1.11.2.2: myeloperoxidase
This is an abbreviated version!
For detailed information about myeloperoxidase, go to the full flat file.
Word Map on EC 1.11.2.2
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1.11.2.2
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neutrophil
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necrosis
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leukocyte
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tnf
-
malondialdehyde
-
dismutase
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colitis
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reperfusion
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pulmonary
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artery
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endothelial
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polymorphonuclear
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ischemia
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catalase
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monocyte
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sham
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bowel
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lps
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mucosal
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ulcer
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edema
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bronchoalveolar
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wistar
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granulocyte
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lavage
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lipopolysaccharide
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sod
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hypochlorous
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hocl
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vasculitis
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ischemia-reperfusion
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factor-alpha
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macroscopic
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tnf-alpha
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eosinophil
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elastase
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dextran
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ancas
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myeloid
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dss-induced
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degranulation
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glomerulonephritis
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lactoferrin
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icam-1
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granulomatosis
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antineutrophil
-
instil
-
medicine
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carrageenan-induced
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lactoperoxidase
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crescent
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analysis
- 1.11.2.2
- neutrophil
- necrosis
- leukocyte
- tnf
- malondialdehyde
- dismutase
- colitis
-
reperfusion
- pulmonary
- artery
- endothelial
-
polymorphonuclear
- ischemia
- catalase
- monocyte
-
sham
- bowel
- lps
- mucosal
- ulcer
- edema
-
bronchoalveolar
- wistar
- granulocyte
-
lavage
- lipopolysaccharide
- sod
-
hypochlorous
- hocl
- vasculitis
-
ischemia-reperfusion
- factor-alpha
-
macroscopic
- tnf-alpha
-
eosinophil
- elastase
- dextran
-
ancas
- myeloid
-
dss-induced
-
degranulation
- glomerulonephritis
- lactoferrin
- icam-1
- granulomatosis
-
antineutrophil
-
instil
- medicine
-
carrageenan-induced
- lactoperoxidase
-
crescent
- analysis
Reaction
Synonyms
donor, hydrogen peroxide oxidoreductase, donor, hydrogen peroxideoxidoreductase, donor: H2O2 oxidoreductase, donor:H2O2 oxidoreductase, donor:hydrogen peroxide oxidoreductase, donor:hydrogen-peroxide oxidoreductase, EC 1.11.1.7, epx2a, hemi-MPO, hemi-myeloperoxidase, LPO, MPO, MPX, myeloperoxidase, peroxinectin, properoxinectin, recombinant human MPO, rhMPO, tissue myeloperoxidase
ECTree
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Inhibitors
Inhibitors on EC 1.11.2.2 - myeloperoxidase
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(5-(((5-amino-3H-[1,2,3]triazolo[4,5-b]pyridin-7-yl)oxy)methyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methanol
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(R)-7-(1,2-diphenylethyl)-1-methyl-1H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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(R)-7-(1-phenyl-3-((2-(trifluoromethyl)benzyl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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(R)-7-(1-phenyl-3-((4-phenylbicyclo[2.2.2]octan-1-yl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine trifluoroacetate salt
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(R)-7-(1-phenyl-3-((pyridin-2-ylmethyl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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(R)-7-(1-phenyl-4-(4-phenylpiperidin-1-yl)butyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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(R)-7-(3-((2-fluoroethyl)(4-phenylbicyclo[2.2.2]octan-1-yl)amino)-1-phenylpropyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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(R)-7-(3-(benzylamino)-1-phenylpropyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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(R)-7-(3-(benzyloxy)-1-phenylpropyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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(R)-7-(3-(methyl(4-phenylbicyclo[2.2.2]octan-1-yl)amino)-1-phenylpropyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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1-(2-[(propan-2-yl)oxy]ethyl)-2-sulfanylidene-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
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i.e. AZD-3241, irreversible inhibitor
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2-(6-(2,5-dimethoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide
PF-1355
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2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide
PF-06282999
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2-[6-(5-chloro-2-methoxyphenyl)-4-oxo-2-sulfanylidene-3,4-dihydropyrimidin-1(2H)-yl]acetamide
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2-[[3,5-bis(trifluoromethyl)benzyl]amino]-N,4-dihydroxypyrimidine-5-carboxamide
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3-((5-amino-3H-[1,2,3]triazolo[4,5-b] pyridin-7-yl)methyl)benzonitrile
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3-([(2R)-oxolan-2-yl]methyl)-2-sulfanylidene-1,2,3,7-tetrahydro-6H-purin-6-one
i.e. TX4, irreversible inhibitor
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3-[(4-fluorophenyl)methyl]-2-sulfanylidene-1,2,3,7-tetrahydro-6H-purin-6-one
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i.e. TX2, irreversible inhibitor
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4'-amino-4-fluorochalcone
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potent inhibition of the chlorinating activity. Compound is not toxic to neutrophils at concentrations below 100 microM
4'-amino-4-methylchalcone
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potent inhibition of the chlorinating activity. Compound is not toxic to neutrophils at concentrations below 100 microM
4'-aminochalcone
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potent inhibition of the chlorinating activity. Compound is not toxic to neutrophils at concentrations below 100 microM
4-(5-fluoro-1H-indol-3-yl)butanamide
reversible myeloperoxidase inhibitor, efficiently prevents enzyme-dependent LDL oxidation
4-aminobenzoic acid hydrazine
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metabolism of chloroacetonitrile to cyanide by MPO/H2O2/Cl- system is significantly reduced by 4-amino benzoic acid hydrazine to 52.6% of control value
4-hydroxy-2,2,6,6-tetra-methyl-1-piperidinyloxy radical
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tempol, 0.01 mM tempol efficiently inhibits peroxidase-mediated RNase nitration
4-hydroxy-2,2,6,6-tetramethyl piperidine-1-oxyl
i.e. tempol, inhibits both H2O2 consumption and taurine chlorination, reacts mostly as a reversible inhibitor of MPO by trapping it as MPO-II and the MPO-II-tempol complex, which are not within the chlorinating cycle
7-(((5-(difluoromethyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((2'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((2,6-dichlorobenzyl)thio)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((2-(1H-pyrazol-1-yl)benzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((2-(methylsulfonyl)benzyl)oxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((3'-fluoro-2-methylbiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((3'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((3-phenylisoxazol-5-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((4-chloro-3'-fluorobiphenyl-3-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((5-(difluoromethyl)-2-phenyl-2H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methoxy)-3H-[1,2,3]triazolo [4,5-b]pyridin-5-amine
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7-((5-phenyloxazol-2-yl)methoxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((R)-1-phenyl-3-(((1R,3R)-3-phenylcyclopentyl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((R)-1-phenyl-3-(((1R,4S)-4-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((R)-1-phenyl-3-(((1S,3S)-3-phenyl-2,3-dihydro-1H-inden-1-yl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((R)-1-phenyl-3-(((3R,6S)-6-phenyltetrahydro-2H-pyran-3-yl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((R)-1-phenyl-3-((trans-4-phenylcyclohexyl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-((R)-3-(((S)-2,3-dihydro-1H-inden-1-yl)amino)-1-phenylpropyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-(1-phenyl-3-((1-phenyl-2-oxabicyclo[2.2.2]octan-4-yl)amino)propyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-(2-methyl-3-(1-methyl-1H-pyrazol-3-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-(3-(1-methyl-1H-pyrazol-3-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-(3-(1-methyl-1H-pyrazol-4-yl)benzyloxy)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-(3-(trifluoromethyl)benzyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-(3-methoxycarbonylbenzyl)-3H-[1,2,3]triazolo [4,5-b]pyridin-5-amine
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7-(5-amino-3H-[1,2,3]triazolo[4,5-b]pyridin-7-yl)-13-(2-phenylethyl)-3,4,10,13-tetraazatricyclo[13.3.1.13,6]icosa-1(19),4,6(20),15,17-pentaen-12-one
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7-(benzyloxy)-3a,7a-dihydro-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
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7-([1-[(3-benzylphenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-([1-[(3-phenoxyphenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-([1-[(3-[[(3S)-pyrrolidin-3-yl]oxy]phenyl)methyl]-1H-pyrazol-3-yl]methyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[(1-benzyl-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[(1-phenyl-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[(1-[[3-(piperidin-4-yl)phenyl]methyl]-1H-pyrazol-3-yl)methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[(17S)-18-phenyl-16-oxa-2,8,9-triazapentacyclo[16.2.2.11,17.16,9.111,15]pentacosa-6(25),7,11(24),12,14-pentaen-5-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[(1R)-1-phenyl-3-[(4-phenylbicyclo[2.2.2]octan-1-yl)amino]propyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[(1R)-3-[[(1R)-2,3-dihydro-1H-inden-1-yl]amino]-1-phenylpropyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[(3R,4S,6S)-4-benzyl-2-oxa-7,13,14-triazatetracyclo[14.3.1.13,6.111,14]docosa-1(20),11(21),12,16,18-pentaen-10-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[14'-oxa-3',4',10'-triazaspiro[cyclopentane-1,12'-tricyclo[13.3.1.13,6]icosane]-1'(19'),4',6'(20'),15',17'-pentaen-7'-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[17-oxa-3,4,10-triazatetracyclo[16.3.1.13,6.112,16]tetracosa-1(22),4,6(24),12(23),13,15,18,20-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[17-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.113,17]pentacosa-1(23),4,6(25),13(24),14,16,19,21-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[18-oxa-3,4,10-triazatetracyclo[18.3.1.13,6.113,17]hexacosa-1(24),4,6(26),13(25),14,16,20,22-octaen-7-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[3-oxa-10,11,17-triazatetracyclo[16.2.2.14,8.110,13]tetracosa-4(24),5,7,11,13(23)-pentaen-14-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[8,9,15-triazatetracyclo[16.3.1.12,6.18,11]tetracosa-1(22),2(24),3,5,9,11(23),18,20-octaen-12-yl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-(1,2,3,4-tetrahydroisoquinolin-6-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-(4-fluorophenyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-(biphenyl-3-yl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-(biphenyl-3-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-(isoquinolin-6-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-(naphthalen-2-ylmethyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-(pyridin-2-yl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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7-[[1-([3-[(2,3-dihydro-1H-isoindol-4-yl)oxy]phenyl]methyl)-1H-pyrazol-3-yl]methyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine
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8-[(2-aminoethyl)amino]-3,7-dihydro-3-methyl-7-(3-phenoxypropyl)-1H-purine-2,6-dione
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betanin
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higher micromolar betanin concentrations inhibit the MPO-mediated chlorination reactions by scavenging of hypochlorous acid
dityrosine
inhibits MPO-derived dityrosine formation in a dose-dependent manner
indicaxanthin
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at neutral pH and depending on their concentration, indicaxanthin can exhibit a stimulating and inhibitory effect on the chlorination activity of MPO, whereas at pH 5.0 only inhibitory effects are observed even at micromolar concentrations
nitrite
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nitrite is an excellent inhibitor of the chlorination activity of myeloperoxidase, there is progressive inhibition of enzyme activity with increasing concentration of nitrite up to a maximum of 80%. Upon addition of 100 mM L-tyrosine, enzyme activity is completely restored
peptide inhibitor of complement C1
11.5fold reduction in enzyme activity at 7.5 mM
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Q3GA
inhibits MPO-derived dityrosine formation in a dose-dependent manner
serotonin
at higher concentrations than 0.02 mM, serotonin almost completely blocks the formation of hypochlorite
Sulfide
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at high sulfide concentrations, enzymic inhibition is observed above 0.25 mM (20% inhibition at 0.3 mM sulfide)
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2-(3,5-bistrifluoromethylbenzylamino)-6-oxo-1H-pyrimidine-5-carbohydroxamic acid
HX1, reversible inhibition
i.e. PF-06282999, irreversible inhibitor
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2-[6-(5-chloro-2-methoxyphenyl)-4-oxo-2-sulfanylidene-3,4-dihydropyrimidin-1(2H)-yl]acetamide
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i.e. PF-06282999, irreversible inhibitor
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most potent inhibitor of peroxidation, it irreversibly inhibits HOCl production by the purified myeloperoxidase. With neutrophils stimulated with opsonized zymosan or phorbol myristate acetate, 4-aminobenzoic acid hydrazide inhibits HOCI production by up to 90%
Br-
bromide binding to the halide-binding site responsible for shifts in the Soret band of the absorption spectrum of myeloperoxidase inhibits the enzyme by effectively competing with H2O2 for access to the distal histidine
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addition of the antioxidant enzyme catalase to incubation mixtures results in 56.1% decrease in cyanide release by MPO/H2O2/Cl- system
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inhibition of taurine chlorination by H2O2 becomes significant at about pH 6.6 and higher
H2O2
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at pH 5.0, H2O2 at high concentrations inhibits the enzyme. The rate of sulfoxide formation increases as the H2O2 concentration increases up to 0.2 mM, while a further increase in concentration results in a decrease in the rate of sulfoxide formation (40% inhibition at 1 mM H2O2)
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metabolism of chloroacetonitrile to cyanide by MPO/H2O2/Cl- system is significantly reduced by indomethacin to 88.9% of control value
quercetin
potent inhibitor, inhibits MPO-derived dityrosine formation in a dose-dependent manner
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salicylhydroxamic acid is a much poorer inhibitor of HOCI production with neutrophils stimulated with opsonized zymosan (0.2 mM is required for complete inhibition)
Sodium azide
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metabolism of chloroacetonitrile to cyanide by MPO/H2O2/Cl- system is significantly reduced by sodium azide to 43.9% of control value
halides serve as substrates or inhibitors, existence of two halide binding sites that have a distinct impact on the heme iron microenvironment in myeloperoxidase
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additional information
enterobactin is not an inhibitor of myeloperoxidase
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additional information
not inhibited by (E)-(5-fluoro-2-hydroxy)-alpha-aminocinnamic acid
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additional information
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not inhibited by (E)-(5-fluoro-2-hydroxy)-alpha-aminocinnamic acid
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