However, in addition to attacking proteins on invading microorganisms, secreted NE also hydrolyzes proteins of the host extracellular matrix, such as collagen-IV and elastin, hence its role in degenerative and inflammatory diseases. NE functions as a promoter of γδ T cell activation via a protease-activated receptor (PAR1)-dependent mechanism [5]. |
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1. Crocetti L, Giovannoni MP, Schepetkin IA, Quinn MT, Khlebnikov AI, Cilibrizzi A, Piaz VD, Graziano A, Vergelli C. (2011) Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase. Bioorg Med Chem, 19 (15): 4460-72. [PMID:21741848]
2. Muscia GC, Hautmann S, Buldain GY, Asís SE, Gütschow M. (2014) Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase. Bioorg Med Chem Lett, 24 (6): 1545-9. [PMID:24556381]
3. 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]
4. Stevens T, Ekholm K, Gränse M, Lindahl M, Kozma V, Jungar C, Ottosson T, Falk-Håkansson H, Churg A, Wright JL et al.. (2011) AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. J Pharmacol Exp Ther, 339 (1): 313-20. [PMID:21791628]
5. Towstyka NY, Shiromizu CM, Keitelman I, Sabbione F, Salamone GV, Geffner JR, Trevani AS, Jancic CC. (2018) Modulation of γδ T-cell activation by neutrophil elastase. Immunology, 153 (2): 225-237. [PMID:28888033]
6. Tsuda M, Muraoka Y, Nagai M, Aoyagi T, Takeuchi T. (1996) Poststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues. J Antibiot, 49 (9): 890-9. [PMID:8931723]
7. von Nussbaum F, Li VM, Allerheiligen S, Anlauf S, Bärfacker L, Bechem M, Delbeck M, Fitzgerald MF, Gerisch M, Gielen-Haertwig H et al.. (2015) Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem, 10 (7): 1163-73. [PMID:26083237]
S1: Chymotrypsin: elastase, neutrophil expressed. Last modified on 07/10/2020. Accessed on 25/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2358.
target has curated data in GtoImmuPdb
