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Literature summary for 5.3.99.5 extracted from

  • 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 (2013), Biochemistry, 52, 1113-1121.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
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 Homo sapiens

Protein Variants

Protein Variants Comment Organism
W133F site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme Homo sapiens
W203F site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme Homo sapiens
W31F site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme Homo sapiens
W31F/W65F/W133F/W203F/W466F site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme Homo sapiens
W466F site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme Homo sapiens
W65F site-directed mutagenesis, ligand binding analysis compared to the wild-type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
clotrimazole as a heme ligand, molecular dynamics simulations of clotrimazole and 2-p-toluidinylnaphthalene-6-sulfonic acid-docking enzyme Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens 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 ?
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?

Organism

Organism UniProt Comment Textmining
Homo sapiens
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-
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Purification (Commentary)

Purification (Comment) Organism
recombinant wild-type and mutant C-terminally His4-tagged modified enzyme from Escherichia coli strain BL21/(DE3)pLys by nickel affinity and hydroxyapatite chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information 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 Homo sapiens ?
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?

Subunits

Subunits Comment Organism
More enzyme structure molecular homology modeling using the crystal structure of human microsomal CYP3A4, PDB entry 1TQN, as the template structure Homo sapiens

Synonyms

Synonyms Comment Organism
thromboxane A2 synthase
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Homo sapiens
thromboxane synthase
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Homo sapiens
TXAS
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Homo sapiens

Cofactor

Cofactor Comment Organism Structure
heme bound at the active site Homo sapiens

General Information

General Information Comment Organism
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 Homo sapiens