Any feedback?
No. of entries
Information on EC 5.3.99.5 - thromboxane-A synthase
for references in articles please use BRENDA:EC5.3.99.5
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
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.
The enzyme appears in viruses and cellular organisms
- 5.3.99.5
- platelet
- prostaglandin
-
arachidonic
- artery
-
cyclooxygenase
- prostacyclin
- indomethacin
- endothelial
-
endoperoxide
- pulmonary
-
prostanoids
- aspirin
- dazoxiben
- coronary
-
eicosanoids
-
vasoconstrictor
-
leukotriene
- imidazole
- hypertension
- thrombosis
- aorta
-
hemodynamic
-
antiplatelet
-
6-keto-pgf1
- cox-2
-
5-lipoxygenase
-
6-keto-prostaglandin
-
vasodilator
-
antithrombotic
- ozagrel
-
endothelium-dependent
- thrombus
- paf
-
endothelium-derived
-
bronchoconstriction
-
6-keto
-
platelet-rich
-
constrictor
-
collagen-induced
-
aa-induced
- analysis
- medicine
-
aspirin-treated
- pharmacology
- ticlopidine
-
reocclusion
- meclofenamate
-
f1alpha
- pgg2
-
iloprost
-
antiaggregatory
-
14c-arachidonic
-
proaggregatory
Reaction Schemes
showSynonyms
thromboxane synthetase, thromboxane synthase, txa2 synthase, txas, thromboxane a2 synthetase, thromboxane a2 synthase, tbxas1, cyp5a1, thromboxane a synthase 1, txa synthase, more
topPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
CYP5A1
Synthetase, thromboxane
-
-
-
-
Thromboxan synthetase
-
-
-
-
thromboxane A2 synthase
Thromboxane A2 synthetase
-
-
-
-
thromboxane synthase
Thromboxane synthetase
-
-
-
-
TXA synthase
-
-
-
-
TXA2 synthase
TXAS
TXS
thromboxane synthase
-
-
TXAS
-
-
-
-
TXAS
-
-
TXS
-
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
REACTION
REACTION DIAGRAM
COMMENTARY
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
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate = (5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
mechanism
-
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate = (5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
role of the thiolate ligand in the oxygen activation mechanism
-
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate = (5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
intramolecular oxidoreduction
-
-
-
-
isomerization
-
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PATHWAY SOURCE
PATHWAYS
BRENDA
MetaCyc
arachidonate metabolites biosynthesis, C20 prostanoid biosynthesis, di-homo-gamma-linolenate metabolites biosynthesis, icosapentaenoate metabolites biosynthesis
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
CAS REGISTRY NUMBER
COMMENTARY
61276-89-9
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9a,11a-epoxy-15-hydroxythromboxa-5,13-dienoate
-
Substrates: -
Products: i.e. TXA2
Products: i.e. TXA2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
12-L-hydroxy-5,8,10-heptadecaotrienoic acid + malondialdehyde
-
Substrates: -
Products: ratio of TXA2/heptadecatrienoic acid/malondialdehyde, 1/1/1
Products: ratio of TXA2/heptadecatrienoic acid/malondialdehyde, 1/1/1
?
15(S)-Hydroxy-11alpha,9alpha-epoxymethano-5(Z),13(E)-prostadienoic acid
?
-
Substrates: in presence of iodosylbenzene
Products: 3 different hydroxylated derivatives of 15(S)-hydroxy-11alpha,9alpha-epoxymethano-5(Z),13(E)-prostadienoic acid
Products: 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
-
Substrates: -
Products: 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
Products: 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-hydroxy-9alpha,11alpha-peroxiprosta-5,13-dienoic acid
?
-
Substrates: -
Products: -
Products: -
?
2 prostaglandin G2
15-hydroperoxythromboxane A2 + 12-hydroperoxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGG2
Products: 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
Products: 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
-
Substrates: i.e. PGG2
Products: -
Products: -
?
2 prostaglandin H3 + H2O
thromboxane B3 + 12(L)-hydroxy-5,8,10,14-heptadecatetraenoic acid + malondialdehyde
-
Substrates: -
Products: the ratio of thromboxane to C17 hydroxyfatty acid formation is 1:1. Thromboxane A2 is fully transformed to thromboxane B2
Products: 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
-
Substrates: -
Products: -
Products: -
?
prostaglandin E2
thromboxane A2 + ?
-
Substrates: -
Products: thromoboxane A2 is non-enzymatically converted to thromboxane B2, which is secretion is measured to analyze the enzyme activity
Products: thromoboxane A2 is non-enzymatically converted to thromboxane B2, which is secretion is measured to analyze the enzyme activity
?
Prostaglandin H3
Thromboxane B3 + DELTA14-12-hydroperoxy-5,8,10-heptadecatrienoic acid
-
Substrates: -
Products: -
Products: -
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
Substrates: -
Products: i.e. TXA2
Products: i.e. TXA2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
649094, 649095, 649437, 650205, 651184, 651899, 651979, 652105, 652714, 652716, 652719, 653003, 653424
Substrates: -
Products: i.e. TXA2
Products: i.e. TXA2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
Substrates: -
Products: -
Products: -
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
-
Substrates: -
Products: thromboxane B1 is scarcely detectable, the major product is 12(L)-hydroxy-8,10-heptadecadienoic acid
Products: thromboxane B1 is scarcely detectable, the major product is 12(L)-hydroxy-8,10-heptadecadienoic acid
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
-
Substrates: activity is equal to that with prostaglandin H2
Products: thromboxane B1 is scarcely detectable, the major product is 12(L)-hydroxy-8,10-heptadecadienoic acid
Products: thromboxane B1 is scarcely detectable, the major product is 12(L)-hydroxy-8,10-heptadecadienoic acid
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
-
Substrates: -
Products: -
Products: -
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
-
Substrates: -
Products: -
Products: -
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
-
Substrates: -
Products: thromboxane B2 is not mentioned as product
Products: thromboxane B2 is not mentioned as product
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
-
Substrates: -
Products: thromboxane B1 is scarcely detectable, the major product is 12(L)-hydroxy-8,10-heptadecadienoic acid
Products: thromboxane B1 is scarcely detectable, the major product is 12(L)-hydroxy-8,10-heptadecadienoic acid
?
prostaglandin H1
12(L)-hydroxy-8,10-heptadecadienoic acid + thromboxane B1
-
Substrates: poor substrate
Products: -
Products: -
?
prostaglandin H2
thromboxane A2
-
Substrates: -
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: the thromboxane A2 that is formed by the enzyme is transformed to thromboxane B2
Products: the thromboxane A2 that is formed by the enzyme is transformed to thromboxane B2
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: + malondialdehyde
Products: + malondialdehyde
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: the ratio of thromboxane to C17 hydroxyfatty acid formation is 1:1
Products: the ratio of thromboxane to C17 hydroxyfatty acid formation is 1:1
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: thromboxane A2 is an intermediate
Products: thromboxane A2 is an intermediate
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
3167, 3169, 3170, 3171, 3174, 3177, 3179, 3180, 3183, 3185, 3186, 3187, 3188, 3189, 3190, 3192, 3193, 3195, 3197, 3198, 37485
Substrates: i.e. PGH2
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: -
Products: -
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: the ratio of 12-hydroxy-5,8,10-heptadecatrienoic acid to thromboxane B2 varries from 1.6 to 2.1 depending on the reaction conditions
Products: the ratio of 12-hydroxy-5,8,10-heptadecatrienoic acid to thromboxane B2 varries from 1.6 to 2.1 depending on the reaction conditions
?
Prostaglandin H2
thromboxane B2 + 12(L)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: i.e. PGH2
Products: -
Products: -
?
prostaglandin H2
thromboxane B2 + 12(S)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: -
Products: -
Products: -
?
prostaglandin H2
thromboxane B2 + 12(S)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: -
Products: -
Products: -
?
prostaglandin H2
thromboxane B2 + 12(S)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: -
Products: -
Products: -
?
additional information
?
-
-
Substrates: production of thromboxane A2, an unstable bioregulator that induces platelet release reaction, platelet aggregation and smooth muscle contraction
Products: -
Products: -
?
additional information
?
-
-
Substrates: TXAS is one of the terminal enzymes of the arachidonic acid cascade and converts prostaglandins H2 into thromobane A2 in the endoplasmic reticulum
Products: -
Products: -
?
additional information
?
-
-
Substrates: cyclooxygenase-2 and thromboxane synthase are involved in the diosgenin-induced megakaryocytic differentiation in HEL cells
Products: for analysis of the thromboxane synthase activity the secretion of thromoxane B2 is measured. Thromboxane B2 is a nonenzymatic conversion product of thromobxane A1, the product of the thromboxane synthase activity
Products: for analysis of the thromboxane synthase activity the secretion of thromoxane B2 is measured. Thromboxane B2 is a nonenzymatic conversion product of thromobxane A1, the product of the thromboxane synthase activity
?
additional information
?
-
-
Substrates: thromboxane A2 synthase catalyzes an isomerization of prostaglandins H2 to give rise to thromboxane A2 along with a fragmentation reaction to 12-L-hydroxy-5,8,10-heptadecatrienoic acid and malondialdehyde. 2-p-Toluidinylnaphthalene-6-sulfonic acid is utilized as a probe to assess the spatial relationship and binding dynamics of ligand-enzyme interactions by steady-state and time-resolved fluorescence spectroscopy
Products: -
Products: -
?
additional information
?
-
-
Substrates: substrate binding analysis using substrate analogues of PGH2, U44069 and U46619
Products: -
Products: -
?
additional information
?
-
Substrates: the enzyme interacts with calreticulin, calnexin, cytochrome P450 2D10, cytochrome P450 2E1, NADPH-cytochrome P450 reductase, endoplasmin, mitochondrial GrpE protein homolog, heat shock 70 kDa protein 1-like, heat shock-related 70 kDa protein 2, protein disulfide isomerase A6, and serine/threonine-protein phosphatase 2B catalytic subunit beta isoform
Products: -
Products: -
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
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
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
12-L-hydroxy-5,8,10-heptadecaotrienoic acid + malondialdehyde
-
Substrates: -
Products: ratio of TXA2/heptadecatrienoic acid/malondialdehyde, 1/1/1
Products: ratio of TXA2/heptadecatrienoic acid/malondialdehyde, 1/1/1
?
prostaglandin H2
thromboxane B2 + 12(S)-hydroxy-5,8,10-heptadecatrienoic acid
-
Substrates: -
Products: -
Products: -
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
Substrates: -
Products: i.e. TXA2
Products: i.e. TXA2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
649094, 649095, 649437, 650205, 651184, 651899, 651979, 652105, 652714, 652716, 652719, 653003, 653424
Substrates: -
Products: i.e. TXA2
Products: i.e. TXA2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
Substrates: -
Products: -
Products: -
?
additional information
?
-
-
Substrates: production of thromboxane A2, an unstable bioregulator that induces platelet release reaction, platelet aggregation and smooth muscle contraction
Products: -
Products: -
?
additional information
?
-
-
Substrates: TXAS is one of the terminal enzymes of the arachidonic acid cascade and converts prostaglandins H2 into thromobane A2 in the endoplasmic reticulum
Products: -
Products: -
?
additional information
?
-
-
Substrates: cyclooxygenase-2 and thromboxane synthase are involved in the diosgenin-induced megakaryocytic differentiation in HEL cells
Products: for analysis of the thromboxane synthase activity the secretion of thromoxane B2 is measured. Thromboxane B2 is a nonenzymatic conversion product of thromobxane A1, the product of the thromboxane synthase activity
Products: for analysis of the thromboxane synthase activity the secretion of thromoxane B2 is measured. Thromboxane B2 is a nonenzymatic conversion product of thromobxane A1, the product of the thromboxane synthase activity
?
additional information
?
-
-
Substrates: thromboxane A2 synthase catalyzes an isomerization of prostaglandins H2 to give rise to thromboxane A2 along with a fragmentation reaction to 12-L-hydroxy-5,8,10-heptadecatrienoic acid and malondialdehyde. 2-p-Toluidinylnaphthalene-6-sulfonic acid is utilized as a probe to assess the spatial relationship and binding dynamics of ligand-enzyme interactions by steady-state and time-resolved fluorescence spectroscopy
Products: -
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
heme
-
the heme-thiolate group of the enzyme is required to split and activate the endoperoxide bond of prostaglandin H2
heme
-
contains one heme per 58000 MW protein. The major part of the enzyme is converted by the elution procedure to the inactive P420 form, a minor part is in its native heme-thiolate conformation
heme
-
comparison of thromboxane A2 synthase model based on the P450BM-3 with another thromboxane A2 synthase model based on the P450cam structure indicates that P450BM-3 is a more suitable template for homology modeling of thromboxane A2 synthase. P450BM-3 and p450cam are hemoprotein domains of cytochrome
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
cyanide binding to substrate-free and substrate-bound CYP5A1 in a detergent-solubilized system and in nanodiscs, binding kinetics, overview
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
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
(5E)-6-[3-(N''-tert-butyl-N'-cyanocarbamimidamido)phenyl]-6-(pyridin-3-yl)hex-5-enoic acid
-
i.e. terbogrel
(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
(Z)-(3-[[6-(2-chlorophenyl)-1,4-dimethyl-7,10-dihydro-4H-pyrido[4',3':4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-9(8H)-yl]methyl]phenyl)-N-(5-ethoxy-5-oxopentyl)(pyridin-3-yl)methanimine N-oxide
-
-
([5-[2-([[(1E)-phenyl(pyridin-3-yl)methylidene]amino]oxy)ethyl]-7,8-dihydronaphthalen-1-yl]oxy)acetic acid
-
i.e. ONO-1301, in addition to inhibitory activity, application of ONO-1301 significantly attenuates the development of pulmonary fibrosis and improves survival after treatment with bleomycin
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-[3-(4-Benzylhydryl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl)-1H-indole-6-carboxylic acid
-
strong thromboxane synthetase inhibition and H1-blocking activity
15-Hydroxy-9alpha,11alpha-peroxidoprosta-5,13-dienoic acid
-
irreversible inactivation during catalysis, protection by (E)-3-[4-(1-imidazolylmethyl)phenyl]-2-propenoate and 15-hydroxy-11alpha,9alpha-(epoxymethano)-prosta-5,13-dienoic acid
1H-Imidazol-1-ylalyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives
-
dual thromboxane synthase inhibitor/thromboxane receptor antagonists
2-[(1H-imidazol-1-yl)methyl]-4,5-dihydro-1-benzothiophene-6-carboxylic acid
-
i.e. CS-518
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-(4-[[(4-chlorobenzene-1-sulfonyl)amino](pyridin-3-yl)methyl]phenyl)propanoic 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-methoxy-N1,N3-bis[(pyridin-3-yl)methyl]benzene-1,3-dicarboxamide
-
i.e. picotamide
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-[3-(imidazol-1-yl)-propyl]-5,6,7,8-tetrahydroquinoline
-
0.0023 mM, 50% inhibition
5E-6-(3-cyanoguanidino)phenyl-6-(3-pyridyl)hex-5-enoic acid
-
0.00043 mM, 50% inhibition
5Z-6[(2S,4R)-4-(4-Chlorophenylsulfonylamino)-1-(3-pyridylmethyl)-2-pyrrolidinyl]-5-hexenoic acid
-
causes marked improvement in the PGI2/TXA2 ratio in diabetic retinopathy by inhibition of thromboxane synthase
8-[(4-chlorobenzene-1-sulfonyl)amino]-4-[3-(pyridin-3-yl)propyl]octanoic acid
-
i.e. CGS-22652
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
-
-
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%
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
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-nitrobenzenesulfonyl]urea
-
0.001 mM, 95% inhibition
N-Substituted 3-(1H-imidazol-1-ylmethyl)indole carboxylic acid derivatives
-
-
-
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
[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 monoethyl ester
-
-
4-{2-[(4-chlorophenyl)methyl]-3-phenylpropanoyl}phenyl hydrogen benzylphosphonate
-
i.e. N-0164
4-{2-[(4-chlorophenyl)methyl]-3-phenylpropanoyl}phenyl hydrogen benzylphosphonate
-
-
9alpha,11alpha-Methanoepoxy-15(S)-hydroxyprosta-5(cis)-13(trans)-dienoic acid
-
no inhibition
9alpha,11alpha-Methanoepoxy-15(S)-hydroxyprosta-5(cis)-13(trans)-dienoic acid
-
weak
furegrelate
-
cultures treated with show a reduced time-dependent increase in cell number compared with vehicle-treated cells. Addition to the growth medium results in reduction in cell invasion and reduction in cell migration.
furegrelate
-
specific inhibitor of thromboxane synthase, i.e. sodium 5-(3-pyridinylmethyl) benzofuran-2-carboxylate
furegrelate
-
inhibition of thromboxane-A synthase, induces a concentration-dependent increase in cAMP-induced steroidogenic acute regulatory protein StAR concomitantly with a significant increase in steroid hormone production
imidazole
-
and derivatives. The potency of 1-substituted imidazoles is increased as the side chain becomes more hydrophobic. Inhibition is competitive with respect to prostaglandin endoperoxide substrate
ozagrel
-
cultures treated with show a reduced time-dependent increase in cell number compared with vehicle-treated cells. Addition to the growth medium results in reduction in cell invasion and reduction in cell migration.
additional information
-
the enzyme is insensitive to sulfhydryl reagents and thiols
-
additional information
-
the enzyme is not affected by nonsteroidal antiinflammatory agents
-
additional information
-
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
-
additional information
-
dual angiotensin converting enzyme/thromboxane synthase inhibitors
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
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
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
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.02
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
23°C, pH 7.5
0.021
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
recombinant TXAS
0.022
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
native TXAS
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.017
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
recombinant TXAS
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
Chlorella powder
-
3.32 microg/ml, tested in an in vitro assay system
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000004
(5E)-6-[3-(N''-tert-butyl-N'-cyanocarbamimidamido)phenyl]-6-(pyridin-3-yl)hex-5-enoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00006 - 0.47
(Z)-(3-[[6-(2-chlorophenyl)-1,4-dimethyl-7,10-dihydro-4H-pyrido[4',3':4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-9(8H)-yl]methyl]phenyl)-N-(5-ethoxy-5-oxopentyl)(pyridin-3-yl)methanimine N-oxide
0.000015
2-[(1H-imidazol-1-yl)methyl]-1-benzothiophene-6-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
2-[(1H-imidazol-1-yl)methyl]-4,5-dihydro-1-benzothiophene-6-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0004
3-(4-[[(4-chlorobenzene-1-sulfonyl)amino](pyridin-3-yl)methyl]phenyl)propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000043
4-methoxy-N1,N3-bis[(pyridin-3-yl)methyl]benzene-1,3-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
8-[(4-chlorobenzene-1-sulfonyl)amino]-4-[3-(pyridin-3-yl)propyl]octanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00006
(Z)-(3-[[6-(2-chlorophenyl)-1,4-dimethyl-7,10-dihydro-4H-pyrido[4',3':4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-9(8H)-yl]methyl]phenyl)-N-(5-ethoxy-5-oxopentyl)(pyridin-3-yl)methanimine N-oxide
Homo sapiens
-
pH and temperature not specified in the publication
0.47
(Z)-(3-[[6-(2-chlorophenyl)-1,4-dimethyl-7,10-dihydro-4H-pyrido[4',3':4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-9(8H)-yl]methyl]phenyl)-N-(5-ethoxy-5-oxopentyl)(pyridin-3-yl)methanimine N-oxide
Homo sapiens
-
pH and temperature not specified in the publication
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
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
additional information
-
application of monoclonal antibodies to develop a tandem immunoradiometric assay
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5 - 8.5
-
very little pH-dependence between pH 5-8.5, above pH 9.0 the reaction is significantly depressed
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
3164, 3167, 3168, 3169, 3170, 3171, 3174, 3175, 3177, 3178, 3179, 3180, 3182, 3183, 3185, 3186, 3187, 3188, 3189, 3190, 3192, 3193, 3194, 3195, 3197, 3198, 3200, 37485, 649094, 649095, 649437, 651184, 651899, 651979, 652105, 652714, 652716, 652719, 653003, 653424, 660657, 661427, 662993, 690411, 692671, 701976, 702474, 702865, 703584, 705219, 705275, 706861, 714914, 727012, 727320, 728292, 748300
-
-
brenda
unrelated families of Tunasian and Pakistani origin with Ghosal hematodiaphyseal dysplasia syndrome (GHDD, i.e. Ghosal syndrome), a rare autosomal recessive disorder characterized by increased bone densitiy
-
-
brenda
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
thromboxane synthase, prostaglandin cyclase and cyclooxygenase COX-1 are widely distributed throughout normal aortic endothelium
brenda
-
TXAS is expressed in the atherosclerotic lesion, associated with increased inflammatory cells, in particular M2 polarized macrophages
brenda
-
TXAS is expressed in the atherosclerotic lesion, associated with increased inflammatory cells, in particular M2 polarized macrophages
brenda
-
in normal lung tissue, TXS is moderately expressed in bronchial epithelial cells and weakly expressed in vascular smooth muscle cells
brenda
-
adenocarcinomas and squamous cell carcinomas, enzyme expression profile, overview. Enzyme expression is higher in adenocarcinoma and female patients
brenda
-
-
3164, 3167, 3168, 3169, 3170, 3171, 3174, 3175, 3177, 3178, 3179, 3180, 3182, 3186, 3189, 3190, 3192, 3194, 3198, 3200, 37485
brenda
-
the higher staining intensities are in the ganglion cell and inner plexiform layers and in the outer plexiform layer, with more staining in the inner nuclear layer than in the outer nuclear layer
brenda
-
the higher staining intensities are in the ganglion cell and inner plexiform layers and in the outer plexiform layer, with more staining in the inner nuclear layer than in the outer nuclear layer
brenda
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
-
-
brenda
Highest Expressing Human Cell Lines
Cell Line LinksPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
physiological function
additional information
malfunction
-
inhibition of thromboxane synthase induces lung cancer cell death via increasing the nuclear p27
malfunction
-
enzyme inhibition induces cell death in vitro. Selective TXS inhibition significantly reduces tumour cell growth and increases apoptosis, while TXS overexpression stimulates cell proliferation and invasiveness, and is protective against apoptosis, quantification of multi-parameter apoptosis signalling, overview
malfunction
blockade of enzyme/thromboxane A2/ thromboxane prostanoid signaling confers renal protection against ischaemia/reperfusion injury through the actions of anti-oxidation, anti-inflammation, anti-apoptosis, antiautophagy and anti-pyroptosis
physiological function
-
thromboxane synthase metabolises prostaglandin H2 into thromboxanes, which are biologically active on cancer cells. TXS overexpression occurs in a range of cancers, and associated with a poor prognosis, although in non-small lung cancer cells, no significant correlation with patient survival is observed
physiological function
-
the enzyme is a membrane-associated cytochrome P450 that metabolizes the cyclooxygenase product prostaglandin into thromboxane A2, a potent inducer of vasoconstriction and platelet aggregation
additional information
-
the adaptive active site in the enzyme might be capable of binding multiple ligands simultaneously because of its large size and flexibility. Ligand and substrate binding structure, competitive binding experiments with Nile Red, a fluorescence dye, and 2-p-toluidinylnaphthalene-6-sulfonic acid, and the computer-simulated TXAS structure with clotrimazole as a heme ligand, molecular dynamics simulations of clotrimazole and 2-p-toluidinylnaphthalene-6-sulfonic acid-docking enzyme, overview
additional information
-
role of membranes in modulating the thermodynamics and kinetics of enzyme substrate binding, redox potential of enzyme incorporated into lipid bilayers of nanodiscs, overview. Binding of substrate to the enzyme can induce conformational changes in the protein that block small-molecule ligand egress
Show AA Sequence and Transmembrane Helices (1272 entries)
Please use the AA Sequence and Transmembrane Helices Search for a specific query.
Please use the AA Sequence and Transmembrane Helices Search for a specific query.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
58000
60000
60000
-
transmembrane TXAS, considered to be an atypical memeber of the cytochrome P450 superfamily as lacks its minooxygenase activity
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
monomer
additional information
-
enzyme structure molecular homology modeling using the crystal structure of human microsomal CYP3A4, PDB entry 1TQN, as the template structure
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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
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
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
additional information
-
treatment with enzyme-specific RNAi results in increased levels of steroidogenic acute regulatory protein StAR and steroidogenesis. Inhibition of enzyme activity reduces the levels of StaR transcriptional repressor DAX-1
W133F
-
site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
partial
recombinant C-terminally His-tagged modified enzyme from Escherichia coli strain DH5alpha by nickel affinity chromatography
-
recombinant wild-type and mutant C-terminally His4-tagged modified enzyme from Escherichia coli strain BL21/(DE3)pLys by nickel affinity and hydroxyapatite chromatography
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
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
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
4 weeks of streptozotocin-induced diabetes do not increase the retinal levels of TxS
after 8 and 16 weeks on the fat diet, aortic arches from low-density lipoprotein receptor deficient mice show a significant increase in TXAS mRNA level when compared with control
-
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
renal cancer, colorectal, prostate, and pancreatic cancers display moderate and strong positivity of enzyme protein expression
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
-
TXAS mRNA expression is increased within the vascular wall in mouse models of atherosclerosis with advanced lesions
-
4 weeks of streptozotocin-induced diabetes do not increase the retinal levels of TxS
-
4 weeks of streptozotocin-induced diabetes do not increase the retinal levels of TxS
-
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
-
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
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
analysis
medicine
pharmacology
analysis
-
application of monoclonal antibodies to develop a tandem immunoradiometric assay
analysis
-
immobilized enzyme is sufficiently stable to be used as a model for studying the properties of the enzyme
medicine
-
the thromboxane A2 synthetase inhibitor/thromboxane A2-receptor antagonist (5Z)-6-[(2S,4R)-4-(4-chlorophenylsulfonylamino)-1-(3-pyridylmethyl)-2-pyrrolidinyl]-5-hexenoic acid hydrochloride may be of clinical relevance for the prevention or treatment of th
medicine
-
thromboxane A2 may somehow mediate coughing induced by the angiotensin converting enzyme inhibitors. Patients on angiotensin converting enzyme inhibitors who develop cough may benefit from thromboxane A2 synthetase inhibitors
medicine
-
improvement of the renal function with the selective thromboxane A2 synthetase inhibitor (+/-)-6-(1-imidazolylmethyl)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid hydrochloride hemihydrate
medicine
-
TXAS mRNA expression was found to be an independent prognostic marker for patients with bladder cancer
medicine
-
in addition to inhibitory activity, application of ONO-1301, i.e. ([5-[2-([[(1E)-phenyl(pyridin-3-yl)methylidene]amino]oxy)ethyl]-7,8-dihydronaphthalen-1-yl]oxy)acetic acid, significantly attenuates the development of pulmonary fibrosis and improves survival after treatment with bleomycin
medicine
-
thromboxane-A synthase protein is consistently upregulated in the cancer tissues from patients with colorectal carcinoma and also highly expressed in colonic cancer cell lines. Depletion of enzyme protein by antisense oligonucleotide inhibits proliferation of cancer cells
medicine
-
the targeted inhibition of TXSA activity improves the efficiency of conventional alkylation chemotherapy in vivo
medicine
-
TBXAS1 gene polymorphisms are a marker for development of cerebral infarction, especially small-artery occlusion type in Korean population
medicine
the enzyme is a prognostic biomarker for renal cancer and, partly, for colorectal, prostate, and pancreatic cancers
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
pharmacology
-
the thromboxane A2 synthetase inhibitor 1-[3-(4-benzylhydryl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl)-1H-indole-6-carboxylic acid is a candidate anti-asthmatic drug
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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
brenda
Shen, R.F.; Tai, H.H.
Monoclonal antibodies to thromboxane synthase from porcine lung. Production and application to development of a tandem immunoradiometric assay
J. Biol. Chem.
261
11585-11591
1986
Sus scrofa
brenda
Shen, R.F.; Tai, H.H.
Immunoaffinity purification and characterization of thromboxane synthase from porcine lung
J. Biol. Chem.
261
11592-11599
1986
Sus scrofa
brenda
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
brenda
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
brenda
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
brenda
Gorman, R.R.
Biology and biochemistry of thromboxane synthetase inhibitors
Adv. Prostaglandin Thromboxane Leukot. Res.
11
235-240
1983
Homo sapiens
brenda
Ullrich, V.; Haurand, M.
Thromboxane synthase as a cytochrome P450 enzyme
Adv. Prostaglandin Thromboxane Leukot. Res.
11
105-110
1983
Homo sapiens
brenda
Yashimoto, T.; Yamamoto, S.
Partial purification and assay of thromboxane A synthase from bovine platelets
Methods Enzymol.
86
106-109
1982
Bos taurus
brenda
Hall, E.R.; Tai, H.H.
Purification of thromboxane synthetase and evidence of two distinct mechanisms for the formation of 12-L-hydroxy-5,8,10-heptadecatrienoic acid by porcine lung microsomes
Biochim. Biophys. Acta
665
498-503
1981
Sus scrofa
brenda
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
brenda
Hammarstroem, S.; Diczfalusy, U.
Inhibition and properties of thromboxane synthetase
Adv. Inflamm. Res.
1
431-438
1979
Homo sapiens
-
brenda
Wlodawer, P.; Hammarstroem, S.
Thromboxane synthase from bovine lung - solubilization and partial purification
Biochem. Biophys. Res. Commun.
80
525-532
1978
Bos taurus
brenda
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
brenda
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
brenda
Diczfalusy, U.; Hammarstrm, S.
Inhibitors of thromboxane synthase in human platelets
FEBS Lett.
82
107-110
1977
Homo sapiens
brenda
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
brenda
Yoshimoto, T.; Yamamoto, S.; Okuma, M.; Hayaishi, O.
Solubilization and resolution of thromboxane synthesizing system from microsomes of bovine blood platelets
J. Biol. Chem.
252
5871-5874
1977
Bos taurus
brenda
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
brenda
Ullrich, V.; Nusing, R.
Thromboxane synthase. From isolation to function
Stroke
21
IV134-IV138
1994
Homo sapiens
brenda
Sone, H.; Okuda, Y.; Kawakami, Y.; Yamashita, K.
Effects of high glucose concentration and a thromboxane synthase inhibitor on the production of thromboxane A2 and prostaglandin I2 and E2 by cultured retinal endothelial cells
Life Sci.
58
239-243
1996
Bos taurus
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
Hall, E.R.; Townsend, G.L.; Tuan, W.M; Venton, D.L.
Immobilization of catalytically active thromboxane synthase
Prostaglandins Leukot. Essent. Fatty Acids
32
51-56
1988
Bos taurus
brenda
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
brenda
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
brenda
Nusing, R.; Schneider-Voss, S.; Ullrich, V.
Immunoaffinity purification of human thromboxane synthase
Arch. Biochem. Biophys.
280
325-330
1990
Homo sapiens
brenda
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
brenda
Kamiya, S.; Matsui, H.; Shirahase, H.; Nakamura, S.; Wada, K.; Kanda, M.; Shimaji, H.; Kakeya, N.
Thromboxane A2 synthetase inhibitors with histamine H1-blocking activity: synthesis and evaluation of a new series of indole derivatives
Chem. Pharm. Bull.
43
1692-1695
1995
Oryctolagus cuniculus
brenda
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
brenda
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
Homo sapiens, Bos taurus
brenda
Albuquerque, M.G.; Rodrigues.C.R.; Bicca de Alencastro, R.
Design of new potential 5-lipoxygenase inhibitors. Dual thromboxane synthase inhibitors, and thromboxane A2 receptor antagonists by AM1
Int. J. Quantum Chem.
22
181-190
1995
Mammalia
-
brenda
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
-
brenda
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
brenda
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
-
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
Yagi, A.; Kabash, A.; Mizuno, K.; Moustafa, S.M.; Khalifa, T.I.; Tsuji, H.
Radical scavenging glycoprotein inhibiting cyclooxygenase-2 and thromboxane A2 synthase from aloe vera gel
Planta Med.
69
269-271
2003
Aloe vera
brenda
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
brenda
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
brenda
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
brenda
Murakami, S.; Nagaya, N.; Itoh, T.; Kataoka, M.; Iwase, T.; Horio, T.; Miyahara, Y.; Sakai, Y.; Kangawa, K.; Kimura, H.
Prostacyclin agonist with thromboxane synthase inhibitory activity (ONO-1301) attenuates bleomycin-induced pulmonary fibrosis in mice
Am. J. Physiol.
290
L59-L65
2006
Mus musculus
brenda
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
brenda
Kawka, D.W.; Ouellet, M.; Hetu, P.; Singer, I.I.; Riendeau, D.
Double-label expression studies of prostacyclin synthase, thromboxane synthase and COX isoforms in normal aortic endothelium
Biochim. Biophys. Acta
1771
45-54
2007
Canis lupus familiaris
brenda
Wang, X.; Yin, X.; Schiffer, R.B.; King, S.R.; Stocco, D.M.; Grammas, P.
Inhibition of thromboxane A synthase activity enhances steroidogenesis and steroidogenic acute regulatory gene expression in MA-10 mouse leydig cells
Endocrinology
149
851-857
2008
Mus musculus
brenda
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
brenda
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
brenda
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
brenda
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
brenda
Lee, J.J.; Yu, J.Y.; Lee, J.H.; Zhang, W.Y.; Kim, T.J.; Myung, C.S.; Yun, Y.P.
The protective effects of paclitaxel on platelet aggregation through the inhibition of thromboxane A2 synthase
Arch. Pharm. Res.
33
387-394
2010
Oryctolagus cuniculus
brenda
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
brenda
Cyrus, T.; Ding, T.; Pratico, D.
Expression of thromboxane synthase, prostacyclin synthase and thromboxane receptor in atherosclerotic lesions: correlation with plaque composition
Atherosclerosis
208
376-381
2010
Mus musculus
brenda
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
brenda
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
brenda
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
brenda
Wright, W.S.; McElhatten, R.M.; Harris, N.R.
Expression of thromboxane synthase and the thromboxane-prostanoid receptor in the mouse and rat retina
Exp. Eye Res.
89
532-537
2009
Rattus norvegicus, Mus musculus
brenda
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
Mus musculus, Homo sapiens
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
Son, D.J.; Akiba, S.; Hong, J.T.; Yun, Y.P.; Hwang, S.Y.; Park, Y.H.; Lee, S.E.
Piperine inhibits the activities of platelet cytosolic phospholipase A2 and thromboxane A2 synthase without affecting cyclooxygenase-1 activity different mechanisms of action are involved in the inhibition of platelet aggregation and macrophage inflammatory response
Nutrients
6
3336-3352
2014
Oryctolagus cuniculus
brenda
Ershov, P.V.; Yablokov, E.; Zgoda, V.; Mezentsev, Y.; Gnedenko, O.; Kaluzhskiy, L.; Svirid, A.; Gilep, A.; Usanov, S.A.; Ivanov, A.
A new insight into subinteractomes of functional antagonists Thromboxane (CYP5A1) and prostacyclin (CYP8A1) synthases
Cell Biol. Int.
45
1175-1182
2021
Homo sapiens (P24557)
brenda
Ji, Y.; Li, R.; Tian, Y.; Chen, G.; Yan, A.
Classification models and SAR analysis on thromboxane A2 synthase inhibitors by machine learning methods
SAR QSAR Environ. Res.
33
429-462
2022
Homo sapiens
brenda
Chueh, T.H.; Cheng, Y.H.; Chen, K.H.; Chien, C.T.
Thromboxane A2 synthase and thromboxane receptor deletion reduces ischaemia/reperfusion-evoked inflammation, apoptosis, autophagy and pyroptosis
Thromb. Haemost.
120
329-343
2020
Mus musculus (P30987)
brenda
EXTERNAL LINKS (specific for EC-Number 5.3.99.5)
html completed
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2026.1 (March 2026)
About BRENDA
Social media
Help
Survey
Download
Contribution
Legal
Curated at
Member of
![DSMZ Digital Diversity]()
![Global Core Biodata Resource]()
![ELIXIR Core Data Resource]()
![German Network for Bioinformatics Infrastructure]()
