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1.14.99.1: prostaglandin-endoperoxide synthase

This is an abbreviated version!
For detailed information about prostaglandin-endoperoxide synthase, go to the full flat file.

Word Map on EC 1.14.99.1

Reaction

arachidonate
+
reduced acceptor
+ 2 O2 =
prostaglandin H2
+
acceptor
+
H2O

Synonyms

(PG)H synthase, COX, COX-1, COX-2, COX1, Cox2, cyclooxygenase, cyclooxygenase 1, cyclooxygenase 2, cyclooxygenase-1, cyclooxygenase-1b, cyclooxygenase-2, cycloxigenase-2, fatty acid cyclooxygenase, hPGHS-1, hPGHS-2, oPGHS-1, PG G/H synthase 2, PG H synthase, PG synthetase, PG-endoperoxide synthase 2, PG-endoperoxide synthetase, PGH-synthase, PGHS, PGHS isoform-1, PGHS-1, PGHS-2, PHS, PHS-1, PHS-2, prostagladin-H synthase, prostaglandin endoperoxide H synthase, prostaglandin endoperoxide H synthase 1, prostaglandin endoperoxide H synthase 2, prostaglandin endoperoxide H synthase-1, prostaglandin endoperoxide H2 synthase-2, prostaglandin endoperoxide synthase, prostaglandin endoperoxide synthase 2, prostaglandin endoperoxide synthase-1, prostaglandin endoperoxide synthase-2, prostaglandin endoperoxide synthetase, prostaglandin G/H synthase, prostaglandin G/H synthase-2, prostaglandin H synthase, prostaglandin H synthase-1, prostaglandin H synthase-2, prostaglandin H2 synthase, prostaglandin H2 synthase-1, prostaglandin synthase, prostaglandin synthase-2, prostaglandin synthetase, prostaglandin-endoperoxide synthase, prostaglandin-endoperoxide synthase 1, prostaglandin-endoperoxide synthase 2, prostaglandin-H-synthase, prostaglandin-H-synthase 1, prostaglandin-H-synthase 2, PTGS 2, PTGS-1, PTGS-2, PTGS1, PTGS2, putative cyclooxygenase-3, synthase, prostaglandin, tPGHS-1, tPGHS-2

ECTree

     1 Oxidoreductases
         1.14 Acting on paired donors, with incorporation or reduction of molecular oxygen
             1.14.99 Miscellaneous
                1.14.99.1 prostaglandin-endoperoxide synthase

Inhibitors

Inhibitors on EC 1.14.99.1 - prostaglandin-endoperoxide synthase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,10-phenanthroline
-
weak
1-Mercapto-9,11,15-trihydroxyprosta-5,13-diene
-
inhibition of prostaglandin G1 synthesis
1-Mercapto-9-oxo-11,15-dihydroxyprosta-5,13-dione
-
inhibition of prostaglandin G1 synthesis
12-nitroarachidonic acid
nitro-fatty acid inhibition is due to a slow, tightly binding mechanism, it inhibits oxygenase and peroxidase activity PGHS-1, kinetics, overview. Inactivation of PGHS by nitroarachidonic acid involves two sequential steps: an initial reversible binding event, followed by a practically irreversible event leading to an inactivated enzyme. Inactivation is associated with irreversible disruption of heme binding to the protein, the inhibitor induces heme release from Fe2+-protoporphyrin-PGHS-1. In activated human platelets, nitroarachidonic acid significantly decreases PGHS-1-dependent thromboxane B2 formation in parallel with a decrease in platelet aggregation
14-nitroarachidonic acid
nitro-fatty acid inhibition is due to a slow, tightly binding mechanism, it inhibits oxygenase and peroxidase activity PGHS-1, kinetics, overview. Inactivation of PGHS by nitroarachidonic acid involves two sequential steps: an initial reversible binding event, followed by a practically irreversible event leading to an inactivated enzyme. Inactivation is associated with irreversible disruption of heme binding to the protein, the inhibitor induces heme release from Fe2+-protoporphyrin-PGHS-1. In activated human platelets, nitroarachidonic acid significantly decreases PGHS-1-dependent thromboxane B2 formation in parallel with a decrease in platelet aggregation
15-nitroarachidonic acid
nitro-fatty acid inhibition is due to a slow, tightly binding mechanism, it inhibits oxygenase and peroxidase activity PGHS-1, kinetics, overview. Inactivation of PGHS by nitroarachidonic acid involves two sequential steps: an initial reversible binding event, followed by a practically irreversible event leading to an inactivated enzyme. Inactivation is associated with irreversible disruption of heme binding to the protein, the inhibitor induces heme release from Fe2+-protoporphyrin-PGHS-1. In activated human platelets, nitroarachidonic acid significantly decreases PGHS-1-dependent thromboxane B2 formation in parallel with a decrease in platelet aggregation
2,2'-bipyridyl
-
weak
2,3-Dimercaptopropanol
-
inhibition of prostaglandin G1 synthesis
2-hydroxybutyric acid
-
weak
3,6-bis(3-[[(furan-2-yl)methyl]amino]propyl)-9H-xanthen-9-one
-
3,6-bis(5-[[(furan-2-yl)methyl]amino]pentyl)-9H-xanthen-9-one
-
3,6-bis[3-(2-methyl-1H-indol-1-yl)propyl]-9H-xanthen-9-one
-
3,6-bis[3-(4-methylpiperazin-1-yl)propyl]-9H-xanthen-9-one
-
3,6-bis[3-(4-nitroanilino)propyl]-9H-xanthen-9-one
-
3,6-bis[3-(cyclohexylamino)propyl]-9H-xanthen-9-one
-
3,6-bis[3-(morpholin-4-yl)propyl]-9H-xanthen-9-one
-
3,6-bis[3-(piperidin-1-yl)propyl]-9H-xanthen-9-one
-
3,6-bis[3-[(1H-pyrazol-3-yl)amino]propyl]-9H-xanthen-9-one
-
3,6-bis[3-[(2-chloropyridin-3-yl)amino]propyl]-9H-xanthen-9-one
-
3,6-bis[3-[(4H-1,2,4-triazol-4-yl)amino]propyl]-9H-xanthen-9-one
-
3,6-bis[3-[(pyrazin-2-yl)amino]propyl]-9H-xanthen-9-one
-
3,6-bis[3-[(pyridin-2-yl)amino]propyl]-9H-xanthen-9-one
-
3,6-bis[4-(1H-imidazol-2-yl)butyl]-9H-xanthen-9-one
-
3,6-bis[5-(2-methyl-1H-indol-1-yl)pentyl]-9H-xanthen-9-one
-
3,6-bis[5-(4-methylpiperazin-1-yl)pentyl]-9H-xanthen-9-one
-
3,6-bis[5-(4-nitroanilino)pentyl]-9H-xanthen-9-one
-
3,6-bis[5-(cyclohexylamino)pentyl]-9H-xanthen-9-one
-
3,6-bis[5-(morpholin-4-yl)pentyl]-9H-xanthen-9-one
-
3,6-bis[5-(piperidin-1-yl)pentyl]-9H-xanthen-9-one
-
3,6-bis[5-[(1H-pyrazol-3-yl)amino]pentyl]-9H-xanthen-9-one
-
3,6-bis[5-[(2-chloropyridin-3-yl)amino]pentyl]-9H-xanthen-9-one
-
3,6-bis[5-[(4H-1,2,4-triazol-4-yl)amino]pentyl]-9H-xanthen-9-one
-
3,6-bis[5-[(piperidin-1-yl)amino]pentyl]-9H-xanthen-9-one
-
3,6-bis[5-[(pyrazin-2-yl)amino]pentyl]-9H-xanthen-9-one
-
3,6-bis[5-[(pyridin-2-yl)amino]pentyl]-9H-xanthen-9-one
-
3,6-bis[6-(1H-imidazol-2-yl)hexyl]-9H-xanthen-9-one
-
5,8,11,14-Eicosatetraynoic acid
5-amino-2-hydroxy-N-(propan-2-yl)benzamide
-
5-amino-N-cyclohexyl-2-hydroxybenzamide
-
5-amino-N-hexyl-2-hydroxybenzamide
-
5-bromo-2-[4-fluorophenyl]-3-[4-methylsulfonylphenyl]-thiophene
5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxy-N-(4-methylphenyl)benzamide
-
6-methoxy-2-naphthyl acetic acid
-
active metabolite of nabumetone, isozyme 1, 50% inhibition at 0.2-0.8 mM, isozyme 2, 50% inhibition at 0.015-0.55 mM
6-methylnaphthylacetic acid
-
recombinant protein, 50% inhibition at 0.08-0.1 mM
6-[2,4-difluorophenoxy]-5-methyl-sulfonylamino-1-indanone
-
CGP28238, an isozyme-2 specific inhibitor, 65% inhibition at 100 nM
8-hydroxyquinoline
-
-
9,11-Dihydroxy-15S-mercaptoprosta-5,13-dienoic acid
-
or 15R-isomer, inhibition of prostaglandin G1 synthesis
9-nitroarachidonic acid
nitro-fatty acid inhibition is due to a slow, tightly binding mechanism, it inhibits oxygenase activity and peroxidase activity of PGHS-1, kinetics, overview. Inactivation of PGHS by nitroarachidonic acid involves two sequential steps: an initial reversible binding event, followed by a practically irreversible event leading to an inactivated enzyme. Inactivation is associated with irreversible disruption of heme binding to the protein, the inhibitor induces heme release from Fe2+-protoporphyrin-PGHS-1. In activated human platelets, nitroarachidonic acid significantly decreases PGHS-1-dependent thromboxane B2 formation in parallel with a decrease in platelet aggregation
acetoacetic acid
-
weak
Acetylsalicylic acid
albumin
-
alpha-linolenic acid
-
anirolac
-
isozyme 1, 50% inhibition at 0.0007 mM, isozyme 2, 50% inhibition at 0.009 mM
aspirin
bicarbonate
-
bicarbonate enhances peroxynitrite-mediated peroxidase inactivation
Butyric acid
-
-
BW 755C
-
recombinant protein, 50% inhibition at 0.01-0.02 mM
crotonic acid
-
-
DCM-extract of Angelicae dahuricae radix
0.1% inhibition of PGHS-1; 38.8% inhibition of PGHS-2
-
DCM-extract of Angelicae sinsesis radix
55.8% inhibition of PGHS-2; 75.0% inhibition of PGHS-1
-
DCM-extract of Atractylodis lanceae rhizoma
46.9% inhibition of PGHS-1; 50.3% inhibition of PGHS-2
-
DCM-extract of Atractylodis macrocephalae rhizoma
47.0% inhibition of PGHS-2; 58.6% inhibition of PGHS-1
-
DCM-extract of Cinnamomi ramulus
48.4% inhibition of PGHS-2; 73.5% inhibition of PGHS-1
-
DCM-extract of Houttuyniae herba
40.9% inhibition of PGHS-2; 46.8% inhibition of PGHS-1
-
DCM-extract of Notopterygii rhizoma seu radix
-2.1% inhibition of PGHS-2; 42.6% inhibition of PGHS-1
-
DCM-extract of Piperis sarmentosi herba
10.1% inhibition of PGHS-2; 47.2% inhibition of PGHS-1
-
DCM-extract of Platycodi radix
70.1% inhibition of PGHS-2; 77.8% inhibition of PGHS-1
-
DCM-extract of Zanthoxyli pericarpium
18.3% inhibition of PGHS-1; 31.3% inhibition of PGHS-2
-
DCM-extract of Zingiberis rhizoma
41.3% inhibition of PGHS-2; 52.9% inhibition of PGHS-1
-
delta-tocopherol-13'-carboxychromanol
-
inhibits isoform Cox-1 and suppresses Cox-1 mediated formation of thromboxane in collagen-stimulated rat's platelets
-
delta-tocotrienol
-
inhibits isoform Cox-1 and suppresses Cox-1 mediated formation of thromboxane in collagen-stimulated rat's platelets
delta-tocotrienol-13'-carboxychromanol
-
inhibits isoform Cox-1 and suppresses Cox-1 mediated formation of thromboxane in collagen-stimulated rat's platelets
-
diclofenac
diethyldithiocarbamate
-
-
dihydrolipoic acid
-
inhibition of prostaglandin G1 synthesis
dithiothreitol
-
inhibition of prostaglandin G1 synthesis
DL-Propanolol
-
-
docosahexaenoic acid
-
isozyme 1, 50% inhibition at 0.011 mM, isozyme 2, 50% inhibition at 0.015 mM
DUP-697
Eicosa-5,8,11,14-tetraynoic acid
-
-
ellagic acid
-
at high concentration and in presence of cofactors inhibition, at low concentrations stimulation
etodalac
-
recombinant protein, 50% inhibition at 0.06-0.07 mM
ETYA
-
recombinant protein, 50% inhibition at 0.015-0.025 mM
fatty acid
-
of low molecular mass
fenclofenac
-
isozyme 1, 50% inhibition at 0.007 mM, isozyme 2, 50% inhibition at 0.004 mM
flosulide
-
selective for isozyme 2, 50% inhibition at 130 nM
Flufenamic acid
-
50% inhibition at 0.02 mM
flurbiprofen
Haptoglobin
-
-
-
Human serum
-
-
-
Ibuprofen
indomethacin
Ketoprofen
L-745
-
isozyme 1, 50% inhibition at 0.369 mM, isozyme 2, 50% inhibition at 0.002 mM
linoleic acid
-
Meclofenamic acid
Mefenamic acid
-
isozyme 1, 50% inhibition at 0.01 mM, isozyme 2, 50% inhibition at 0.0003 mM
meloxicam
-
isozyme 1, 50% inhibition at 0.005 mM, isozyme 2, 50% inhibition at 0.0004 mM
N-butyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
N-cyclohexyl-5-[(E)-[(2,5-dihydroxyphenyl)methylidene]amino]-2-hydroxybenzamide
-
N-cyclohexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
n-hexane extract of Angelicae dahuricae radix
42.4% inhibition of PGHS-2; 52.5% inhibition of PGHS-1
-
n-hexane extract of Angelicae sinsesis radix
61.5% inhibition of PGHS-2; 73.0% inhibition of PGHS-1
-
n-hexane extract of Atractylodis lanceae rhizoma
67.4% inhibition of PGHS-1; 68.3% inhibition of PGHS-2
-
n-hexane extract of Atractylodis macrocephalae rhizoma
46.1% inhibition of PGHS-1; 48.9% inhibition of PGHS-2
-
n-hexane extract of Cinnamomi ramulus
23.6% inhibition of PGHS-2; 46.6% inhibition of PGHS-1
-
n-hexane extract of Houttuyniae herba
43.4% inhibition of PGHS-2; 50.3% inhibition of PGHS-1
-
n-hexane extract of Notopterygii rhizoma seu radix
64.9% inhibition of PGHS-2; 69.6% inhibition of PGHS-1
-
n-hexane extract of Piperis sarmentosi herba
52.4% inhibition of PGHS-1; 65.0% inhibition of PGHS-2
-
n-hexane extract of Platycodi radix
48.7% inhibition of PGHS-1; 55.1% inhibition of PGHS-2
-
n-hexane extract of Zanthoxyli pericarpium
24.9% inhibition of PGHS-2; 48.5% inhibition of PGHS-1
-
n-hexane extract of Zingiberis rhizoma
77.5% inhibition of PGHS-2; 83.4% inhibition of PGHS-1
-
N-hexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide
-
N-[2-cyclohexyloxy-4-nitrophenyl]methanesulfonamide
naproxen
niflumic acid
-
isozyme 1, 50% inhibition at 0.016 mM, isozyme 2, 50% inhibition at 0.0001 mM
nimesulide
Non-steroidal anti-inflammatory agents
-
NS-398
NS398
-
-
O2
-
the cyclooxygenase reaction is inhibited by an excess of dissolved oxygen, 0.5 mM O2 causes twofold decrease in the initial rate and maximal yield
p-Aminophenol
-
-
PD-98059
MEK inhibitor, blocks specifically the activation of ERK1/2 and the PGHS-2 mRNA response to oxygen and glucose depivation, hence ERK is a mediator of PGHS-2 gene expression
peroxynitrite
-
-
piroxicam
propionic acid
-
-
quercetin
quercetin 3-O-glucoside
SB203580
inhibitor of p38, reduces the PGHS-2 response to oxygen and glucose depivation by approximately 50%
SC-560
SC58125
-
isozyme 1, 50% inhibition at 0.039 mM, isozyme 2, 50% inhibition at 0.0003 mM
sulindac sulfide
-
isozyme 1, 50% inhibition at 0.0004 mM, isozyme 2, 50% inhibition at 0.012 mM
suprofen
-
isozyme 1, 50% inhibition at 0.0005 mM, isozyme 2, 50% inhibition at 0.002mM
Tannic acid
-
at high concentration and in presence of cofactors inhibition, at low concentrations stimulation
U0126
MEK inhibitor, blocks specifically the activation of ERK1/2 and the PGHS-2 mRNA response to oxygen and glucose depivation, hence ERK is a mediator of PGHS-2 gene expression
valeryl salicylate
-
-
additional information
-