Neutrophil elastase

A neutrophil elastase that is encoded in the genome of human. [PRO:CNA, UniProtKB:P08246]

Synonyms

EC 3.4.21.37;
Bone marrow serine protease;
Elastase-2;
Human leukocyte elastase;
HLE;
Medullasin;
PMN elastase

Research

Bioassay Publications (57)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	1 (1.75)	18.7374
1990's	19 (33.33)	18.2507
2000's	11 (19.30)	29.6817
2010's	19 (33.33)	24.3611
2020's	7 (12.28)	2.80

Compounds (83)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
3,4-dichloroisocoumarin	Homo sapiens (human)	IC50	3.0000	1	1
pimagedine	Homo sapiens (human)	IC50	72.0000	1	1
stallimycin	Homo sapiens (human)	IC50	100.1000	2	2
emodin	Homo sapiens (human)	IC50	52.0000	1	1
phenylmethylsulfonyl fluoride	Homo sapiens (human)	IC50	73.6905	2	2
2-methylanthraquinone	Homo sapiens (human)	IC50	39.0000	1	1
chrysophanic acid	Homo sapiens (human)	IC50	18.0000	1	1
physcione	Homo sapiens (human)	IC50	6.2000	1	1
bentranil	Homo sapiens (human)	IC50	17.0000	1	1
bentranil	Homo sapiens (human)	Ki	9.5499	2	2
ng-nitroarginine methyl ester	Homo sapiens (human)	IC50	2.7000	1	1
closantel	Homo sapiens (human)	IC50	25.0000	1	0
lovastatin	Homo sapiens (human)	IC50	0.0270	1	1
ursolic acid	Homo sapiens (human)	IC50	0.4160	1	1
epigallocatechin gallate	Homo sapiens (human)	IC50	12.8000	1	1
midesteine	Homo sapiens (human)	IC50	1.0000	1	1
n-benzyloxycarbonylphenylalanyl-valine	Homo sapiens (human)	IC50	50.0000	1	0
sivelestat	Homo sapiens (human)	IC50	0.1273	9	9
sivelestat	Homo sapiens (human)	Ki	0.1152	4	4
l 658758	Homo sapiens (human)	Ki	1.7000	1	1
e 64	Homo sapiens (human)	IC50	300.0000	1	1
4-methyoxybenzoyl-n-glycine	Homo sapiens (human)	IC50	25.0000	1	0
l 659286	Homo sapiens (human)	IC50	2.0000	1	1
foy 251	Homo sapiens (human)	IC50	100.0000	1	1
omega-n-methylarginine	Homo sapiens (human)	IC50	0.3000	2	2
l 738167	Homo sapiens (human)	IC50	0.0030	2	2
1-hydroxy-2-methylanthraquinone	Homo sapiens (human)	IC50	11.0000	1	1
2-phenyl-1,2-benzisothiazol-3-(2h)-one	Homo sapiens (human)	IC50	1.1107	1	0
sb 203580	Homo sapiens (human)	IC50	0.0250	1	1
l 694,458	Homo sapiens (human)	IC50	0.0295	2	2
ono 6818	Homo sapiens (human)	Ki	0.0121	4	4
2-(3-nitrophenyl)-3,1-benzoxazin-4-one	Homo sapiens (human)	Ki	4.3652	1	1
bortezomib	Homo sapiens (human)	Ki	2.3000	1	1
propolin c	Homo sapiens (human)	IC50	22.8000	1	1
propolin c	Homo sapiens (human)	Ki	15.7000	1	1
N-(3-dibenzofuranyl)-4-morpholinecarboxamide	Homo sapiens (human)	IC50	50.0000	1	0
(4-Methyl-2-oxochromen-7-yl) furan-2-carboxylate	Homo sapiens (human)	IC50	0.0497	1	0
2-furancarboxylic acid (2-acetyl-1-benzothiophen-3-yl) ester	Homo sapiens (human)	IC50	1.5028	1	0
(4-Methoxyphenyl)-(2-methylsulfanyl-6,7-dihydro-[1,4]dioxino[2,3-f]benzimidazol-3-yl)methanone	Homo sapiens (human)	IC50	3.5062	1	0
6-fluoro-2-phenyl-1,2-benzothiazol-3-one	Homo sapiens (human)	IC50	2.3100	1	0
6-fluoro-2-(2-methylphenyl)-1,2-benzothiazol-3-one	Homo sapiens (human)	IC50	4.8000	1	0
n(6)-(1-iminoethyl)lysine	Homo sapiens (human)	IC50	2.4000	1	1
3-chloro-1-(4-methoxyphenyl)-4-(3-methyl-1-piperidinyl)pyrrole-2,5-dione	Homo sapiens (human)	IC50	50.0000	1	0
telaprevir	Homo sapiens (human)	IC50	5.5600	3	3
2-bromo-6-[1,4-dioxa-8-azaspiro[4.5]decan-8-yl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone	Homo sapiens (human)	IC50	50.0000	1	0
N,N-dimethyl-3-(3-oxo-1,2-benzothiazol-2-yl)benzenesulfonamide	Homo sapiens (human)	IC50	7.6300	1	0
quercetin	Homo sapiens (human)	IC50	18.3390	2	1
quercetin	Homo sapiens (human)	Ki	11.9000	1	1
apigenin	Homo sapiens (human)	IC50	46.1000	1	1
apigenin	Homo sapiens (human)	Ki	49.9000	1	1
luteolin	Homo sapiens (human)	IC50	12.7000	1	1
luteolin	Homo sapiens (human)	Ki	10.1000	1	1
clavulanic acid	Homo sapiens (human)	IC50	40.0000	1	1
amentoflavone	Homo sapiens (human)	IC50	1.2700	1	1
robustaflavone	Homo sapiens (human)	IC50	1.3300	1	1
camostat mesylate	Homo sapiens (human)	IC50	100.0000	1	1
benzyloxycarbonyl-phe-ala-fluormethylketone	Homo sapiens (human)	IC50	100.0000	1	1
sb 258719	Homo sapiens (human)	Ki	0.0316	1	2
sb 271046	Homo sapiens (human)	Ki	3.9811	1	1
N-(4-ethylphenyl)-3-(1-pyrrolyl)propanamide	Homo sapiens (human)	IC50	50.0000	1	0
5-Chloro-3-pyridinyl 2-furoate	Homo sapiens (human)	IC50	0.7412	1	0
rwj 68354	Homo sapiens (human)	IC50	0.0063	1	1
sb 223245	Homo sapiens (human)	Ki	0.0020	1	1
zd 8321	Homo sapiens (human)	Ki	0.0130	2	2
n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide	Homo sapiens (human)	IC50	42.3333	3	3
mdl 101146	Homo sapiens (human)	Ki	0.0238	3	4
2-(4-methoxyphenyl)-1,2-benzothiazol-3-one	Homo sapiens (human)	IC50	5.3500	1	0
2-(4-chlorophenyl)-1,2-benzothiazol-3-one	Homo sapiens (human)	IC50	1.1000	1	0
PF-00835231	Homo sapiens (human)	IC50	10.0000	1	1
2-(3-chlorophenyl)-1,2-benzothiazol-3-one	Homo sapiens (human)	IC50	1.9010	1	0
archazolid a	Homo sapiens (human)	IC50	0.3520	1	1
archazolid b	Homo sapiens (human)	IC50	0.3160	1	1
5-fluoro-2-phenyl-1,2-benzothiazol-3-one	Homo sapiens (human)	IC50	1.0300	1	0
2-(2-fluorophenyl)-1,2-benzothiazol-3-one	Homo sapiens (human)	IC50	2.2600	1	0
lyngbyastatin 7	Homo sapiens (human)	IC50	0.0260	2	2
mk-7009	Homo sapiens (human)	IC50	55.0000	2	2
delanzomib	Homo sapiens (human)	IC50	3.5500	1	1
bi 201335	Homo sapiens (human)	IC50	30.0000	1	1
6-(3,5-difluoroanilino)-9-(2,2-difluoroethyl)-2-purinecarbonitrile	Homo sapiens (human)	IC50	85.1138	1	1
e-6-o-p-coumaroyl scandoside methyl ester	Homo sapiens (human)	IC50	100.0000	1	1
2-(3-oxo-1,2-benzothiazol-2-yl)-N-phenylacetamide	Homo sapiens (human)	IC50	6.6900	1	0
n-((5-(methanesulfonyl)pyridin-2-yl)methyl)-6-methyl-5-(1-methyl-1h-pyrazol-5-yl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide	Homo sapiens (human)	IC50	0.0120	1	1
n-((5-(methanesulfonyl)pyridin-2-yl)methyl)-6-methyl-5-(1-methyl-1h-pyrazol-5-yl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide	Homo sapiens (human)	Ki	0.0120	1	2
4-hydroxy-6-methyl-2-pyrone	Homo sapiens (human)	Ki	8,128.3100	1	1
elasnin	Homo sapiens (human)	Ki	93.3254	1	1
rpx7009	Homo sapiens (human)	IC50	1,000.0000	1	1
sulfated pentagalloylglucoside	Homo sapiens (human)	IC50	0.0400	1	1
N-[4-(6-chloro-5-nitro-1H-benzimidazol-2-yl)phenyl]acetamide	Homo sapiens (human)	IC50	50.0000	1	0

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
7-amino-4-chloro-3-methoxy-2-benzopyran-1-one	Homo sapiens (human)	[I]	6.0000	1	1
7-amino-3-(2-bromoethoxy)-4-chloroisocoumarin	Homo sapiens (human)	[I]	0.0700	1	1
telaprevir	Homo sapiens (human)	IC90	100.0000	1	1
n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide	Homo sapiens (human)	IC90	100.0000	1	1
mk-7009	Homo sapiens (human)	IC90	100.0000	1	1

Enables

This protein enables 8 target(s):

Target	Category	Definition
protease binding	molecular function	Binding to a protease or a peptidase. [GOC:hjd]
transcription corepressor activity	molecular function	A transcription coregulator activity that represses or decreases the transcription of specific gene sets via binding to a DNA-bound DNA-binding transcription factor, either on its own or as part of a complex. Corepressors often act by altering chromatin structure and modifications. For example, one class of transcription corepressors modifies chromatin structure through covalent modification of histones. A second class remodels the conformation of chromatin in an ATP-dependent fashion. A third class modulates interactions of DNA-bound DNA-binding transcription factors with other transcription coregulators. [GOC:txnOH-2018, PMID:10213677, PMID:16858867]
endopeptidase activity	molecular function	Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain. [http://merops.sanger.ac.uk/about/glossary.htm#ENDOPEPTIDASE]
serine-type endopeptidase activity	molecular function	Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
heparin binding	molecular function	Binding to heparin, a member of a group of glycosaminoglycans found mainly as an intracellular component of mast cells and which consist predominantly of alternating alpha-(1->4)-linked D-galactose and N-acetyl-D-glucosamine-6-sulfate residues. [GOC:jl, ISBN:0198506732]
peptidase activity	molecular function	Catalysis of the hydrolysis of a peptide bond. A peptide bond is a covalent bond formed when the carbon atom from the carboxyl group of one amino acid shares electrons with the nitrogen atom from the amino group of a second amino acid. [GOC:jl, ISBN:0815332181]
cytokine binding	molecular function	Binding to a cytokine, any of a group of proteins that function to control the survival, growth and differentiation of tissues and cells, and which have autocrine and paracrine activity. [GOC:ai, GOC:bf, ISBN:0198599471]

Located In

This protein is located in 11 target(s):

Target	Category	Definition
extracellular region	cellular component	The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators]
extracellular space	cellular component	That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684]
cytoplasm	cellular component	The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
cytosol	cellular component	The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
cell surface	cellular component	The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm]
secretory granule	cellular component	A small subcellular vesicle, surrounded by a membrane, that is formed from the Golgi apparatus and contains a highly concentrated protein destined for secretion. Secretory granules move towards the periphery of the cell and upon stimulation, their membranes fuse with the cell membrane, and their protein load is exteriorized. Processing of the contained protein may take place in secretory granules. [GOC:mah, ISBN:0198506732]
azurophil granule lumen	cellular component	The volume enclosed by the membrane of an azurophil granule, a primary lysosomal granule found in neutrophil granulocytes that contains a wide range of hydrolytic enzymes and is released into the extracellular fluid. [GOC:bf, PMID:17152095]
specific granule lumen	cellular component	The volume enclosed by the membrane of a specific granule, a granule with a membranous, tubular internal structure, found primarily in mature neutrophil cells. Most are released into the extracellular fluid. Specific granules contain lactoferrin, lysozyme, vitamin B12 binding protein and elastase. [GOC:bf, PMID:7334549]
phagocytic vesicle	cellular component	A membrane-bounded intracellular vesicle that arises from the ingestion of particulate material by phagocytosis. [GOC:go_curators, ISBN:0198506732]
collagen-containing extracellular matrix	cellular component	An extracellular matrix consisting mainly of proteins (especially collagen) and glycosaminoglycans (mostly as proteoglycans) that provides not only essential physical scaffolding for the cellular constituents but can also initiate crucial biochemical and biomechanical cues required for tissue morphogenesis, differentiation and homeostasis. The components are secreted by cells in the vicinity and form a sheet underlying or overlying cells such as endothelial and epithelial cells. [GOC:BHF, GOC:rph, PMID:21123617]
extracellular exosome	cellular component	A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894]

Active In

This protein is active in 1 target(s):

Target	Category	Definition
extracellular space	cellular component	That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684]

Part Of

This protein is part of 1 target(s):

Target	Category	Definition
transcription repressor complex	cellular component	A protein complex that possesses activity that prevents or downregulates transcription. [GOC:mah]

Involved In

This protein is involved in 25 target(s):

Target	Category	Definition
negative regulation of transcription by RNA polymerase II	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH]
response to yeast	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a yeast species. [PMID:14707091]
leukocyte migration involved in inflammatory response	biological process	The movement of a leukocyte within or between different tissues and organs of the body contributing to an inflammatory response. [GOC:add, ISBN:0781735149, PMID:14680625, PMID:14708592, PMID:7507411, PMID:8600538]
biosynthetic process of antibacterial peptides active against Gram-negative bacteria	biological process	The chemical reactions and pathways resulting in the formation of an antibacterial peptide with activity against Gram-negative bacteria. [GOC:add, PMID:11807545]
proteolysis	biological process	The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah]
intracellular calcium ion homeostasis	biological process	A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah]
response to UV	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ultraviolet radiation (UV light) stimulus. Ultraviolet radiation is electromagnetic radiation with a wavelength in the range of 10 to 380 nanometers. [GOC:hb]
extracellular matrix disassembly	biological process	A process that results in the breakdown of the extracellular matrix. [GOC:jid]
protein catabolic process	biological process	The chemical reactions and pathways resulting in the breakdown of a protein by the destruction of the native, active configuration, with or without the hydrolysis of peptide bonds. [GOC:mah]
response to lipopolysaccharide	biological process	Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464]
negative regulation of chemokine production	biological process	Any process that stops, prevents, or reduces the frequency, rate, or extent of chemokine production. [GOC:mah]
negative regulation of interleukin-8 production	biological process	Any process that stops, prevents, or reduces the frequency, rate, or extent of interleukin-8 production. [GOC:mah]
positive regulation of interleukin-8 production	biological process	Any process that activates or increases the frequency, rate, or extent of interleukin-8 production. [GOC:mah]
defense response to bacterium	biological process	Reactions triggered in response to the presence of a bacterium that act to protect the cell or organism. [GOC:jl]
positive regulation of MAP kinase activity	biological process	Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators]
positive regulation of smooth muscle cell proliferation	biological process	Any process that activates or increases the rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc]
negative regulation of inflammatory response	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai]
positive regulation of immune response	biological process	Any process that activates or increases the frequency, rate or extent of the immune response, the immunological reaction of an organism to an immunogenic stimulus. [GOC:ai]
negative regulation of chemotaxis	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of the directed movement of a motile cell or organism in response to a specific chemical concentration gradient. [GOC:ai]
pyroptosis	biological process	A caspase-1-dependent cell death subroutine that is associated with the generation of pyrogenic mediators such as IL-1beta and IL-18. [GOC:mtg_apoptosis, PMID:18846107, PMID:21760595]
neutrophil-mediated killing of gram-negative bacterium	biological process	The directed killing of a gram-negative bacterium by a neutrophil. [GOC:add, ISBN:0781765196]
neutrophil-mediated killing of fungus	biological process	The directed killing of a fungal cell by a neutrophil. [GOC:add, ISBN:0781765196]
positive regulation of leukocyte tethering or rolling	biological process	Any process that activates or increases the frequency, rate or extent of leukocyte tethering or rolling. [GO_REF:0000058, GOC:als, GOC:TermGenie, PMID:18308860]
phagocytosis	biological process	A vesicle-mediated transport process that results in the engulfment of external particulate material by phagocytes and their delivery to the lysosome. The particles are initially contained within phagocytic vacuoles (phagosomes), which then fuse with primary lysosomes to effect digestion of the particles. [ISBN:0198506732]
acute inflammatory response to antigenic stimulus	biological process	An acute inflammatory response to an antigenic stimulus. An acute inflammatory response occurs within a matter of minutes or hours, and either resolves within a few days or becomes a chronic inflammatory response. [GO_REF:0000022, GOC:add, ISBN:0781735149]