Information on EC 1.6.3.1 - NAD(P)H oxidase (H2O2-forming) and Organism(s) Homo sapiens

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea


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EC NUMBER
COMMENTARY hide
1.6.3.1
-
RECOMMENDED NAME
GeneOntology No.
NAD(P)H oxidase (H2O2-forming)
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
NAD(P)H + H+ + O2 = NAD(P)+ + H2O2
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
oxidation
-
-
-
-
redox reaction
-
-
-
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reduction
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
NAD(P)H:oxygen oxidoreductase (H2O2-forming)
Requires FAD, heme and calcium. When calcium is present, this transmembrane glycoprotein generates H2O2 by transfering electrons from intracellular NAD(P)H to extracellular molecular oxygen. The electron bridge within the enzyme contains one molecule of FAD and probably two heme groups. This flavoprotein is expressed at the apical membrane of thyrocytes, and provides H2O2 for the thyroid peroxidase-catalysed biosynthesis of thyroid hormones.
CAS REGISTRY NUMBER
COMMENTARY hide
9032-22-8
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
-
tight regulation, critical to avoid excessive production of deleterious superoxide, is evident from the large number of proteins involved in oxidase assembly. These include Nox2 itself, p22phox, p47phox, p67phox, and p40phox, all essential subunits whose mutations can cause CGD Also crucial is Rac GTPase, which binds p67phox and the dehydrogenase domain of Nox2. In the resting state, Nox2 and p22phox form an inactive membrane complex known as cytochrome b558. Product superoxide is the first reactive oxygen species in a cascade of metabolites including hydrogen peroxide and peroxynitrite
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
NAD(P)H + H+ + O2
NAD(P)+ + H2O2
show the reaction diagram
NADH + H+ + O2
NAD+ + H2O2
show the reaction diagram
NADPH + O2
NADP+ + O2-
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
NAD(P)H + H+ + O2
NAD(P)+ + H2O2
show the reaction diagram
NADH + H+ + O2
NAD+ + H2O2
show the reaction diagram
NADPH + H+ + O2
NADP+ + H2O2
show the reaction diagram
-
-
-
-
?
NADPH + O2
NADP+ + O2-
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
FMN
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can replace for FAD
NADPH
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Fe2+
-
heme iron
additional information
-
Mg2+ cannot substitute for Ca2+, metal binding/dissociation kinetics, overview
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-epicatechin
-
serves as prodrug for conversion into apocynin-like NAD(P)H oxidase inhibitors
(-)-epicatechin glucuronide
-
acts both as a superoxide anion scavenger,and inhibitory to NAD(P)H oxidase, with apocynin-like mode of NADPH oxidase inhibition
(-)-epigallocatechin gallate
-
inhibition of intracellular reactive oxygen species generation
(2Z)-2-(5-hydroxy-4,6-dimethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N,N-di(prop-2-en-1-yl)hydrazinecarbothioamide
-
complete inhibition at 0.01 mM
(3Z)-3-(3,4-dihydroxybenzylidene)-5-nitro-1,3-dihydro-2H-indol-2-one
-
complete inhibition at 0.01 mM
(3Z)-3-[4-hydroxy-3,5-di(propan-2-yl)benzylidene]-1,3-dihydro-2H-indol-2-one
-
complete inhibition at 0.01 mM
1-(2-chlorobenzyl)-4-methyl-5-[3-(2-oxopyrrolidin-1-yl)propyl]-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
1-(4-fluorobenzyl)-5-[2-(1H-indol-3-yl)ethyl]-4-methyl-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
1-acetyl-2-(2-chlorophenyl)-4-methyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
1-acetyl-4-methyl-2-(2-methylphenyl)-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
1-acetyl-4-methyl-2-phenyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
1-[(3-methoxyphenyl)acetyl]-4-methyl-2-phenyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
15-cis-(4-propyl-cyclohexyl)-16,17,18,19,20-pentanor-9-deoxy-9alpha,6-nitrilo-prostaglandin F1 methyl ester
-
0.021 mM, 50% inhibition of the enzyme in neutrophils possible due to scavenging of O2-, inhibition of SDS-induced activation in cell free extracts, 0.22 mM, 50% inhibition
2,3,8,9-tetrahydroxy-5-(2-hydroxy-5-nitrobenzyl)phenanthridin-6(5H)-one
-
complete inhibition at 0.01 mM
2,3,8,9-tetrahydroxy-5-(3-nitrobenzyl)phenanthridin-6(5H)-one
-
complete inhibition at 0.01 mM
2,3,8,9-tetrahydroxy-5-(4-nitrobenzyl)phenanthridin-6(5H)-one
-
93% inhibition at 0.01 mM
2,3,8,9-tetrahydroxy-5-[2-(phenylsulfonyl)benzyl]phenanthridin-6(5H)-one
-
95% inhibition at 0.01 mM
2,4,5-trimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2,4-dimethyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-(1,3-benzothiazol-2-yl)-1-(2-chlorobenzyl)-4-methyl-5-(morpholin-4-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(1,3-benzothiazol-2-yl)-4-ethyl-5-(2-methoxyethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(1,3-benzothiazol-2-yl)-4-methyl-1-(pyridin-2-ylmethyl)-5-(tetrahydrofuran-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(1,3-benzothiazol-2-yl)-4-methyl-5-(morpholin-4-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(1,3-benzothiazol-2-yl)-5-[2-(1H-imidazol-4-yl)ethyl]-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(1,3-benzothiazol-2-yl)-5-[2-(1H-indol-3-yl)ethyl]-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2,5-dichlorobenzyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-(2-chloro-4-fluorobenzyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-(2-chloro-4-fluorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]-pyridine-3,6(2H,5H)-dione
-
-
2-(2-chloro-4-fluorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chloro-4-fluorophenyl)-5-(2-pyridin-2-ylethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-(2-fluorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-([methyl(phenyl)amino]methyl)-5-[2-(pyridin-2-yl)ethyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-methyl-5-(3-phenylprop-2-yn-1-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-methyl-5-(4-[(4-methylpiperazin-1-yl)methyl]benzyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo-[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-methyl-5-[(6-morpholin-4-ylpyridin-2-yl)-methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-[[4-(3-methoxyphenyl)piperazin-1-yl]-methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-4-[[methyl(phenyl)amino]methyl]-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-5-(3-ethoxypropyl)-4-methyl-1-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-5-(3-hydroxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-5-(cyclohexylmethyl)-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-4-[[methyl(pyridin-3-ylmethyl)amino]methyl]-1H-pyrazolo[4,3-c]-pyridine-3,6(2H,5H)-dione
-
-
2-(2-chlorophenyl)-5-[2-(dimethylamino)ethyl]-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-fluorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(2-methoxyethyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-6-methoxy-4H-chromen-4-one
-
complete inhibition at 0.01 mM
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
-
complete inhibition at 0.01 mM
2-(3,4-dihydroxyphenyl)-5-hydroxy-3,7-dimethoxy-4H-chromen-4-one
-
88% inhibition at 0.01 mM
2-(3-chlorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(4-chlorobenzyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-(4H-3,1-benzothiazin-2-yl)-1-benzyl-4-methyl-5-(tetrahydrofuran-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
2-(7-chloroquinolin-4-yl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-benzyl-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoic acid
-
89% inhibition at 0.01 mM
2-[(2,3,8,9-tetrahydroxy-6-oxophenanthridin-5(6H)-yl)methyl]benzonitrile
-
97% inhibition at 0.01 mM
2-[(2E)-2-(3,4-dihydroxybenzylidene)hydrazinyl]-N-(3-nitrophenyl)-2-oxoacetamide
-
96% inhibition at 0.01 mM
2-[2-(4-chlorophenoxy)ethyl]-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
2-[4-(benzyloxy)phenyl]-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
3'-(or 4'-)methylluteolin
-
-
3'-O-methyl epicatechin
-
-
3,5,7-trihydroxy-2-(4-hydroxy-3-methylphenyl)-4H-chromen-4-one
-
94% inhibition at 0.01 mM
3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
-
complete inhibition at 0.01 mM
3-(3,4-dihydroxycyclohexa-2,4-dien-1-yl)-2,7-dihydroxy-4H-chromen-4-one
-
86% inhibition at 0.01 mM
3-(3-chlorophenyl)-N-[2-(piperazin-1-yl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
Shionigi compound
3-(3-chlorophenyl)-N-[4-(piperidin-4-yl)phenyl]pyrazolo[1,5-a]pyrimidine-5-carboxamide
-
-
3-(4,5-dimethyl-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl)benzonitrile
-
-
4'-O-methyl epicatechin
-
-
4,5-dimethyl-2-(4-phenyl-1,3-thiazol-2-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4,5-dimethyl-2-(5-[(4-methylpiperazin-1-yl)sulfonyl]pyridin-2-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4-(2-amino-ethyl)-benzolsulphonyl-fluoride
-
-
4-(2-aminoethyl)-benzenesulfonyl fluoride
-
-
4-methyl-2-(2-methylphenyl)-5-(pyridine-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4-methyl-2-phenyl-5-(2-phenylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4-methyl-2-phenyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]-pyridine-3,6(2H,5H)-dione
-
-
4-methyl-3-methylidene-2-(2-phenylethyl)-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
4-methyl-3-methylidene-2-[2-(morpholin-4-yl)ethyl]-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
-
4-methyl-5-(3-phenoxybenzyl)-2-([1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4-[(4-fluorophenoxy)methyl]-5-(2-methoxyethyl)-2-(2-morpholin-4-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4-[[(2-chlorobenzyl)oxy]methyl]-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
4-[[2-(1,3-benzothiazol-2-yl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]methyl]benzoic acid
-
-
4-[[2-(2-chlorophenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]methyl]benzenesulfonamide
-
-
4-[[benzyl(methyl)amino]methyl]-2-(2-chloro-4-fluorophenyl)-5-(3-methoxypropyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
-
complete inhibition at 0.01 mM
5-(1,3-benzodioxol-5-ylmethyl)-4-methyl-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
5-(E)-6,9-deoxa-6,9alpha-methylene-15-cyclopentyl-16,17,18,19,20-pentanor-prostaglandin I2
-
inhibition of sodiumdodecylsulfate-induced activation in cell free extracts, 0.17 mM, 50% inhibition
5-(furan-2-ylmethyl)-4-methyl-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
5-benzyl-2-(4-fluorophenyl)-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
-
5-[(2,5-dihydroxybenzyl)amino]-2-hydroxybenzoic acid
-
82% inhibition at 0.01 mM
abruquinone C
-
-
apocynin
ATDITGPIILQTYRA
-
a peptide inhibitor derived from human p47phox
AYRRNSVRFL
-
inhibits NADPH oxidase activation
AYRRNSVRFVRFLN
-
a peptide inhibitor derived from human p47phox
betaPix
-
guanine nucleotide exchange factor, overexpression of the central PH domain of betaPix results in inhibition of superoxide anion generation in response to EGF
-
betulinic acid
-
attenuates the expression of NAD(P)H oxidase subunits Nox4 and p22phox, thereby reducing oxidative stress and improving endothelial nitric oxide synthase function. Treated cells show in increased production of bioactive nitric oxide
bilirubin
-
bilirubin concentration-dependently reduces NADPH oxidase-dependent superoxide production stimulated by phorbol 12-myristate 13-acetate
Cdc42
-
a small monomeric GTPase, competitive inhibitor of Nox2, might also be a competitive inhibitor of Nox1
-
CERLVRFWRSQQKVV
-
a peptide inhibitor derived from human gp91phox/NOX2
COMT-methylated procyanidin B2
-
-
-
CSTRVRRQLDRNLTFHK
-
a peptide inhibitor derived from human gp91phox/NOX2
dihydrokaempferol
-
-
dihydrotamarixetin
-
-
diosmetin
-
-
diphenylene iodinium
-
treatment of NB-4 cells blocks basal generation of reactive oxygen species and arsenic trioxide-induced apoptosis
diphenylene iodinium chloride
-
enzyme inhibitor, pretreatment of cells completely blocks insulin-stimulated activation of hypoxia-inducible factor 1
diphenylene iodonium
diphenyleneiodonium
diphenyliodonium
-
-
endothelin-1
-
inhibits NADPH oxidase activity, superoxide generation, and cell proliferation in human abdominal aortic endothelial cells via the ETB1-Pyk2-Rac1-Nox1 pathway. Endothelin-1 significantly attenuates NADPH oxidase activity and cell proliferation, which can be abolished by silencing of the Nox1 gene. RNA interference silencing of ETB1 receptors significantly increases NADPH oxidase activity, and blocks the inhibitory effect of endothelin-1 on NADPH oxidase activity. Endothelin-1 also attenuates angiotensin II-induced activation of NADPH oxidase and cell proliferation
Epicatechin gallate
-
-
epigallocatechin
-
-
epigallocatechin gallate
-
-
FAVHHDEEDVITG
-
a peptide inhibitor derived from human gp91phox/NOX2
FAVHHDEEKDVITG
-
-
ferulic acid
-
-
FIRHIALLGFEKRFV
-
a peptide inhibitor derived from human p47phox
FLRGSSACCSTRVRRQL
fulvene-5
-
-
GK-136901
-
inhibition of NOX1 and NOX4
gliotoxin
-
-
gomisin C
-
-
hesperetin
-
-
honokiol
IRNAHSIHQRSRKRL
-
a peptide inhibitor derived from human p47phox
ISNSESGPRGVHFIFNKENF
-
a peptide inhibitor derived from human gp91phox/NOX2
isorhamnetin
-
-
isorhamnetin glucuronide
-
-
KTIELQMKKKGFKM
-
a peptide inhibitor derived from human gp91phox/NOX2
LKLKKIYFYWLCRDTHAF
-
a peptide inhibitor derived from human gp91phox/NOX2
LKSVWYKYCN
-
a peptide inhibitor derived from human gp91phox/NOX2
LKSVWYKYCNN
-
a peptide inhibitor derived from human gp91phox/NOX2
magnolol
-
-
methimazol
-
partial
methyl 2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoate
-
91% inhibition at 0.01 mM
ML171
-
inhibition NOX1
N'1,N'2-bis[(E)-(2,3-dihydroxyphenyl)methylidene]ethanedihydrazide
-
complete inhibition at 0.01 mM
N'1,N'2-bis[(E)-(3,4-dihydroxyphenyl)methylidene]ethanedihydrazide
-
complete inhibition at 0.01 mM
N-(1-cyclohexylethyl)-4-phenylphthalazin-1-amine
-
-
N-(3-aminophenyl)-N'-[1-(4-hydroxy-3-methoxyphenyl)ethyl]ethanediamide
-
complete inhibition at 0.01 mM
N-[(3Z)-3-(4-hydroxy-3-methoxybenzylidene)-2-oxo-2,3-dihydro-1H-indol-5-yl]acetamide
-
complete inhibition at 0.01 mM
N-[1-(3,4-dihydroxyphenyl)ethyl]-N'-(3-nitrophenyl)ethanediamide
-
complete inhibition at 0.01 mM
N-[2-(2-chlorophenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(4-fluorophenoxy)acetamide
-
-
N-[3-(4,5-dimethyl-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl)phenyl]acetamide
-
-
N4-(3-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine
-
98% inhibition at 0.01 mM
N4-(4-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine
-
complete inhibition at 0.01 mM
naringenin
-
-
neopterin
norathyriol
-
-
Nox2ds-tat
-
inhibition of NAOX1 and NOX2
-
O-methyl-epicatechin
-
inhibits endothelial NAD(P)H oxidase activity and prevents superoxide anion formation
-
perhexilline
-
-
phallacidin
-
pretreatment of human pulmonary artery endothelial cells before induction of hyperoxia attenuates hyperoxia-induced cortical actin thickening and reactive oxygen species production
Phenylarsine oxide
-
-
Plumbagin
-
inhibition of NOX4
procyanidin B2
-
acts both as a superoxide anion scavenger, and inhibitory to NAD(P)H oxidase, with apocynin-like mode of NADPH oxidase inhibition
prodigiosin
-
-
propylthiouracil
-
partial
prostaglandin E1
-
inhibition of sodiumdodecylsulfate-induced activation in cell free extracts, 0.044 mM, 50% inhibition
PTKISRCPPHLLDFFK
-
a peptide inhibitor derived from human p47phox
QRRRQARPGPQSPG
-
a peptide inhibitor derived from human p47phox
quercetin 3-O-alpha-D-glucopyranoside
-
complete inhibition at 0.01 mM
quercetin glucuronide
-
-
RFVPSQHYVYMFLVK
-
a peptide inhibitor derived from human p47phox
RGVHFIF
rosiglitazone
-
activates 5'-AMP-activated protein kinase which, in turn, prevents hyperactivity of NAD(P)H oxidase induced by high glucose, possibly through protein kinase C inhibition. Rosiglitazone protects endothelial cells against glucose-induced oxidative stress with an 5'-AMP-activated protein kinase-dependent and a PPARgamma-independent mechanism
RRNSVRFLQQRRRQA
-
a peptide inhibitor derived from human p47phox
RRSSIRNAHSIHQRSRKRLS
-
a peptide inhibitor derived from human p47phox
RSRKRLSQDAYRRNSVRF
RSRKRLSQDAYRRNSVRFLQQR
-
a peptide inhibitor derived from human p47phox
SNSESGPRGVHFIFNKEN
-
-
SRKRLSQDAYRRNS
-
a peptide inhibitor derived from human p47phox
STRVRRQLDRNLTF
-
a peptide inhibitor derived from human gp91phox/NOX2
tamarixetin
-
-
VAS2870
VAS3947
-
i.e. 3-benzyl-7-(2-oxazolyl)thio-1,2,3-triazolo[4,5-d]pyrimidine, specific low micromolar NADPH oxidase inhibitor
VWYYRVYDIPPKFFYTRKLL
-
a peptide inhibitor derived from human gp91phox/NOX2
WWFCQMKAKRGWIPA
-
a peptide inhibitor derived from human p47phox
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+)-(S)-2-(6-methoxynaphthalen-2-yl)propanoic acid
-
i.e. naproxen, nonsteroidal anti-inflammatory drug. Treatment increases isoform Nox2 expression in endothelial cells and diminishes production of bioactive nitric oxide. In healthy volunteers, treatment reduces nitroglycerin-induced, nitric oxide-mediated vasodilatation of the brachial artery
2-(2-(2,6-dichlorophenylamino)-phenyl)acetic acid
-
i.e. diclofenac, nonsteroidal anti-inflammatory drug. Treatment increases isoform Nox2 expression in endothelial cells and diminishes production of bioactive nitric oxide. In healthy volunteers, treatment reduces nitroglycerin-induced, nitric oxide-mediated vasodilatation of the brachial artery
4-(4-methylsulfonylphenyl)-3-phenyl-5H-furan-2-one
-
i.e. rofecoxib, nonsteroidal anti-inflammatory drug. Treatment increases isoform Nox2 expression in endothelial cells and diminishes production of bioactive nitric oxide. In healthy volunteers, treatment reduces nitroglycerin-induced, nitric oxide-mediated vasodilatation of the brachial artery
4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
-
i.e. celecoxib, nonsteroidal anti-inflammatory drug. Treatment increases isoform Nox2 expression in endothelial cells and diminishes production of bioactive nitric oxide. In healthy volunteers, treatment reduces nitroglycerin-induced, nitric oxide-mediated vasodilatation of the brachial artery
5-cyclopropyl-2-[1-(2-fluoro-benzyl)-1H-pyrazolo[3,4-b] pyridin-3-yl]-pyrimidin-4-ylamine
-
i.e. BAY 41-2272. THP-1 cells treated with BAY 41-2272 for 48 h significantly increase the superoxide anion release. BAY 41-2272 increases subunit gp91phox gene expression and causes a significant increase in cGMP and cAMP levels
A23127
-
a calcium ionophore
-
A23187
-
calcium ionophore. HaCaT keratinocytes overexpressing calcium- and arachidonic acid binding proteins S100A8/S100A9 showed enhanced, transient reactive oxygen species generation in response to A23187, as well as nuclear factor kappaB activation and increase in interleukin-8 mRNA levels
angiotensin II
apigenin
-
apigenin reduces cell viability, and induces apoptotic cell death in a dose-dependent manner. In addition, it evokes a dose-related elevation of intracellular reactive oxygen species level. Treatment with various inhibitors of the NADPH oxidase significantly blunts both the generation of reactive oxygen species and induction of apoptosis induced by apigenin
betaPix
-
a Rac1 guanine nucleotide exchange factor, appears to be constitutively bound to Nox1 and essential for its activity
-
cytochalasin D
-
enhancement of basal and hyperoxia-induced reactive oxygen species formation
formyl-Met-Leu-Phe
H2O2
-
Nox5 can be upregulated and activated by minute concentrations of hydrogen peroxide
heat shock protein 90
-
binding of heat shock protein 90 to the C-terminus of Nox5 appears to stabilize the protein and enhance expression and activity
-
interleukin-1beta
-
stimulates Nox1
-
ionomycin
-
-
isoobtusilactone A
-
isoobtusilactone A elicits a concentration-dependent growth impediment with IC50 value of 37.5 microM. Treated cells also display transient increase of reactive oxygen species during the earlier stage of the experiment, followed by the disruption of mitochondrial transmembrane potential. The presence of a reactive oxygen species scavenger N-acetyl-L-cysteine and the inhibitor of NADPH oxidase diphenyleneiodonium chloride block reactive oxygen species production and the subsequent apoptotic cell death
latrunculin A
-
enhancement of basal and hyperoxia-induced reactive oxygen species formation
N-formyl-L-methionyl-L-leucyl-L-phenylalanine
-
store-operated Ca2+ entry is required at the beginning of NADPH oxidase activation in response to N-formyl-L-methionyl-L-leucyl-L-phenylalanine in neutrophil-like HL-60 cells. When extracellular Ca2+ is initially removed, early addition of Ca2+ after stimulation causes a complete restoration of Ca2+ entry and H2O2production. Both Ca2+ entry and H2O2 production are decreased by purported SOCE blockers, 2-aminoethoxydiphenyl borane (2-APB) and SK&F 96365. Ca2+ influx in HL-60 cells relies on different membrane transient receptor potential canonical channels and Orai1 for allowing NADPH oxidase activation
NOXA1
-
in contrast to its Noxo1 partner, Noxa1 activity appears to be tightly regulated. Noxa1 contains four Rac-binding TPR motifs, a Nox activation domain and an SH3 domain that interacts with the prolinerich region of an organizer subunit, But the p40phox-binding PB1 domain is not well conserved and the SH3 domain in the middle of the molecule is missing. Phosphorylation of Noxa1 by protein kinase A favors binding to 14-3-3 and dissociation from Nox1, whereas other kinases appear to decrease Noxa1 affinity for Rac1 and Nox1. In contrast, phosphorylation of Noxa1 by Src on tyrosine 110 increases Nox1 activity
-
NOXO1
-
In contrast to its Noxo1 partner, Noxa1 activity appears to be tightly regulated. Unlike p47phox, because Noxo1 lacks an autoinhibitory domain, it is thought to constitutively bind the cytochrome, but similar to p47phox, Noxo1 facilitates oxidase assembly by binding both an activator subunit and p22phox. The proline-rich region of Noxo1 binds to an SH3 domain of the activator, whereas the tandem SH3 domains of Noxo1 bind to the proline-rich region of p22phox. Noxo1 also binds to the dehydrogenase domain of Nox1. The PX domain of Noxo1 provides an essential affinity for membrane phosphoinositides
-
p67phox
-
activation domain of p67phox triggers FAD reduction by Nox2. P40phox appears to increase oxidase activity in cooperation with p47phox not by inducing translocation to the membrane, but by retaining the oxidase at the phagosome
-
peptide C5a
-
-
-
phorbol 12-myristate 13-acetate
phorbol myristate acetate
-
-
phosphate
-
-
phosphatidylinositol 3-phosphate
-
subunit p40phox phosphatidylinositol 3-phosphate binding PX domain has phosphatidylinositol 3-phosphate-dependent and -independent functions. Translocation of subunit p67phox requires the PX domain but not 3-phosphoinositide binding. Activation of the oxidase by p40phox, however, requires both phosphatidylinositol 3-phosphate binding and an Src homology 3 domain competent to bind to poly-Pro ligands
platelet-activating factor
-
-
Poldip2
-
reactive oxygen species production is enhanced by the multifunctional Poldip2, which also interacts with p22phox, presumably at the beginning of the cytosolic C-terminus, upstream of the region dispensable for Nox4 activity
-
Protein kinase C
-
-
-
Rac
-
small GTPase Rac plays a positive role in isoform Nox3 activation in the presence of subunit p47phox and either subunits p67phox or Noxa1, whereas Rac fails to upregulate Nox3 activity when p47phox is replaced with Noxo1. Expression of constitutively active Rac1 mutant Q61L enhances not only superoxide production but also membrane translocation of p67phox
-
Rac1
-
in addition to cytosolic organizers and activators, Nox1 also requires Rac1 for activity. Rac1 interacts directly with the C-terminus of Nox1, even in the absence of Noxa1. Nox1 is stimulated by constitutively active Rac1 and inhibited by Rac1 knockdown. Rac1 provides a crucial mechanism for activation by agonists, particularly in cells that exclusively express Nox1/Noxo1/Noxal. Rac1 does not activate Nox4 in transfected cells. Rac1 may participate in Nox5 activation
-
salbutamol
-
salbutamol treatment enhances superoxide anion production in asthma patients through nitric oxide-mediated mechanisms. It exerts beneficial antioxidant effects through activation of catalase and attenuation of lipid peroxidation
sodiumdodecylsulfate
-
-
thrombin
-
thyrotropin
-
-
-
TNF-alpha
-
stimulates Nox1
-
Trp-Lys-Tyr-Met-Val-Met
-
activates
tumor necrosis factor-alpha
-
treatment of monocytic cells and isolated monocytes results in up-regulation of the NAD(P)H oxidase gene, neutrophil cytosolic factor 2. Treated cells have increased levels of mRNA and up-regulated expression of NADPH oxidase subunits p47phox, p67phox, and gp91phox, as well as increased oxidase activity. Pharmacological inhibitors of NF-kappaB activation block tumor necrosis factor-induced up-regulation, which correlates with a reduction in expression of the corresponding oxidase proteins and decreased superoxide anion production
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.1
NADH
-
pH 7.4, 30C, 1.5 mM Ca2+, patients with Grave's disease
0.015 - 0.1
NADPH
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.03
1-(2-chlorobenzyl)-4-methyl-5-[3-(2-oxopyrrolidin-1-yl)propyl]-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
Ki above 0.03 mM, 0.1 M phosphate buffer, pH 7.4, 37C
0.03
1-(4-fluorobenzyl)-5-[2-(1H-indol-3-yl)ethyl]-4-methyl-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
Ki above 0.03 mM, 0.1 M phosphate buffer, pH 7.4, 37C
0.00024
1-acetyl-2-(2-chlorophenyl)-4-methyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000398
1-acetyl-4-methyl-2-(2-methylphenyl)-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000409
1-acetyl-4-methyl-2-phenyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000285
1-[(3-methoxyphenyl)acetyl]-4-methyl-2-phenyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.002175
2,4,5-trimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000387
2,4-dimethyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.03
2-(1,3-benzothiazol-2-yl)-1-(2-chlorobenzyl)-4-methyl-5-(morpholin-4-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
Ki above 0.03 mM, 0.1 M phosphate buffer, pH 7.4, 37C
0.03
2-(1,3-benzothiazol-2-yl)-4-methyl-1-(pyridin-2-ylmethyl)-5-(tetrahydrofuran-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
Ki above 0.03 mM, 0.1 M phosphate buffer, pH 7.4, 37C
0.001208
2-(1,3-benzothiazol-2-yl)-4-methyl-5-(morpholin-4-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.004729
2-(1,3-benzothiazol-2-yl)-5-[2-(1H-imidazol-4-yl)ethyl]-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.001845
2-(1,3-benzothiazol-2-yl)-5-[2-(1H-indol-3-yl)ethyl]-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000218
2-(2,5-dichlorobenzyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000342
2-(2-chloro-4-fluorobenzyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000213
2-(2-chloro-4-fluorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]-pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000235
2-(2-chloro-4-fluorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000114
2-(2-chloro-4-fluorophenyl)-5-(2-pyridin-2-ylethyl)-4-(pyrrolidin-1-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000215
2-(2-chlorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000128
2-(2-chlorophenyl)-4-(2-fluorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000172
2-(2-chlorophenyl)-4-([methyl(phenyl)amino]methyl)-5-[2-(pyridin-2-yl)ethyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000158
2-(2-chlorophenyl)-4-methyl-5-(3-phenylprop-2-yn-1-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000515
2-(2-chlorophenyl)-4-methyl-5-(4-[(4-methylpiperazin-1-yl)methyl]benzyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000165
2-(2-chlorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1H-pyrazolo-[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000236
2-(2-chlorophenyl)-4-methyl-5-[(6-morpholin-4-ylpyridin-2-yl)-methyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000428
2-(2-chlorophenyl)-4-methyl-5-[4-(4-methylpiperazin-1-yl)-4-oxobutyl]-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000114
2-(2-chlorophenyl)-4-[(4-fluorophenoxy)methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000065
2-(2-chlorophenyl)-4-[[4-(3-methoxyphenyl)piperazin-1-yl]-methyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000151
2-(2-chlorophenyl)-4-[[methyl(phenyl)amino]methyl]-5-(pyridin-4-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.03
2-(2-chlorophenyl)-5-(3-ethoxypropyl)-4-methyl-1-(pyridin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
Ki above 0.03 mM, 0.1 M phosphate buffer, pH 7.4, 37C
0.000565
2-(2-chlorophenyl)-5-(3-hydroxypropyl)-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.00052
2-(2-chlorophenyl)-5-(cyclohexylmethyl)-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000047
2-(2-chlorophenyl)-5-[(1-methyl-1H-pyrazol-3-yl)methyl]-4-[[methyl(pyridin-3-ylmethyl)amino]methyl]-1H-pyrazolo[4,3-c]-pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000235
2-(2-chlorophenyl)-5-[2-(dimethylamino)ethyl]-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000308
2-(2-fluorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000313
2-(2-methoxyethyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.00034
2-(3-chlorophenyl)-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000259
2-(4-chlorobenzyl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.03
2-(4H-3,1-benzothiazin-2-yl)-1-benzyl-4-methyl-5-(tetrahydrofuran-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
Ki above 0.03 mM, 0.1 M phosphate buffer, pH 7.4, 37C
0.000458
2-(7-chloroquinolin-4-yl)-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000463
2-benzyl-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000326
2-[2-(4-chlorophenoxy)ethyl]-4-methyl-3-methylidene-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.00306
2-[4-(benzyloxy)phenyl]-4,5-dimethyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000293
3-(4,5-dimethyl-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl)benzonitrile
-
0.1 M phosphate buffer, pH 7.4, 37C
0.001947
4,5-dimethyl-2-(4-phenyl-1,3-thiazol-2-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.001418
4,5-dimethyl-2-(5-[(4-methylpiperazin-1-yl)sulfonyl]pyridin-2-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000173
4-methyl-2-(2-methylphenyl)-5-(pyridine-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.005232
4-methyl-2-phenyl-5-(2-phenylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000373
4-methyl-2-phenyl-5-(pyridin-3-ylmethyl)-1H-pyrazolo[4,3-c]-pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000334
4-methyl-3-methylidene-2-(2-phenylethyl)-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000445
4-methyl-3-methylidene-2-[2-(morpholin-4-yl)ethyl]-5-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-6H-pyrazolo[4,3-c]pyridin-6-one
-
0.1 M phosphate buffer, pH 7.4, 37C
0.03
4-methyl-5-(3-phenoxybenzyl)-2-([1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
Ki above 0.03 mM, 0.1 M phosphate buffer, pH 7.4, 37C
0.000153
4-[(4-fluorophenoxy)methyl]-5-(2-methoxyethyl)-2-(2-morpholin-4-ylethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000095
4-[(benzyloxy)methyl]-2-(2-chlorophenyl)-5-(pyrazin-2-ylmethyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000082
4-[[(2-chlorobenzyl)oxy]methyl]-2-(2-chlorophenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.004222
4-[[2-(1,3-benzothiazol-2-yl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]methyl]benzoic acid
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000259
4-[[2-(2-chlorophenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]methyl]benzenesulfonamide
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000165
4-[[benzyl(methyl)amino]methyl]-2-(2-chloro-4-fluorophenyl)-5-(3-methoxypropyl)-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.00544
5-(1,3-benzodioxol-5-ylmethyl)-4-methyl-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.00949
5-(furan-2-ylmethyl)-4-methyl-2-phenyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000878
5-benzyl-2-(4-fluorophenyl)-4-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
-
0.1 M phosphate buffer, pH 7.4, 37C
0.031
methimazol
-
-
0.000218
N-[2-(2-chlorophenyl)-4-methyl-3,6-dioxo-1,2,3,6-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(4-fluorophenoxy)acetamide
-
0.1 M phosphate buffer, pH 7.4, 37C
0.000328
N-[3-(4,5-dimethyl-3,6-dioxo-1,3,5,6-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl)phenyl]acetamide
-
0.1 M phosphate buffer, pH 7.4, 37C
0.026
propylthiouracil
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0049
(-)-epicatechin glucuronide
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.001
(2Z)-2-(5-hydroxy-4,6-dimethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N,N-di(prop-2-en-1-yl)hydrazinecarbothioamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.00113
(3Z)-3-(3,4-dihydroxybenzylidene)-5-nitro-1,3-dihydro-2H-indol-2-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00063
(3Z)-3-[4-hydroxy-3,5-di(propan-2-yl)benzylidene]-1,3-dihydro-2H-indol-2-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00017
2,3,8,9-tetrahydroxy-5-(2-hydroxy-5-nitrobenzyl)phenanthridin-6(5H)-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00026
2,3,8,9-tetrahydroxy-5-(3-nitrobenzyl)phenanthridin-6(5H)-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00158
2,3,8,9-tetrahydroxy-5-(4-nitrobenzyl)phenanthridin-6(5H)-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00158
2,3,8,9-tetrahydroxy-5-[2-(phenylsulfonyl)benzyl]phenanthridin-6(5H)-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00074
2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-6-methoxy-4H-chromen-4-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00085
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00102
2-(3,4-dihydroxyphenyl)-5-hydroxy-3,7-dimethoxy-4H-chromen-4-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00096
2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoic acid
Homo sapiens;
-
pH and temperature not specified in the publication
0.00059
2-[(2,3,8,9-tetrahydroxy-6-oxophenanthridin-5(6H)-yl)methyl]benzonitrile
Homo sapiens;
-
pH and temperature not specified in the publication
0.00102
2-[(2E)-2-(3,4-dihydroxybenzylidene)hydrazinyl]-N-(3-nitrophenyl)-2-oxoacetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0061
3'-(or 4'-)methylluteolin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.0079
3'-O-methyl epicatechin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.00068
3,5,7-trihydroxy-2-(4-hydroxy-3-methylphenyl)-4H-chromen-4-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.0012
3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00079
3-(3,4-dihydroxycyclohexa-2,4-dien-1-yl)-2,7-dihydroxy-4H-chromen-4-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.0207
4'-O-methyl epicatechin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.00113
5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
Homo sapiens;
-
pH and temperature not specified in the publication
0.00134
5-[(2,5-dihydroxybenzyl)amino]-2-hydroxybenzoic acid
Homo sapiens;
-
pH and temperature not specified in the publication
0.03
CERLVRFWRSQQKVV
Homo sapiens;
-
pH and temperature not specified in the publication
0.0045
COMT-methylated procyanidin B2
Homo sapiens;
-
25C, pH 7.4, cell lysate
-
0.002
CSTRVRRQLDRNLTFHK
Homo sapiens;
-
pH and temperature not specified in the publication
0.0049
dihydrokaempferol
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.0041
dihydrotamarixetin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.0076
diosmetin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.015
Epicatechin gallate
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.008
epigallocatechin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.0035
epigallocatechin gallate
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.01
FAVHHDEEDVITG
Homo sapiens;
-
pH and temperature not specified in the publication
0.0049
ferulic acid
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.001
FLRGSSACCSTRVRRQL
Homo sapiens;
-
pH and temperature not specified in the publication
0.0074
hesperetin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.004
ISNSESGPRGVHFIFNKENF
Homo sapiens;
-
pH and temperature not specified in the publication
0.0028
isorhamnetin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.0049
isorhamnetin glucuronide
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.02
KTIELQMKKKGFKM
Homo sapiens;
-
pH and temperature not specified in the publication
0.025
LKLKKIYFYWLCRDTHAF
Homo sapiens;
-
pH and temperature not specified in the publication
0.01
LKSVWYKYCN
Homo sapiens;
-
pH and temperature not specified in the publication
0.05
LKSVWYKYCNN
Homo sapiens;
-
pH and temperature not specified in the publication
0.00127
methyl 2-hydroxy-5-[(2-hydroxybenzyl)amino]benzoate
Homo sapiens;
-
pH and temperature not specified in the publication
0.00091
N'1,N'2-bis[(E)-(2,3-dihydroxyphenyl)methylidene]ethanedihydrazide
Homo sapiens;
-
pH and temperature not specified in the publication
0.00116
N'1,N'2-bis[(E)-(3,4-dihydroxyphenyl)methylidene]ethanedihydrazide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0013
N-(3-aminophenyl)-N'-[1-(4-hydroxy-3-methoxyphenyl)ethyl]ethanediamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0014
N-[(3Z)-3-(4-hydroxy-3-methoxybenzylidene)-2-oxo-2,3-dihydro-1H-indol-5-yl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.00164
N-[1-(3,4-dihydroxyphenyl)ethyl]-N'-(3-nitrophenyl)ethanediamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.00024
N4-(3-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine
Homo sapiens;
-
pH and temperature not specified in the publication
0.00107
N4-(4-aminophenyl)[1]benzothieno[3,2-d]pyrimidine-4,8-diamine
Homo sapiens;
-
pH and temperature not specified in the publication
0.0079
naringenin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.0038
procyanidin B2
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.00083
quercetin 3-O-alpha-D-glucopyranoside
Homo sapiens;
-
pH and temperature not specified in the publication
0.0049
quercetin glucuronide
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.004
RGVHFIF
Homo sapiens;
-
pH and temperature not specified in the publication
0.04
STRVRRQLDRNLTF
Homo sapiens;
-
pH and temperature not specified in the publication
0.0074
tamarixetin
Homo sapiens;
-
25C, pH 7.4, cell lysate
0.034
VWYYRVYDIPPKFFYTRKLL
Homo sapiens;
-
pH and temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
voltage-clamp experiments, enzyme activity depends on both membrane potential and concentration of NADPH, the shape of the Ie-V curve is influenced by the concentration of NADPH in the submillimolar range
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5 - 8
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
20
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
abdominal aortic endothelial cells
Manually annotated by BRENDA team
-
expression of isoform Nox4 mRNA in glioblastomas of WHO grade IV is significantly higher than other astrocytomas of WHO grades II and III
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
the cytosolic N-terminal segment, containing 4 calcium binding EF-hands is missing in Nox5S, a short calcium-insensitive variant, which is the dominant isoform in carcinoma cells, and expressed together with the long Nox5L in endothelial cells. Nox5S may be constitutively active or be a competitive inhibitor of calcium-dependent activation when present in the same tetrameric complex as Nox5L
Manually annotated by BRENDA team
-
in ischemic cardiomyocytes, Nox2 is upregulated in the cytosol and targeted to the nuclear pore complex
Manually annotated by BRENDA team
-
high expression
Manually annotated by BRENDA team
-
specimens obtained by directional coronary artherectomy
Manually annotated by BRENDA team
-
dermal fibroblasts overexpress specifically Nox4
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
adventitial and cardial
Manually annotated by BRENDA team
-
expression of isoform Nox4 mRNA in glioblastomas of WHO grade IV is significantly higher than other astrocytomas of WHO grades II and III
Manually annotated by BRENDA team
-
human microvascular endothelial cells
Manually annotated by BRENDA team
-
polymorphonuclear leukocyte
Manually annotated by BRENDA team
Duox1 and Duox2 localize distinctly in lung epithelial cells as well as in ex-vivo differentiated lung epithelia. The localization of functional Duox-DuoxA heterodimers seems to be controlled by the associated DuoxA subunit; Duox1 and Duox2 localize distinctly in lung epithelial cells as well as in ex-vivo differentiated lung epithelia. The localization of functional Duox-DuoxA heterodimers seems to be controlled by the associated DuoxA subunit, including Duox2 expression in ciliated cells in an ex vivo differentiated lung epithelium
Manually annotated by BRENDA team
-
peripheral blood lymphocyte
Manually annotated by BRENDA team
-
monocytic cell
Manually annotated by BRENDA team
-
muscle biopsies of patients with Barrett's esophagus
Manually annotated by BRENDA team
-
NADPH oxidase mediates angiotensin II-stimulated protein synthesis downstream of the type 1 receptor AT1 in myometrium smooth muscle cells
Manually annotated by BRENDA team
-
platelet-rich plasma
Manually annotated by BRENDA team
-
deficient for von Hippel-Lindau tumor suppressor gene
Manually annotated by BRENDA team
-
Barretts esophageal adenocarcinoma cells
Manually annotated by BRENDA team
-
neuroblastoma cell, cells differentiated by retinoic acid die after exposure to glycated albumin, a model of advanced glycation end product-modified protein. Undifferentiated cells are resistant to glycated albumin. Differentiated cells pre-treated with NAD(P)K oxidase inhibitor diphenyleneiodinium or with rottlerin, an inhibitor of protein kinase C delta, are able to prevent neuronal death induced by glycated albumin
Manually annotated by BRENDA team
-
very weak signal
Manually annotated by BRENDA team
-
primary tracheobronchial epithelial cell. Study on enzyme isoforms Duox1 and Duox2 mRNA expression after treatment with multiple cytokines. Duox1 expression is increased severalfold by treatment with Th2 cytokines IL-4 and IL-13, and by polyinosine-polycytydilic acid and rhinovirus infection. Duox2 expression is highly induced following treatment with Th1-cytokine IFN-gamma
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
; NOX1, Nox1 stimulation in endosomes is dependent on ClC-3, where this ion exchanger is required to balance the electrogenic activity of the enzyme
Manually annotated by BRENDA team
-
Burkholderia cenocepacia resides in macrophage vacuoles displaying an altered recruitment of the NADPH oxidase complex at the phagosomal membrane
Manually annotated by BRENDA team
-
after Fcgamma receptor-induced phagocytosis, yellow fluorescent protein-tagged subunits p67phox and p40phox translocate to granulocyte phagosomes before phagosome internalization and accumulation of a probe for phosphoinositol 3-phosphate. p67phox and p47phox accumulation on nascent and internalized phagosomes does not require p40phox or PI3 kinase activity. Translocation of p40phox to nascent phagosomes requires binding to p67phox but not phosphoinositol 3-phosphate
-
Manually annotated by BRENDA team
-
in resting cells, enzyme complex components p22phox and gp91phox are located in the plasma membrane and membranes of specific granules
Manually annotated by BRENDA team
-
critical role for granules as a site for assembly and activation of the oxidase enzyme system
Manually annotated by BRENDA team
additional information
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
65000
-
SDS-PAGE
138000
-
calculated from cDNA sequence
160000
-
SDS-PAGE, deglycosylated form
164000
-
SDS-PAGE
165000
-
x * 165000, SDS-PAGE
180000
190000
-
SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
-
1 * 22000-23000 + 1 * 76000-91000, subunits of the membrane component of the enzyme complex, cytochrome b558, SDS-PAGE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
phosphoprotein
side-chain modification
-
phosphorylation of cytosolic component p47-phox
additional information
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
association with p22phox is required for Nox4 activity, the 2 proteins stabilize each other
-
Nox1 activity is dependent on chaperones Hsp90 and PDI, which appear to be necessary not only for protein folding after synthesis, but also to maintain enzyme stability
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cytochrome b558 and cytosolic components p47-phox and p67-phox
-
recombinant His6-tagged wild-type and E99Q/E143Q mutant Ca2+ binding domain of NOX5 from Escherichia coli strain BL21(DE3) by nickel affinity and hydrophobic interaction chromatography, followed by ultrafiltration
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cloning of full length cDNA
-
Cos-7, CHO, Hek293, NIH3T3, HeLa and PLB-XCGD cells transfected with ThOX2 DNA, protein is expressed but is exclusively found in cytoplasm and shows no activity
-
expressed in Escherichia coli
-
expressed in HEK-293 cells
-
expression in COS-7 cell
-
expression in H9C2 cell
-
expression in HeLa cell
-
expression in HeLa cells and COS-7 cells
-
expression of His6-tagged wild-type and E99Q/E143Q mutant Ca2+ binding domain, residues 1-169, of NOX5 in Escherichia coli strain BL21(DE3)
-
stable transfection of COS-7 cells of subunits gp91phox, p22phox, p67phox, p47phox, and also p40phox fused to the N-terminus of green fluorescent protein
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside-induced suppression of NAD(P)H oxidase subunit expression is AMP-activated protein kinase alpha2-dependent
-
interleukin-3 incubation stimulates the synthesis of Nox2 cytosolic sub-unit p47phox
-
leptin suppresses NADPH oxidase expression/activity
-
loss of AMP-activated protein kinase activity increases NAD(P)H oxidase subunit expression (gp91phox, p47phox, p67phox, NOX1 and -4) and NAD(P)H oxidase-mediated superoxide production
-
NAD(P)H oxidase activity is increased in hypertension
-
NOX1 is upregulated by angiotensin II, PDGF, PGF, LDL, TNF-alpha, oscillatory shear stress BMP4, aldosterone plus salt, IFN-gamma, ET-1, T3, urokinase8, oxidized LDL, and vascular injury. NOX2 is upregulated by angiotensin II, ET-1, TGF-beta, IFN-gamma, oxidized LDL oscillatory shear stress, aldosterone plus salt, Ischemia, and vascular injury.NOX4 is upregulated by TGF-beta, thromboxane, TNF-alpha. IFN-gamma, urotensin, urokinase, oscillatory shear stress, hypoxia, hyperoxia vascular injury. NOX5 iss upregulated by angiotensin II, ET-1, thromboxane A2, TNF-alpha, atherosclerosis. Nox5 can be upregulated and activated by minute concentrations of hydrogen peroxide. In ischemic cardiomyocytes, Nox2 is upregulated in the cytosol and targeted to the nuclear pore complex
-
NOX4 gene expression is stronger in brain samples from stroke patients compared to healthy controls
-
Nox4 mRNA expression increases to 88% in fibroblasts cultured on 3-deoxyglucosone-collagen for 24 h compared to fibroblasts cultured on native collagen
-
the BRAFV600E oncogene upregulates the enzyme NOX4 via TGF-beta1 signaling pathway in papillary thyroid cancer cell line
-
the enzyme is elevated in human radio-induced thyroid tumors and in sporadic thyroid tumors
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D484T
-
mutant of the alpha-helical loop of isoform Nox2, neither NADPH oxidase nor iodonitrotetrazolium reductase activity
D500A
-
mutant of the alpha-helical loop of isoform Nox2, neither NADPH oxidase nor iodonitrotetrazolium reductase activity
D500G
-
mutant of the alpha-helical loop of isoform Nox2, neither NADPH oxidase nor iodonitrotetrazolium reductase activity
D500R
-
mutant of the alpha-helical loop of isoform Nox2, neither NADPH oxidase nor iodonitrotetrazolium reductase activity
E99Q/E143Q
-
site-directed mutagenesis, mutation in the Ca2+ binding domain of NOX5
K195A
-
mutation in D-loop of isoform Nox2, complete loss of enzymic activity, but normal p47phox translocation and normal iodonitrotetrazolium reductase activity
K195E
-
mutation in D-loop of isoform Nox2, complete loss of enzymic activity, but normal p47phox translocation and normal iodonitrotetrazolium reductase activity
medicine
epigenetic silencing of Duox is frequently observed in lung cancer
P437H
-
the mutation in the canonical NADPH binding motif of Nox4, analogous to the Nox2 mutation of a CGD patient, abolishes activity
Q36H
-
naturally occuring missense mutation. Mutation completely prevents routing of the protein to the cell surface. Protein is predominantly present as core N-glycosylated, thiol-reduced folding intermediate and retained within the endoplasmic reticulum
R198A/R198A
-
mutation in D-loop of isoform Nox2, complete loss of enzymic activity, but normal p47phox translocation and normal iodonitrotetrazolium reductase activity
R198Q/R199Q
-
mutation in D-loop of isoform Nox2, complete loss of enzymic activity, but normal p47phox translocation and normal iodonitrotetrazolium reductase activity
R199E
-
mutation in D-loop of isoform Nox2, complete loss of enzymic activity, but normal p47phox translocation and normal iodonitrotetrazolium reductase activity
R199Q
-
mutation in D-loop of isoform Nox2. Formylmethionine-activated mutant shows 4- to 8fold higher activity than wild-type
R376W
-
naturally occuring missense mutation. Mutation completely prevents routing of the protein to the cell surface. Protein is predominantly present as core N-glycosylated, thiol-reduced folding intermediate and retained within the endoplasmic reticulum
R57Q
-
mutation in the phophatidylinositol 3-phosphate binding region of subunit p47phox. Mutation abrogates phophatidylinositol 3-phosphate binding and produces a dominant inhibitory effect on agonist-induced superoxide production and membrane translocation of subunits p47phox and p67phox. Mutant p40phox displayes increased association with actin and moesin and is found enriched in the Triton X-100-insoluble fraction along with p67phox and p47phox
R57Q/D289A
-
double mutant of subunit p40phox. Mutant fails to associate with subunits p67phox or p47phox in co-immunoprecipitation and Western blotting assays and abolishes the dominant inhibitory effect of mutant R57Q in phorbol 12-myristate 13-acetate- or formyl-Met-Leu-Phe-induced superoxide production
R96E
-
Nox4 is inhibited by an R96E mutation in the cytosolic B loop, a region of the amino-terminal domain that interacts with the NADPH binding site
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine