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Information on EC 5.3.99.5 - thromboxane-A synthase and Organism(s) Homo sapiens

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EC Tree
     5 Isomerases
         5.3 Intramolecular oxidoreductases
             5.3.99 Other intramolecular oxidoreductases
                5.3.99.5 thromboxane-A synthase
IUBMB Comments
A cytochrome P-450 heme-thiolate enzyme. Converts prostaglandin H2 into thromboxane A2.
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This record set is specific for:
Homo sapiens
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
thromboxane synthetase, thromboxane synthase, txa2 synthase, txas, thromboxane a2 synthetase, thromboxane a2 synthase, tbxas1, cyp5a1, thromboxane a synthase 1, txa synthase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
CYP5A1
-
-
Synthetase, thromboxane
-
-
-
-
Thromboxan synthetase
-
-
-
-
thromboxane A synthase 1
-
-
thromboxane A-synthase
-
-
thromboxane A2 synthase
-
-
thromboxane A2 synthase 1
-
-
Thromboxane A2 synthetase
-
-
-
-
Thromboxane synthetase
-
-
-
-
TXA synthase
-
-
-
-
TxA-synthase
-
-
TXA2 synthase
-
-
TxSI
-
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate = (5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
intramolecular oxidoreduction
-
-
-
-
isomerization
-
-
-
-
PATHWAY SOURCE
PATHWAYS
-
-, -, -, -
SYSTEMATIC NAME
IUBMB Comments
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate isomerase
A cytochrome P-450 heme-thiolate enzyme. Converts prostaglandin H2 into thromboxane A2.
CAS REGISTRY NUMBER
COMMENTARY hide
61276-89-9
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
show the reaction diagram
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
12-L-hydroxy-5,8,10-heptadecaotrienoic acid + malondialdehyde
show the reaction diagram
15(S)-Hydroxy-11alpha,9alpha-epoxymethano-5(Z),13(E)-prostadienoic acid
?
show the reaction diagram
-
in presence of iodosylbenzene
3 different hydroxylated derivatives of 15(S)-hydroxy-11alpha,9alpha-epoxymethano-5(Z),13(E)-prostadienoic acid
?
15-hydroperoxyeicosatetraenoic acid
13-hydroxy-14,15-epoxy-5,8,11-eicosatrienoic acid + 15-ketoeicosatetraenoic acid + 13-hydroxy-14,15-epoxy-5,8,11-eicosatrienoic acid + 15-ketoeicosatetraenoic acid
show the reaction diagram
-
-
13-hydroxy-14,15-epoxy-5,8,11-eicosatrienoic acid and 15-ketoeicosatetraenoic acid result from homolytic cleavage of the O-O bond, whereas 13-hydroxy-14,15-epoxy-5,8,11-eicosatrienoic acid + 15-ketoeicosatetraenoic acid results from heterolytic cleavage. About 60% of substrate is cleaved homolytically, and maximal velocity of homolytic cleavage is about 1.4fold faster than heterolytic cleavage
-
?
15-Ketoprostaglandin H2
?
show the reaction diagram
-
-
-
-
?
2 prostaglandin G2
15-hydroperoxythromboxane A2 + 12-hydroperoxy-5,8,10-heptadecatrienoic acid
show the reaction diagram
-
i.e. PGG2
the reaction products are transformed to thromboxane B2 and 12-hydroxy-5,8,10-heptadecatrienoic acid by SnCl2 reduction and to 12-keto-5,8,10-heptadecatrienoic acid and 15-ketothromboxane B2 by lead tetraacetate dehydration
?
2 prostaglandin G2 + H2O
15-hydroperoxythromboxane B2 + 12-hydroperoxy-5,8,10-heptadecatrienoic acid
show the reaction diagram
2 prostaglandin H3 + H2O
thromboxane B3 + 12(L)-hydroxy-5,8,10,14-heptadecatetraenoic acid + malondialdehyde
show the reaction diagram
-
-
the ratio of thromboxane to C17 hydroxyfatty acid formation is 1:1. Thromboxane A2 is fully transformed to thromboxane B2
?
8-Isoprostaglandin H2
8-cis-12-Hydroperoxy-5,8,10-heptadecatrienoic acid
show the reaction diagram
-
-
-
?
prostaglandin E2
thromboxane A2 + ?
show the reaction diagram
-
-
thromoboxane A2 is non-enzymatically converted to thromboxane B2, which is secretion is measured to analyze the enzyme activity
-
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
show the reaction diagram
prostaglandin H2
thromboxane A2
show the reaction diagram
-
-
-
-
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
show the reaction diagram
prostaglandin H2
thromboxane B2 + 12(S)-hydroxy-5,8,10-heptadecatrienoic acid
show the reaction diagram
-
-
-
-
?
Prostaglandin H3
Thromboxane B3 + DELTA14-12-hydroperoxy-5,8,10-heptadecatrienoic acid
show the reaction diagram
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
show the reaction diagram
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
12-L-hydroxy-5,8,10-heptadecaotrienoic acid + malondialdehyde
show the reaction diagram
prostaglandin H2
thromboxane A2
show the reaction diagram
-
-
-
-
?
prostaglandin H2
thromboxane B2 + 12(S)-hydroxy-5,8,10-heptadecatrienoic acid
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cytochrome P450
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
cyanide binding to substrate-free and substrate-bound CYP5A1 in a detergent-solubilized system and in nanodiscs, binding kinetics, overview
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+)-(E)-7-[4-[4-[[[2-(trans)-phenylcyclopropyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000085 mM, 50% inhibition
(+)-5-(2-imidazole-1-ethyloxy)-1-indan-carboxylic acid
-
trivial name camonagrel
(+/-)-6-(1-Imidazolylmethyl)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid hydrochloride hemihydrate
-
improvement of the renal function with the selective thromboxane A2 synthetase inhibitor
(-)-(E)-7-[4-[4-[[[2-(trans)-phenylcyclopropyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000059 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3,3-dimethyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000026 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-(1-adamantyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000003 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-(2-dimethylaminoethyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.0029 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-(2-methylpropyl)guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000025 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-(3-methylbutyl)guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000003 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-(3-pyridylmethyl)-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000032 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-benzylguanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000011 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-cyclohexyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000003 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-cyclopentyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000003 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-cyclopropyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.00038 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-isopropyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000024 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-methyl)guanidinophenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.00025 mM, 50% inhibition
(5E)-6-(3-(2-cyano-3-tert-butyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.000004 mM, 50% inhibition
(5E)-6-(4-(2-cyano-3-cyclopentyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.00018 mM, 50% inhibition
(5E)-6-(4-(2-cyano-3-cyclopropyl-guanidino)phenyl)-6-(3-pyridyl)hex-5-enoic acid
-
0.0039 mM, 50% inhibition
(5Z)-6-[(2S,4R)-4-(4-Chlorophenylsulphonylamino)-1-(3-pyridylmethyl)-2-pyrrolidinyl]-5-hexenoic acid hydrochloride
-
thromboxane A2 synthetase inhibitor/thromboxane A2-receptor antagonist
(E)-6-[4-(3-tert-butyl-2-cyanoguanidino)phenyl]-6-(3-pyridyl)hex-5-enoic acid
-
trivial name terbogrel
(E)-7-[4-[4-[(benzylamino)carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.000025 mM, 50% inhibition
(E)-7-[4-[4-[(pentylamino)carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridiyl)hept-6-enoic acid
-
0.000031 mM, 50% inhibition
(E)-7-[4-[4-[(phenylethylamino)carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000094 mM, 50% inhibition
(E)-7-[4-[4-[[(2-phenoxybutyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.000049 mM, 50% inhibition
(E)-7-[4-[4-[[(2-phenoxyethyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000026 mM, 50% inhibition
(E)-7-[4-[4-[[(2-phenoxypentyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.000049 mM, 50% inhibition
(E)-7-[4-[4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.000055 mM, 50% inhibition
(E)-7-[4-[4-[[(4-cyclopropylmethyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.000025 mM, 50% inhibition
(E)-7-[4-[4-[[3-(morpholinopropyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000051 mM, 50% inhibition
(E)-7-[4-[4-[[[2-(benzyloxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.000048 mM, 50% inhibition
(E)-7-[4-[4-[[[2-(cyclohexylmethoxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000037 mM, 50% inhibition
(E)-7-[4-[4-[[[2-(cyclohexyloxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000033 mM, 50% inhibition
(E)-7-[4-[4-[[[2-(tetrahydropyran-2-ylmethoxy)ethyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000063 mM, 50% inhibition
(E)-7-[4-[4-[[[3-(1-cyclohexylethoxy)propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000012 mM, 50% inhibition
(E)-7-[4-[4-[[[3-(4-methoxyphenyl)propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000027 mM, 50% inhibition
(E)-7-[4-[4-[[[3-(cyclohexyloxy)propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000042 mM, 50% inhibition
(E)-7-[4-[4-[[[3-[(cis)-4-methoxycyclohexyl]propyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000029 mM, 50% inhibition
(E)-7-[4-[4-[[[4-(cyclohexyloxy)butyl]amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid
-
0.0000049 mM, 50% inhibition
1(omega-Carboxylalkyl)imidazoles
-
very potent
-
1-(2-Isopropylphenyl)-imidazole
-
strong
1-Benzylimidazole
1-Decylimidazole
-
strong
1-Methyl imidazole
-
-
1-Nonylimidazole
-
strong
1-[2-(4,5,6,7-tetrahydrobenzo[b]furan-4-yl)ethyl]-1H-imidazole
-
0.001 mM, 50% inhibition
1-[2-(4,5,6,7-tetrahydrobenzo[b]furan-4-ylidene)ethyl]-1H-imidazole
-
E isomer, 0.00355 mM, 50% inhibition; Z isomer, 0.0041 mM, 50% inhibition
1-[2-(4,5,6,7-tetrahydrobenzo[b]thiophen-4-yl)ethyl]-1H-imidazole
-
0.0012 mM, 50% inhibition
1-[2-(4,5,6,7-tetrahydrobenzo[b]thiophen-4-ylidene)ethyl]-1H-imidazole
-
E isomer, 0.0017 mM, 50% inhibition; Z isomer, 0.0013 mM, 50% inhibition
1-[2-(benzo[b]thiophen-4-yl)ethyl]-1H-imidazole
-
0.0053 mM, 50% inhibition
12L-Hydroperoxy-5,8,10,14-eicosatetraenoic acid
-
0.1 mM, 50% inhibition
1H-Imidazol-1-ylalyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives
-
dual thromboxane synthase inhibitor/thromboxane receptor antagonists
2-Isopropyl-3-nicotinylindole
2-[4-Carboxy-8-(5-imidazol[1,5-a]pyridinyl)octanoyl]-2,3-dihydro-1H-1-isoindole-1-carboxylic acid
-
-
2-[[1-(Carboxymethyl)-2,3,4,5,-tetrahydro-2-oxo-1H-1-benzazepin-3-yl]amino]-6-[[5-[5-chloro-1-methyl-2-(3-pyridinyl)-1H-indol-3-yl]pentanoyl]amino]hexanoic acid
-
-
2-[[1-(Carboxymethyl)-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-3-yl]amino]6-[[5-[5-chloro-1-methyl-2-(3-pyridinyl)-1H-indol-3-yl]pentanoyl](2-hydroxyethyl)amino]hexanoic acid
-
-
2-[[1-(Carboxymethyl)-2,3,4,5-tetrahydro-2-oxo-1H-benzazepin-3-yl]amino]-6-[[1-[5-[5-chloro-1-methyl-2-(3-pyridinyl)1H-indol-3-yl]pentanoyl]piperidin-4-yl]amino]hexanoic acid
-
-
2-[[1-(Carboxymethyl)-2,3,4,5-tetrahydro-2-oxo-1H-benzazepin-3-yl]amino]-6-[[5-[5-chloro-1-methyl-2-(3-pyridinyl)1H-indol-3-yl]pentanoyl][2-(methylamino)ethyl]amino]hexanoic acid
-
-
2-[[1-(Carboxymethyl)-2,3,4,5-tetrahydro-2-oxo-1H-benzazepin-3-yl]amino]-7-[[2-[[5-[5-chloro-1-methyl-2-(3-pyridinyl)1H-indol-3-yl]pentanoyl]amino]ethyl]amino]heptanoic acid
-
-
3-Pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives
-
dual thromboxane synthase inhibitor/thromboxane receptor antagonists
4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)imidazole
-
trivial name SB203580
4-(Benzylamino)-2-(3'-pyridyl)quinazoline
-
-
4-(Benzylamino)-2-(imidazol-1-yl)-quinazoline
-
-
4-{2-[(4-chlorophenyl)methyl]-3-phenylpropanoyl}phenyl hydrogen benzylphosphonate
5-[2-(imidazol-1-yl)-ethyl]-5,6,7,8-tetrahydroquinoline
-
0.00063 mM, 50% inhibition
5-[2-(imidazol-1-yl)ethyl]-1,2,3,4-tetrahydronaphthalene
-
0.0034 mM, 50% inhibition
5-[2-(imidazol-1-yl)ethyl]-7,8-dihydroquinoline
-
0.00029 mM, 50% inhibition
5-[2-(imidazol-1-yl)ethyl]quinoline
-
0.0012 mM, 50% inhibition
5-[3-(imidazol-1-yl)-propyl]-5,6,7,8-tetrahydroquinoline
-
0.0023 mM, 50% inhibition
5-[3-(imidazol-1-yl)-propyl]-7,8-dihydroquinoline
-
0.00068 mM, 50% inhibition
5-[imidazol-1-yl-methyl]-5,6,7,8-tetrahydroquinoline
-
0.002 mM, 50% inhibition
5-[imidazol-1-yl-methyl]-7,8-dihydroquinoline
-
0.0015 mM, 50% inhibition
5E-6-(3-cyanoguanidino)phenyl-6-(3-pyridyl)hex-5-enoic acid
-
0.00043 mM, 50% inhibition
7-[(imidazol-1-yl)methyl]isoquinoline
-
0.0054 mM, 50% inhibition
8-[2-(3-Pyridinyl)-1H-indol-1-yl]octanoic acid 1-(carboxymethyl)-3-[(1-carboxy-3-phenylpropyl)amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-5-yl ester
-
-
9,11(Epoxymethano) prostanoic acid
-
-
9,11-Azo-15-hydroxyprosta-5,13-dienoic acid
-
-
9,11-Azoprosta-5,13 dienoic acid
-
-
9,11-Azoprosta-5,13-dienoic acid
-
-
9,11-Epoxymethano-15-hydroxy-prosta-5,13-dienoic acid
-
-
9alpha,11alpha-Azo-15-(S)Hydroxyprosta-5(cis)-13(trans)-dienoic acid
-
-
9alpha,11alpha-Methanoepoxy-15(S)-hydroxyprosta-5(cis)-13(trans)-dienoic acid
Benzydamine
-
-
BM 567
-
i.e. 2-(cyclohexylamino)-5-nitro-N-[(pentylamino)carbonyl]-benzenesulfonamide, 10 microM, a specific inhibitor for thromboxane synthase, decrease the acitivity 2.1fold before diosgenin treatment
carboxyheptyl imidazole
-
10 microM, concentration of thromboxane B2 in culture supernatants: reduction of thromboxane B2 in prostate cancer cells PC-3 from 1295 pg/ml to 685 pg/ml, reduction of thromboxane B2 in erythroleukemia cells HEL from 580 pg/ml to 292 pg/ml. In PC-3 cell lysates reduction of thromboxane B2 level by 86%
CGS 13080
-
-
Chlorella powder
-
the potent inhibition of cyclooxygenase-2 and thromboxane synthase contribute to the purported anti-inflmammatory and anti-thrombotic effect of Chlorella. This might be exploited for the prevention or treatment of several serious pathologies, including inflammatory diseases, immune and cancer
-
clotrimazole
-
as a heme ligand, molecular dynamics simulations of clotrimazole and 2-p-toluidinylnaphthalene-6-sulfonic acid-docking enzyme
CV4151
-
0.0000049 mM, 50% inhibition
-
dazoxiben
furegrelate
imidazole
indomethacin
-
0.000017 mM, 50% inhibition of PGE2 formation, 0.000013 mM, 50% inhibition of 12-HHT formation
linoleic acid
-
significant inhibition of cyclooxygenase/thromboxane synthase activity, determined by TXB2 production with an ELISA-based assay
linolelaidic acid
-
significant inhibition of cyclooxygenase/thromboxane synthase activity, determined by TXB2 production with an ELISA-based assay
N-isopropyl-N'-[(2-(3'-methylphenylamino)-5-nitrobenzene)sulfonyl]urea
-
-
N-isopropyl-N'-[2-(3'-methylphenylamino)-5-nitrobenzenesulfonyl]urea
-
0.001 mM, 95% inhibition
N-pentyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea
-
-
N-tert-butyl-N'-(2-cyclohexylamino-5-nitrobenzenesulfonyl)urea
-
-
N-tert-butyl-N'-[(2-(4'-methylphenylamino)-5-nitrobenzene)sulfonyl]urea
-
-
N-tert-butyl-N'-[(2-cyclohexylamino-5-nitrobenzene)sulfonyl]urea
-
-
NO
-
irreversible in a concentration-dependent manner
OKY 1581
-
-
ozagrel
prostaglandin H2
-
suicide inactivation
R68070
-
0.0000015 mM, 50% inhibition
ridogrel
-
0.000004 mM, 50% inhibition
samixogrel
-
0.000004 mM, 50% inhibition
Sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate
-
immobilized enzyme
Sodium 5-(3'pyridinylmethyl)benzofuran-2-carboxylate
-
-
Sodium p-benzyl-4-[1-oxo-2-(4-chlorobenzyl)-3-phenyl propyl]phenyl phosphonate
-
-
thromboxane A2
-
the production of thromboxane A2 by the enzyme is self-limiting, the enzyme is inactivated during the reaction
UK 37,248
-
-
[3-[[Hydroxy[4-[3-methyl-2-(3-pyridinyl)indol-1-yl]butyl]phosphinyl]oxy]2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepin-1-yl]acetic acid
-
-
[4-[3-Methyl-2-(3-pyridinyl)-1H-indol-1-yl]butyl]phosphonic acid
-
-
[4-[3-Methyl-2-(3-pyridinyl)-1H-indol-1-yl]butyl]phosphonic acid monoethyl ester
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
diosgenin
-
10 microM increases cyclooxygenase-2 and thromboxane synthase expression and activities in HEL cells, 3.5fold at 96 h and 4.5fold at 144 h
phosphatidylcholine
-
-
phosphatidylethanolamine
-
-
phosphatidylserine
-
-
additional information
-
the catalytic activities of the binary phosphatidylethanolamine/phosphatidylcholine and phosphatidylserine/phosphatidylcholine and ternary phosphatidylcholine/phosphatidylethanolamine/phosphatidylserine are similar and increase relative to the unary phosphatidylcholine system
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.02 - 0.022
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
0.071 - 0.087
15-hydroperoxyeicosatetraenoic acid
0.023
prostaglandin G2
-
prostaglandin H3
0.024
Prostaglandin H1
-
-
0.004 - 0.022
prostaglandin H2
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.017
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
recombinant TXAS
28.2
prostaglandin G2
-
-
26.7 - 27.1
prostaglandin H2
20.4 - 59.4
prostaglandin H3
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.1
12L-Hydroperoxy-5,8,10,14-eicosatetraenoic acid
-
-
additional information
Chlorella powder
-
3.32 microg/ml, tested in an in vitro assay system
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.255
-
-
0.259
-
-
1.15
-
-
2.95
-
recombinant TXAS
24.1
-
-
additional information
-
accumulation of thromboxane B2 in the culture supernatants of prostate cancer cells PC-3 1295 pg/ml compared with 580 pg/ml in supernatants from erythroleukemia cells HEL and 30 pg/ml from prostate cancer cells DU145. In cell lysates from PC-3 cells 22.5 pg thromboxane B2 per million cells, in cell lysates from prostate cancer cells DU145 0.475 pg per million cells
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
broad
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5 - 8.5
-
very little pH-dependence between pH 5-8.5, above pH 9.0 the reaction is significantly depressed
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
20 - 37
-
activity at 37°C is not significantly higher than at 20°C
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
TXAS is expressed in the atherosclerotic lesion, associated with increased inflammatory cells, in particular M2 polarized macrophages
Manually annotated by BRENDA team
-
low activity
Manually annotated by BRENDA team
-
bladder cancer cell lines T24 and TCC-SUP
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
colorectal carcinoma
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
low activity
Manually annotated by BRENDA team
-
low activity
Manually annotated by BRENDA team
-
low activity
Manually annotated by BRENDA team
-
human erythroleukemia cells
Manually annotated by BRENDA team
-
low activity
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
a squamous cell carcinoma cell line
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
low activity
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
intrinsic protein
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
CP2S1_HUMAN
504
2
55817
Swiss-Prot
Secretory Pathway (Reliability: 1)
THAS_HUMAN
533
0
60518
Swiss-Prot
Secretory Pathway (Reliability: 4)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
58000
58800
-
x * 58800, SDS-PAGE
60000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
-
x * 58000, SDS-PAGE
additional information
-
enzyme structure molecular homology modeling using the crystal structure of human microsomal CYP3A4, PDB entry 1TQN, as the template structure
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A408L
-
42% of wild-type activity
A415V
-
82% of wild-type activity
C480H
-
no activity
C480S
-
no activity
C480Y
-
no activity
E134D
-
35% of wild-type activity
E135D
-
123% of wild-type activity
E414D
-
39% of wild-type activity
F409Y
-
42% of wild-type activity
F411Y
-
38% of wild-type activity
L488P
-
in alpha-helix, indroducing a coil in the secondary structure, crucial for enzyme activity
L83P
-
in beta-sheet, indroducing a coil in the secondary structure, crucial for enzyme activity
N110I
-
no activity
Q482W
-
changing an aliphatic amino acid with low steric hindrance into an aromatic amino acid with high steric hindrance in the vicinitx of the catalytic site, modifying the interaction of the enzyme-substarte complex, crucial for enzyme activity
R137A
-
2% of wild-type activity
R137K
-
5% of wild-type activity
R410G
-
46% of wild-type activity
R413K
-
1% of wild-type activity
R431E
-
decreased enzyme activity, 1% residual activity
R431K
-
decreased enzyme activity, 1% residual activity
R478A
-
no activity
T412S
-
41% of wild-type activity
V136A
-
69% of wild-type activity
W133F
W203F
-
site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme
W31F
-
site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme
W31F/W65F/W133F/W203F/W466F
-
site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme
W466F
-
site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme
W65F
-
site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
4.5
-
unstable below
3200
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
immobilized enzyme is inactivated at pH 3.0
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
intrinsic membrane protein, detergent treatment is necessary
-
one-step immunoaffinity purification
-
partial
-
recombinant C-terminally His-tagged modified enzyme from Escherichia coli strain DH5alpha by nickel affinity chromatography
-
recombinant His-tagged TXAS
-
recombinant TXAS
-
recombinant TXAS, Ni-NTA, column, DEAE-column, Octyl-column
-
recombinant wild-type and mutant C-terminally His4-tagged modified enzyme from Escherichia coli strain BL21/(DE3)pLys by nickel affinity and hydroxyapatite chromatography
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
characterization of the gene TBXAX1 encoding thromboxane synthase
-
expression in Escherichia coli
-
expression of C-terminally His-tagged enzyme replacing the first 29 amino acid residues in the N-terminal transmembrane domain with the hydrophilic sequence MAKKTSS for TXAS cDNA in Escherichia coli strain DH5alpha
-
expression of wild-type and mutant C-terminally His4-tagged enzyme replacing the first 28 amino acid residues in the N-terminal transmembrane domain with the hydrophilic sequence MAKKTSS for TXAS cDNA in Escherichia coli strain BL21/(DE3)pLys
-
overexpression in Escherichia coli
-
stable overexpression of thromboxane synthase in SKMES-1 cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
an overall increase in TXS expression is observed in tumor tissues relative to normal, increased TXS expression at mRNA level is reported in renal cell carcinoma, breast carcinoma, prostate cancer and uterine cancer when compared with matched normal tissues
-
inhibition of platelet TXA2 generation (acetylsalicylic acid), lowering of cholesterol (statins), inhibition of platelet aggregation (clopidogrel), or promoting vasodilatation (dipyridamole) has no effect on TXAS mRNA expression levels
-
smokers tend to express more TxAS than nonsmokers
-
TNF-alpha, U46619 and 8-isoprostane F2alpha and hypoxia all augment TXAS protein expression. NADPH oxidase-1 (but not NADPH oxidase-4) gene silencing, as well as picotamide and iloprost inhibit the increase in TXAS expression and activity
-
TXAS increases in atherosclerotic lesions of patients with recent symptoms of thrombotic events
-
TXSA is upregulated in human glial tumors
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
pharmacology
-
development of a screening assay for the in vitro evaluation of thromboxane A2 synthase inhibitors. Inhibitors of thromboxane synthase are regarded as potentially useful agents in the treatment of cardiovascular diseases and in the prevention of tumor cell metastases
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Hecker, M.; Haurand, M.; Ullrich, V.; Diczfalusy, U.; Hammarstrm, S.
Products, kinetics, and substrate specificity of homogeneous thromboxane synthase from human platelets: development of a novel enzyme assay
Arch. Biochem. Biophys.
254
124-135
1987
Homo sapiens
Manually annotated by BRENDA team
Hall, E.R.; Tuan, W.; Venton, D.L.
Production of platelet thromboxane A2 inactivates purified human platelet thromboxane synthase
Biochem. J.
233
637-641
1986
Homo sapiens
Manually annotated by BRENDA team
Haurand, M.; Ullrich, V.
Isolation and characterization of thromboxane synthase from human platelets as a cytochrome P-450 enzyme
J. Biol. Chem.
260
15059-15067
1985
Homo sapiens
Manually annotated by BRENDA team
Hecker, M.; Baader, W.J.; Weber, P.; Ullrich, V.
Thromboxane synthase catalyses hydroxylations of prostaglandin H2 analogs in the presence of iodosylbenzene
Eur. J. Biochem.
169
563-569
1987
Homo sapiens
Manually annotated by BRENDA team
Gorman, R.R.
Biology and biochemistry of thromboxane synthetase inhibitors
Adv. Prostaglandin Thromboxane Leukot. Res.
11
235-240
1983
Homo sapiens
Manually annotated by BRENDA team
Ullrich, V.; Haurand, M.
Thromboxane synthase as a cytochrome P450 enzyme
Adv. Prostaglandin Thromboxane Leukot. Res.
11
105-110
1983
Homo sapiens
Manually annotated by BRENDA team
Hammarstroem, S.
Enzymatic synthesis of 15-hydroperoxythromboxane A2 and 12-hydroperoxy-5,8,10-heptadecatrienoic acid
J. Biol. Chem.
255
518-521
1980
Homo sapiens
Manually annotated by BRENDA team
Hammarstroem, S.; Diczfalusy, U.
Inhibition and properties of thromboxane synthetase
Adv. Inflamm. Res.
1
431-438
1979
Homo sapiens
-
Manually annotated by BRENDA team
Tai, H.H.; Yuan, B.
On the inhibitory potency of imidazole and its derivatives on thromboxane synthetase
Biochem. Biophys. Res. Commun.
80
236-242
1978
Homo sapiens
Manually annotated by BRENDA team
Diczfalusy, U.; Falardeau, P.; Hammarstrm, S.
Conversion of prostaglandin endoperoxides to C17-hydroxy acids catalyzed by human platelet thromboxane synthase
FEBS Lett.
84
271-274
1977
Homo sapiens
Manually annotated by BRENDA team
Diczfalusy, U.; Hammarstrm, S.
Inhibitors of thromboxane synthase in human platelets
FEBS Lett.
82
107-110
1977
Homo sapiens
Manually annotated by BRENDA team
Hammarstroem, S.; Falardeau, P.
Resolution of prostaglandin synthase and thromboxane synthase of human platelets
Proc. Natl. Acad. Sci. USA
74
3691-3695
1977
Homo sapiens
Manually annotated by BRENDA team
Sun, F.F.
Biosynthesis of thromboxanes in human platelets. I. Characterization and assay of thromboxane synthetase
Biochem. Biophys. Res. Commun.
74
1432-1440
1977
Homo sapiens
Manually annotated by BRENDA team
Ullrich, V.; Nusing, R.
Thromboxane synthase. From isolation to function
Stroke
21
IV134-IV138
1994
Homo sapiens
Manually annotated by BRENDA team
Umemura, K.; Nakashima, M.; Saruta, T.
Thromboxane A2 synthetase inhibition suppresses cough induced by angiotensin converting enzyme inhibitors
Life Sci.
60
1583-1588
1997
Homo sapiens
Manually annotated by BRENDA team
Ledergerber, D.; Hartmann, R.W.
Development of a screening assay for the in vitro evaluation of the thromboxane A2 synthase inhibitors
J. Enzyme Inhib.
9
253-261
1995
Homo sapiens
Manually annotated by BRENDA team
Yoshida, T.; Kameda, H.; Masashi, A.; Homma, M.; Ikeda, Y.
Improvement of renal function with selective thromboxane A2 synthetase inhibitor, DP-1904 in Lupus nephritis
Adv. Exp. Med. Biol.
433
113-117
1997
Homo sapiens
Manually annotated by BRENDA team
Miyata, A.; Yokoyama, C.; Ihara, H.; Bandoh, S.; Takeda, O.; Takahashi, E.I.; Tanabe, T.
Characterization of the human gene (TBXAS1) encoding thromboxane synthase
Eur. J. Biochem.
224
273-279
1994
Homo sapiens
Manually annotated by BRENDA team
Lee, S.J.; Konishi, Y.; Yu, D.T.; Miskowski, T.A.; Riviello, C.M.; Macina, O.T.; Frierson, M.R.; Kondo, K.; Sugitani, M.; Suvar, J.C.; Blazejewski, K.M.
Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities
J. Med. Chem.
38
3547-3557
1995
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Dickinson, R.P.; Dack, K.N.; Long, C.J.; Steele, J.
Thromboxane modulating agents. 3. 1H-Imidazol-1-ylalkyl- and 3-pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists
J. Med. Chem.
40
3442-3452
1997
Homo sapiens
Manually annotated by BRENDA team
Ksander, G.M.; Erion, M.; Yuan, A.M.; Diefenbacher, C.G.; El-Chebabi, L.; Cote, D.; Levens, N.
Dual angiotensin converting enzyme/thromboxane synthase inhibitors
J. Med. Chem.
37
1823-1832
1994
Homo sapiens
Manually annotated by BRENDA team
Ruan, K.H.; Milfeld, K.; Kulmacz, R.J.; Wu, K.K.
Comparison of the construction of a 3-D model for human thromboxane synthase using P450cam and BM-3 as templates: implications for the substrate binding pocket
Protein Eng.
7
1345-1351
1994
Homo sapiens
Manually annotated by BRENDA team
Nusing, R.; Schneider-Voss, S.; Ullrich, V.
Immunoaffinity purification of human thromboxane synthase
Arch. Biochem. Biophys.
280
325-330
1990
Homo sapiens
Manually annotated by BRENDA team
Orlandi, M.; Bartolini, G.; Belletti, B.; Spisni, E.; Tomasi, V.
Thromboxane A2 synthase activity in platelet free human monocytes
Biochim. Biophys. Acta
1215
285-290
1994
Homo sapiens
Manually annotated by BRENDA team
Uematsu, T.; Kosuge, K.; Umemura, M.; Nakano, M.; Terakawa, M.; Nakashima, M.
Pharmacokinetic and pharmacodynamic properties of FK070(KDI-792), a novel thromboxane receptor antagonist/thromboxane synthetase inhibitor, after single and multiple oral administrations to healthy volunteers
J. Pharm. Pharmacol.
48
380-385
1996
Homo sapiens
Manually annotated by BRENDA team
Jones, D.A.; Fitzpatrick, F.A.
"Suicide" inactivation of thromboxane A2 synthase. Characteristics of mechanism-based inactivation with isolated enzyme and intact platelets
J. Biol. Chem.
265
20166-20171
1990
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Haurand, M.; Ullrich, V.
Thromboxane synthase and prostacyclin synthase as P-450 enzymes with regard to the mechanisms of PGI2 and TXA2 biosynthesis
Front. Biotransform.
6
183-199
1992
Homo sapiens, Sus scrofa
-
Manually annotated by BRENDA team
Wade, M.L.; Fitzpatrick, F.A.
Nitric oxide modulates the activity of the hemoproteins prostaglandin I2 synthase and thromboxane A2 synthase
Arch. Biochem. Biophys.
347
174-180
1997
Homo sapiens
Manually annotated by BRENDA team
Michaux, C.; Norberg, B.; Dogne, J.M.; Durant, F.; Masereel, B.; Delarge, J.; Wouters, J.
Terbogrel, a dual-acting agent for thromboxane receptor antagonism and thromboxane synthase inhibition
Acta Crystallogr. Sect. C
56
1265-1266
2000
Homo sapiens
-
Manually annotated by BRENDA team
Michaux, C.; Dogne, J.M.; Norberg, B.; Durant, F.; Masereel, B.
N-tert-butyl-N'-(2-cyclohexylamino-5-nitrobenzenesulfonyl)urea, BM531, a dual-acting agent for thromboxane receptor antagonism and thromboxane synthase inhibition
Acta Crystallogr. Sect. C
58
o621-623
2002
Homo sapiens
Manually annotated by BRENDA team
Hsu, P.Y.; Tsai, A.L.; Wang, L.H.
Identification of thromboxane synthase amino acid residues involved in heme-propionate binding
Arch. Biochem. Biophys.
383
119-127
2000
Homo sapiens
Manually annotated by BRENDA team
Chen, Z.; Wang, L.H.; Schelvis, J.P.
Resonance Raman investigation of the interaction of thromboxane synthase with substrate analogues
Biochemistry
42
2542-2551
2003
Homo sapiens
Manually annotated by BRENDA team
Michaux, C.; Dogne, J.M.; Rolin, S.; Masereel, B.; Wouters, J.; Durant, F.
A pharmacophore model for sulphonyl-urea (-cyanoguanidine) compounds with dual action, thromboxane receptor antagonists and thromboxane synthase inhibitors
Eur. J. Med. Chem.
38
703-710
2003
Homo sapiens
Manually annotated by BRENDA team
Borsch-Haubold, A.G.; Pasquet, S.; Watson, S.P.
Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. SB 203580 also inhibits thromboxane synthase
J. Biol. Chem.
273
28766-28772
1998
Homo sapiens
Manually annotated by BRENDA team
Hsu, P.Y.; Tsai, A.L.; Kulmacz, R.J.; Wang, L.H.
Expression, purification, and spectroscopic characterization of human thromboxane synthase
J. Biol. Chem.
274
762-769
1999
Homo sapiens
Manually annotated by BRENDA team
Wang, L.H.; Tsai, A.L.; Hsu, P.Y.
Substrate binding is the rate-limiting step in thromboxane synthase catalysis
J. Biol. Chem.
276
14737-14743
2001
Homo sapiens
Manually annotated by BRENDA team
Takeuchi, K.; Kohn, T.J.; True, T.A.; Mais, D.E.; Wikel, J.H.; Utterback, B.G.; Wyss, V.L.; Jakubowski, J.A.
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounds
J. Med. Chem.
41
5362-5374
1998
Homo sapiens
Manually annotated by BRENDA team
Soyka, R.; Guth, B.D.; Weisenberger, H.M.; Luger, P.; Muller, T.H.
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors
J. Med. Chem.
42
1235-1249
1999
Homo sapiens
Manually annotated by BRENDA team
Jacobs, C.; Frotscher, M.; Dannhardt, G.; Hartmann, R.W.
1-Imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase
J. Med. Chem.
43
1841-1851
2000
Homo sapiens
Manually annotated by BRENDA team
Dogne, J.M.; Wouters, J.; Rolin, S.; Michaux, C.; Pochet, L.; Durant, F.; Delarge, J.; Masereel, B.
Design, synthesis and biological evaluation of a sulfonylcyanoguanidine as thromboxane A2 receptor antagonist and thromboxane synthase inhibitor
J. Pharm. Pharmacol.
53
669-680
2001
Homo sapiens
Manually annotated by BRENDA team
Villalobos, M.A.; De La Cruz, J.P.; Escalante, R.; Arrebola, M.M.; Guerrero, A.; Sanchez de la Cuesta, F.
Effects of camonagrel, a selective inhibitor of platelet thromboxane synthase, on the platelet-subendothelium interaction
Pharmacology
69
44-50
2003
Homo sapiens
Manually annotated by BRENDA team
Nie, D.; Che, M.; Zacharek, A.; Qiao, Y.; Li, L.; Li, X.; Lamberti, M.; Tang, K.; Cai, Y.; Guo, Y.; Grignon, D.; Honn, K.V.
Differential expression of thromboxane synthase in prostate carcinoma: role in tumor cell motility
Am. J. Pathol.
164
429-439
2004
Homo sapiens
Manually annotated by BRENDA team
Moussa, O.; Yordy, J.S.; Abol-Enein, H.; Sinha, D.; Bissada, N.K.; Halushka, P.V.; Ghoneim, M.A.; Watson, D.K.
Prognostic and functional significance of thromboxane synthase gene overexpression in invasive bladder cancer
Cancer Res.
65
11581-11587
2005
Homo sapiens
Manually annotated by BRENDA team
Stachowska, E.; Dolegowska, B.; Olszewska, M.; Gutowska, I.; Chlubek, D.
Isomers of trans fatty acids modify the activity of platelet 12-P lipoxygenase and cyclooxygenase/thromboxane synthase
Nutrition
20
570-571
2004
Homo sapiens
Manually annotated by BRENDA team
Yeh, H.C.; Tsai, A.L.; Wang, L.H.
Reaction mechanisms of 15-hydroperoxyeicosatetraenoic acid catalyzed by human prostacyclin and thromboxane synthases
Arch. Biochem. Biophys.
461
159-168
2007
Homo sapiens
Manually annotated by BRENDA team
Sakai, H.; Suzuki, T.; Takahashi, Y.; Ukai, M.; Tauchi, K.; Fujii, T.; Horikawa, N.; Minamimura, T.; Tabuchi, Y.; Morii, M.; Tsukada, K.; Takeguchi, N.
Upregulation of thromboxane synthase in human colorectal carcinoma and the cancer cell proliferation by thromboxane A2
FEBS Lett.
580
3368-3374
2006
Homo sapiens
Manually annotated by BRENDA team
Cailleteau, C.; Liagre, B.; Battu, S.; Jayat-Vignoles, C.; Beneytout, J.L.
Increased cyclooxygenase-2 and thromboxane synthase expression is implicated in diosgenin-induced megakaryocytic differentiation in human erythroleukemia cells
Anal. Biochem.
380
26-34
2008
Homo sapiens
Manually annotated by BRENDA team
Cheng, F.C.; Feng, J.J.; Chen, K.H.; Imanishi, H.; Fujishima, M.; Takekoshi, H.; Naoki, Y.; Shimoda, M.
Chlorella powder inhibits the activities of peptidase cathepsin S, PLA2, cyclooxygenase-2, thromboxane synthase, tyrosine phosphatases, tumor necrosis factor-alpha converting enzyme, calpain and kinases
Int. J. Food Sci. Nutr.
60 Suppl 1
89-98
2008
Homo sapiens
Manually annotated by BRENDA team
Genevieve, D.; Proulle, V.; Isidor, B.; Bellais, S.; Serre, V.; Djouadi, F.; Picard, C.; Vignon-Savoye, C.; Bader-Meunier, B.; Blanche, S.; de Vernejoul, M.C.; Legeai-Mallet, L.; Fischer, A.M.; Le Merrer, M.; Dreyfus, M.; Gaussem, P.; Munnich, A.; Cormier-Daire, V.
Thromboxane synthase mutations in an increased bone density disorder (Ghosal syndrome)
Nat. Genet.
40
284-286
2008
Homo sapiens
Manually annotated by BRENDA team
Vila, L.; Martinez-Perez, A.; Camacho, M.; Buil, A.; Alcolea, S.; Pujol-Moix, N.; Soler, M.; Anton, R.; Souto, J.C.; Fontcuberta, J.; Soria, J.M.
Heritability of thromboxane A2 and prostaglandin E2 biosynthetic machinery in a Spanish population
Arterioscler. Thromb. Vasc. Biol.
30
128-134
2010
Homo sapiens
Manually annotated by BRENDA team
Cathcart, M.C.; Reynolds, J.V.; OByrne, K.J.; Pidgeon, G.P.
The role of prostacyclin synthase and thromboxane synthase signaling in the development and progression of cancer
Biochim. Biophys. Acta
1805
153-166
2010
Homo sapiens
Manually annotated by BRENDA team
Park, S.A.; Park, B.L.; Park, J.H.; Lee, T.K.; Sung, K.B.; Lee, Y.K.; Chang, H.S.; Park, C.S.; Shin, H.D.
Association of polymorphisms in thromboxane A2 receptor and thromboxane A synthase 1 with cerebral infarction in a Korean population
BMB Rep.
42
200-205
2009
Homo sapiens
Manually annotated by BRENDA team
Leung, K.C.; Hsin, M.K.; Chan, J.S.; Yip, J.H.; Li, M.; Leung, B.C.; Mok, T.S.; Warner, T.D.; Underwood, M.J.; Chen, G.G.
Inhibition of thromboxane synthase induces lung cancer cell death via increasing the nuclear p27
Exp. Cell Res.
315
2974-2981
2009
Homo sapiens
Manually annotated by BRENDA team
Gabrielsen, A.; Qiu, H.; Baeck, M.; Hamberg, M.; Hemdahl, A.L.; Agardh, H.; Folkersen, L.; Swedenborg, J.; Hedin, U.; Paulsson-Berne, G.; Haeggstroem, J.Z.; Hansson, G.K.
Thromboxane synthase expression and thromboxane A2 production in the atherosclerotic lesion
J. Mol. Med.
88
795-806
2010
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Schauff, A.; Kim, E.; Leppert, J.; Nadrowitz, R.; Wuestenberg, R.; Brockmann, M.; Giese, A.
Inhibition of invasion-associated thromboxane synthase sensitizes experimental gliomas to gamma-radiation
J. Neurooncol.
91
241-249
2009
Homo sapiens
Manually annotated by BRENDA team
Schmidt, N.O.; Ziu, M.; Cargioli, T.; Westphal, M.; Giese, A.; Black, P.M.; Carroll, R.S.
Inhibition of thromboxane synthase activity improves glioblastoma response to alkylation chemotherapy
Transl. Oncol.
3
43-49
2010
Homo sapiens
Manually annotated by BRENDA team
Muzaffar, S.; Shukla, N.; Massey, Y.; Angelini, G.D.; Jeremy, J.Y.
NADPH oxidase 1 mediates upregulation of thromboxane A2 synthase in human vascular smooth muscle cells: inhibition with iloprost
Eur. J. Pharmacol.
658
187-192
2011
Homo sapiens
Manually annotated by BRENDA team
Chao, W.C.; Lu, J.F.; Wang, J.S.; Yang, H.C.; Pan, T.A.; Chou, S.C.; Wang, L.H.; Chou, P.T.
Probing ligand binding to thromboxane synthase
Biochemistry
52
1113-1121
2013
Homo sapiens
Manually annotated by BRENDA team
Das, A.; Varma, S.S.; Mularczyk, C.; Meling, D.D.
Functional investigations of thromboxane synthase (CYP5A1) in lipid bilayers of nanodiscs
ChemBioChem
15
892-899
2014
Homo sapiens
Manually annotated by BRENDA team
Cathcart, M.C.; Gately, K.; Cummins, R.; Kay, E.; OByrne, K.J.; Pidgeon, G.P.
Examination of thromboxane synthase as a prognostic factor and therapeutic target in non-small cell lung cancer
Mol. Cancer
10
25
2011
Homo sapiens
Manually annotated by BRENDA team
Sathler, P.; Santana, M.; Loureno, A.; Rodrigues, C.; Abreu, P.; Cabral, L.; Castro, H.
Human thromboxane synthase Comparative modeling and docking evaluation with the competitive inhibitors dazoxiben and ozagrel
J. Enzyme Inhib. Med. Chem.
29
527-531
2014
Homo sapiens
Manually annotated by BRENDA team