BRENDA - Enzyme Database
show all sequences of 5.3.99.5

Functional investigations of thromboxane synthase (CYP5A1) in lipid bilayers of nanodiscs

Das, A.; Varma, S.S.; Mularczyk, C.; Meling, D.D.; ChemBioChem 15, 892-899 (2014)

Data extracted from this reference:

Activating Compound
Activating Compound
Commentary
Organism
Structure
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
Homo sapiens
phosphatidylcholine
-
Homo sapiens
phosphatidylethanolamine
-
Homo sapiens
phosphatidylserine
-
Homo sapiens
Cloned(Commentary)
Cloned (Commentary)
Organism
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
Homo sapiens
Localization
Localization
Commentary
Organism
GeneOntology No.
Textmining
endoplasmic reticulum membrane
associated
Homo sapiens
5789
-
Metals/Ions
Metals/Ions
Commentary
Organism
Structure
additional information
cyanide binding to substrate-free and substrate-bound CYP5A1 in a detergent-solubilized system and in nanodiscs, binding kinetics, overview
Homo sapiens
Natural Substrates/ Products (Substrates)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
ID
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
Homo sapiens
-
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
-
?
Organism
Organism
UniProt
Commentary
Textmining
Homo sapiens
-
-
-
Purification (Commentary)
Purification (Commentary)
Organism
recombinant C-terminally His-tagged modified enzyme from Escherichia coli strain DH5alpha by nickel affinity chromatography
Homo sapiens
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
Substrate Product ID
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
727320
Homo sapiens
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
-
-
?
additional information
substrate binding analysis using substrate analogues of PGH2, U44069 and U46619
727320
Homo sapiens
?
-
-
-
-
Synonyms
Synonyms
Commentary
Organism
CYP5A1
-
Homo sapiens
thromboxane synthase
-
Homo sapiens
Cofactor
Cofactor
Commentary
Organism
Structure
heme
-
Homo sapiens
Activating Compound (protein specific)
Activating Compound
Commentary
Organism
Structure
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
Homo sapiens
phosphatidylcholine
-
Homo sapiens
phosphatidylethanolamine
-
Homo sapiens
phosphatidylserine
-
Homo sapiens
Cloned(Commentary) (protein specific)
Commentary
Organism
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
Homo sapiens
Cofactor (protein specific)
Cofactor
Commentary
Organism
Structure
heme
-
Homo sapiens
Localization (protein specific)
Localization
Commentary
Organism
GeneOntology No.
Textmining
endoplasmic reticulum membrane
associated
Homo sapiens
5789
-
Metals/Ions (protein specific)
Metals/Ions
Commentary
Organism
Structure
additional information
cyanide binding to substrate-free and substrate-bound CYP5A1 in a detergent-solubilized system and in nanodiscs, binding kinetics, overview
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
ID
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
Homo sapiens
-
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
-
?
Purification (Commentary) (protein specific)
Commentary
Organism
recombinant C-terminally His-tagged modified enzyme from Escherichia coli strain DH5alpha by nickel affinity chromatography
Homo sapiens
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
ID
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
727320
Homo sapiens
(5Z,13E)-(15S)-9alpha,11alpha-epoxy-15-hydroxythromboxa-5,13-dienoate
-
-
-
?
additional information
substrate binding analysis using substrate analogues of PGH2, U44069 and U46619
727320
Homo sapiens
?
-
-
-
-
General Information
General Information
Commentary
Organism
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
Homo sapiens
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
Homo sapiens
General Information (protein specific)
General Information
Commentary
Organism
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
Homo sapiens
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
Homo sapiens
Other publictions for EC 5.3.99.5
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Synonyms
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
727320
Das
Functional investigations of t ...
Homo sapiens
ChemBioChem
15
892-899
2014
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748300
Sathler
Human thromboxane synthase Co ...
Homo sapiens
J. Enzyme Inhib. Med. Chem.
29
527-531
2014
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748790
Son
Piperine inhibits the activit ...
Oryctolagus cuniculus
Nutrients
6
3336-3352
2014
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727012
Chao
Probing ligand binding to thro ...
Homo sapiens
Biochemistry
52
1113-1121
2013
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1
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6
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1
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6
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1
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1
1
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714914
Muzaffar
NADPH oxidase 1 mediates upreg ...
Homo sapiens
Eur. J. Pharmacol.
658
187-192
2011
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1
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728292
Cathcart
Examination of thromboxane syn ...
Homo sapiens
Mol. Cancer
10
25
2011
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2
2
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701961
Lee
The protective effects of pacl ...
Oryctolagus cuniculus
Arch. Pharm. Res.
33
387-394
2010
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701976
Vila
Heritability of thromboxane A2 ...
Homo sapiens
Arterioscler. Thromb. Vasc. Biol.
30
128-134
2010
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701992
Cyrus
Expression of thromboxane synt ...
Mus musculus
Atherosclerosis
208
376-381
2010
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1
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702474
Cathcart
The role of prostacyclin synth ...
Homo sapiens
Biochim. Biophys. Acta
1805
153-166
2010
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1
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11
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11
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1
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705219
Gabrielsen
Thromboxane synthase expressio ...
Homo sapiens, Mus musculus
J. Mol. Med.
88
795-806
2010
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706861
Schmidt
Inhibition of thromboxane synt ...
Homo sapiens
Transl. Oncol.
3
43-49
2010
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702865
Park
Association of polymorphisms i ...
Homo sapiens
BMB Rep.
42
200-205
2009
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703584
Leung
Inhibition of thromboxane synt ...
Homo sapiens
Exp. Cell Res.
315
2974-2981
2009
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703587
Wright
Expression of thromboxane synt ...
Mus musculus, Rattus norvegicus
Exp. Eye Res.
89
532-537
2009
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705275
Schauff
Inhibition of invasion-associa ...
Homo sapiens
J. Neurooncol.
91
241-249
2009
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679522
Wang
Inhibition of thromboxane A sy ...
Mus musculus
Endocrinology
149
851-857
2008
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690411
Cailleteau
Increased cyclooxygenase-2 and ...
Homo sapiens
Anal. Biochem.
380
26-34
2008
1
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692671
Cheng
Chlorella powder inhibits the ...
Homo sapiens
Int. J. Food Sci. Nutr.
60 Suppl 1
89-98
2008
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694313
Genevieve
Thromboxane synthase mutations ...
Homo sapiens
Nat. Genet.
40
284-286
2008
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5
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-
-
677820
Yeh
Reaction mechanisms of 15-hydr ...
Homo sapiens
Arch. Biochem. Biophys.
461
159-168
2007
-
-
1
-
-
-
-
2
-
-
-
-
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
678436
Kawka
Double-label expression studie ...
Canis lupus familiaris
Biochim. Biophys. Acta
1771
45-54
2007
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
677451
Murakami
Prostacyclin agonist with thro ...
Mus musculus
Am. J. Physiol.
290
L59-L65
2006
-
1
-
-
-
-
1
-
-
-
-
-
-
3
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
679825
Sakai
Upregulation of thromboxane sy ...
Homo sapiens
FEBS Lett.
580
3368-3374
2006
-
1
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
661427
Moussa
Prognostic and functional sign ...
Homo sapiens
Cancer Res.
65
11581-11587
2005
-
1
-
-
-
-
2
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
660657
Nie
Differential expression of thr ...
Homo sapiens
Am. J. Pathol.
164
429-439
2004
-
1
-
-
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
662993
Stachowska
Isomers of trans fatty acids m ...
Homo sapiens
Nutrition
20
570-571
2004
-
-
-
-
-
-
2
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
650205
Chen
Resonance Raman investigation ...
Homo sapiens
Biochemistry
42
2542-2551
2003
-
-
1
-
-
-
-
-
-
-
-
1
-
2
-
-
1
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
651184
Michaux
A pharmacophore model for sulp ...
Homo sapiens
Eur. J. Med. Chem.
38
703-710
2003
-
-
-
-
-
-
4
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
653424
Villalobos
Effects of camonagrel, a selec ...
Homo sapiens
Pharmacology
69
44-50
2003
-
-
-
-
-
-
2
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
653579
Yagi
Radical scavenging glycoprotei ...
Aloe vera
Planta Med.
69
269-271
2003
-
-
-
-
-
-
1
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
649095
Michaux
N-tert-butyl-N'-(2-cyclohexyla ...
Homo sapiens
Acta Crystallogr. Sect. C
58
o621-623
2002
-
-
-
-
-
-
1
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652105
Wang
Substrate binding is the rate- ...
Homo sapiens
J. Biol. Chem.
276
14737-14743
2001
-
-
1
-
-
-
-
2
1
-
-
2
-
2
-
-
1
-
-
-
-
-
2
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
2
1
-
-
2
-
-
-
1
-
-
-
-
2
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
653003
Dogne
Design, synthesis and biologic ...
Homo sapiens
J. Pharm. Pharmacol.
53
669-680
2001
-
-
-
-
-
-
2
-
-
-
-
1
-
5
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
649094
Michaux
-
Terbogrel, a dual-acting agent ...
Homo sapiens
Acta Crystallogr. Sect. C
56
1265-1266
2000
-
-
-
-
-
-
1
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
649437
Hsu
Identification of thromboxane ...
Homo sapiens
Arch. Biochem. Biophys.
383
119-127
2000
-
-
1
-
19
-
-
-
1
-
-
1
-
1
-
-
1
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
19
-
-
-
-
-
1
-
-
1
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652719
Jacobs
1-Imidazolyl(alkyl)-substitute ...
Homo sapiens
J. Med. Chem.
43
1841-1851
2000
-
-
-
-
-
-
15
-
-
-
-
2
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
15
-
-
-
-
-
2
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
651979
Hsu
Expression, purification, and ...
Homo sapiens
J. Biol. Chem.
274
762-769
1999
-
-
1
-
-
-
-
1
-
-
-
1
-
4
-
-
1
-
-
-
1
-
1
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
1
-
-
-
1
-
-
-
1
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652716
Soyka
Guanidine derivatives as combi ...
Homo sapiens
J. Med. Chem.
42
1235-1249
1999
-
-
-
-
-
-
18
-
-
-
-
1
-
3
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
18
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
651899
Borsch-Haubold
Direct inhibition of cyclooxyg ...
Homo sapiens
J. Biol. Chem.
273
28766-28772
1998
-
-
-
-
-
-
1
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652714
Takeuchi
Development of dual-acting age ...
Homo sapiens
J. Med. Chem.
41
5362-5374
1998
-
-
-
-
-
-
22
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
22
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3185
Umemura
Thromboxane A2 synthetase inhi ...
Homo sapiens
Life Sci.
60
1583-1588
1997
-
1
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3187
Yoshida
Improvement of renal function ...
Homo sapiens
Adv. Exp. Med. Biol.
433
113-117
1997
-
1
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3190
Dickinson
Thromboxane modulating agents. ...
Homo sapiens
J. Med. Chem.
40
3442-3452
1997
-
-
-
-
-
-
2
-
1
-
-
-
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
37485
Wade
Nitric oxide modulates the act ...
Homo sapiens
Arch. Biochem. Biophys.
347
174-180
1997
-
-
-
-
-
-
1
-
1
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3184
Sone
Effects of high glucose concen ...
Bos taurus
Life Sci.
58
239-243
1996
-
-
-
-
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3197
Uematsu
Pharmacokinetic and pharmacody ...
Homo sapiens
J. Pharm. Pharmacol.
48
380-385
1996
-
1
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3186
Ledergerber
Development of a screening ass ...
Homo sapiens
J. Enzyme Inhib.
9
253-261
1995
-
1
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3189
Lee
Discovery of potent cyclic GMP ...
Homo sapiens, Rattus norvegicus
J. Med. Chem.
38
3547-3557
1995
-
-
-
-
-
-
3
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3196
Kamiya
Thromboxane A2 synthetase inhi ...
Oryctolagus cuniculus
Chem. Pharm. Bull.
43
1692-1695
1995
-
1
-
-
-
-
2
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3199
Albuquerque
-
Design of new potential 5-lipo ...
Mammalia
Int. J. Quantum Chem.
22
181-190
1995
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
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1
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-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3183
Ullrich
Thromboxane synthase. From iso ...
Homo sapiens
Stroke
21
IV134-IV138
1994
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
15
-
-
1
-
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-
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-
-
1
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-
1
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-
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-
-
-
-
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-
-
15
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3188
Miyata
Characterization of the human ...
Homo sapiens
Eur. J. Biochem.
224
273-279
1994
-
-
1
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
2
-
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1
-
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1
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2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3192
Ksander
Dual angiotensin converting en ...
Homo sapiens
J. Med. Chem.
37
1823-1832
1994
-
-
-
-
-
-
11
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
-
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-
-
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-
11
-
-
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-
-
-
-
-
-
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1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3193
Ruan
Comparison of the construction ...
Homo sapiens
Protein Eng.
7
1345-1351
1994
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
1
-
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-
-
-
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1
-
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-
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1
-
-
-
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-
-
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-
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-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3195
Orlandi
Thromboxane A2 synthase activi ...
Homo sapiens
Biochim. Biophys. Acta
1215
285-290
1994
-
-
-
-
-
-
1
1
-
-
-
-
-
2
-
-
-
-
-
3
-
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1
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1
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1
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-
-
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-
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-
-
3
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3200
Haurand
-
Thromboxane synthase and prost ...
Homo sapiens, Sus scrofa
Front. Biotransform.
6
183-199
1992
-
-
-
-
-
-
3
-
2
-
-
-
-
2
-
-
-
1
-
4
-
-
7
-
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-
-
-
-
-
-
1
2
-
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-
-
-
-
2
-
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-
-
3
-
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2
-
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-
-
4
-
-
7
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
3194
Nusing
Immunoaffinity purification of ...
Homo sapiens
Arch. Biochem. Biophys.
280
325-330
1990
-
-
-
-
-
-
-
1
1
-
1
-
-
2
-
-
1
-
-
1
1
-
1
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
1
1
-
1
-
-
-
-
1
-
1
1
-
1
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3198
Jones
'Suicide' inactivation of thro ...
Bos taurus, Homo sapiens
J. Biol. Chem.
265
20166-20171
1990
-
-
-
-
-
-
1
1
2
-
-
-
-
2
-
-
1
-
-
2
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
2
-
-
-
-
-
-
1
-
2
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3191
Hall
Immobilization of catalyticall ...
Bos taurus
Prostaglandins Leukot. Essent. Fatty Acids
32
51-56
1988
-
1
-
-
-
-
1
2
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3164
Hecker
Products, kinetics, and substr ...
Homo sapiens
Arch. Biochem. Biophys.
254
124-135
1987
-
-
-
-
-
-
-
3
-
-
-
-
-
2
-
-
-
-
-
1
-
-
6
-
-
-
1
-
4
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
1
-
-
6
-
-
1
-
4
1
-
-
-
-
-
-
-
-
-
3169
Hecker
Thromboxane synthase catalyses ...
Homo sapiens
Eur. J. Biochem.
169
563-569
1987
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
1
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3165
Shen
Monoclonal antibodies to throm ...
Sus scrofa
J. Biol. Chem.
261
11585-11591
1986
-
1
-
-
-
-
-
-
1
-
1
-
-
3
-
-
1
-
-
8
1
-
1
1
-
-
-
-
-
1
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
1
-
8
1
-
1
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
3166
Shen
Immunoaffinity purification an ...
Sus scrofa
J. Biol. Chem.
261
11592-11599
1986
-
-
-
-
-
-
6
1
-
-
-
-
-
5
-
-
1
-
-
2
1
-
1
-
-
1
-
-
-
-
-
-
1
1
-
-
-
-
-
1
-
-
-
-
6
1
1
-
-
-
-
-
-
-
1
-
2
1
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
3167
Hall
Production of platelet thrombo ...
Homo sapiens
Biochem. J.
233
637-641
1986
-
-
-
-
-
1
3
-
-
-
-
-
-
2
-
-
1
-
-
2
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
3
-
-
-
-
-
-
-
-
-
1
-
2
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3168
Haurand
Isolation and characterization ...
Homo sapiens
J. Biol. Chem.
260
15059-15067
1985
-
-
-
-
-
-
-
-
1
-
1
-
-
3
-
-
1
-
-
1
1
-
1
1
-
-
-
-
1
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
1
-
1
-
-
-
-
1
-
1
1
-
1
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
3170
Gorman
Biology and biochemistry of th ...
Homo sapiens
Adv. Prostaglandin Thromboxane Leukot. Res.
11
235-240
1983
-
-
-
-
-
-
2
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3171
Ullrich
Thromboxane synthase as a cyto ...
Homo sapiens
Adv. Prostaglandin Thromboxane Leukot. Res.
11
105-110
1983
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
1
-
-
1
1
-
1
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
1
-
1
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3172
Yashimoto
Partial purification and assay ...
Bos taurus
Methods Enzymol.
86
106-109
1982
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
1
-
1
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
1
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3173
Hall
Purification of thromboxane sy ...
Sus scrofa
Biochim. Biophys. Acta
665
498-503
1981
-
-
-
-
-
-
1
-
1
-
-
-
-
2
-
-
1
-
-
2
1
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
1
-
2
1
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
3174
Hammarstroem
Enzymatic synthesis of 15-hydr ...
Homo sapiens
J. Biol. Chem.
255
518-521
1980
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3175
Hammarstroem
-
Inhibition and properties of t ...
Homo sapiens
Adv. Inflamm. Res.
1
431-438
1979
-
-
-
-
-
-
9
-
1
-
-
-
-
1
-
-
1
-
-
1
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
9
-
-
1
-
-
-
-
-
-
1
-
1
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3176
Wlodawer
Thromboxane synthase from bovi ...
Bos taurus
Biochem. Biophys. Res. Commun.
80
525-532
1978
-
-
-
-
-
-
-
-
1
-
-
-
-
2
-
-
1
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3177
Tai
On the inhibitory potency of i ...
Homo sapiens
Biochem. Biophys. Res. Commun.
80
236-242
1978
-
-
-
-
-
-
4
-
1
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
1
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3178
Diczfalusy
Conversion of prostaglandin en ...
Homo sapiens
FEBS Lett.
84
271-274
1977
-
-
-
-
-
-
5
-
1
-
-
1
-
2
-
-
-
-
-
2
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
5
-
-
1
-
-
1
-
-
-
-
-
2
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3179
Diczfalusy
Inhibitors of thromboxane synt ...
Homo sapiens
FEBS Lett.
82
107-110
1977
-
-
-
-
-
-
4
-
1
-
-
-
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
1
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3180
Hammarstroem
Resolution of prostaglandin sy ...
Homo sapiens
Proc. Natl. Acad. Sci. USA
74
3691-3695
1977
-
-
-
-
-
-
2
-
1
-
-
-
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
2
1
-
1
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3181
Yoshimoto
Solubilization and resolution ...
Bos taurus
J. Biol. Chem.
252
5871-5874
1977
-
-
-
-
-
-
-
-
1
-
-
-
-
2
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3182
Sun
Biosynthesis of thromboxanes i ...
Homo sapiens
Biochem. Biophys. Res. Commun.
74
1432-1440
1977
-
-
-
-
-
-
3
-
1
-
-
-
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
1
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-