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Literature summary extracted from

  • Katane, M.; Saitoh, Y.; Hanai, T.; Sekine, M.; Furuchi, T.; Koyama, N.; Nakagome, I.; Tomoda, H.; Hirono, S.; Homma, H.
    Thiolactomycin inhibits D-aspartate oxidase: a novel approach to probing the active site environment (2010), Biochimie, 92, 1371-1378.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.4.3.1 expression of GST-tagged, N-terminally His-tagged, and S-tagged DDO Mus musculus

Protein Variants

EC Number Protein Variants Comment Organism
1.4.3.1 R237A site-directed mutagenesis, active site mutant, shows reduced binding of inhibitor thiolactomycin compared to the wild-type enzyme Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.4.3.1 (5R)-4-hydroxy-3,5-dimethyl-5-[(1E)-2-methyl-1,3-butadienyl]-2(5H)-thiophenone i.e. thiolactomycin, active site-directed DDO inhibitor, competitive inhibition, competes with both the substrate and the coenzyme FAD; i.e. thiolactomycin, competitive inhibition, competes with both the substrate and the coenzyme FAD Homo sapiens
1.4.3.1 (5R)-4-hydroxy-3,5-dimethyl-5-[(1E)-2-methyl-1,3-butadienyl]-2(5H)-thiophenone i.e. thiolactomycin, active site-directed DDO inhibitor involving binding via Arg237, mixed type of inhibition, competes with both the substrate and the coenzyme FAD, structural models of mouse DDO/TLM complexes; i.e. thiolactomycin, competitive inhibition, competes with both the substrate and the coenzyme FAD Mus musculus
1.4.3.1 malonate
-
 Homo sapiens
1.4.3.1 malonate competitive inhibition Mus musculus
1.4.3.1 meso-tartrate
-
 Homo sapiens
1.4.3.1 meso-tartrate competitive inhibition Mus musculus
1.4.3.3 (5R)-4-hydroxy-3,5-dimethyl-5-[(1E)-2-methyl-1,3-butadienyl]-2(5H)-thiophenone i.e. thiolactomycin, competitive inhibition, competes with both the substrate and the coenzyme FAD Sus scrofa

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.4.3.1 D-aspartate + H2O + O2 Mus musculus
-
 oxaloacetate + NH3 + H2O2
-
 ?
1.4.3.1 D-aspartate + H2O + O2 Homo sapiens
-
 oxaloacetate + NH3 + H2O2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.4.3.1 Homo sapiens
-
-
-
1.4.3.1 Mus musculus
-
-
-
1.4.3.1 Mus musculus
-
 male ICR mice
-
1.4.3.3 Sus scrofa
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.4.3.1 Hep-G2 cell
-
 Homo sapiens
-
1.4.3.3 commercial preparation
-
 Sus scrofa
-
1.4.3.3 kidney
-
 Sus scrofa
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.4.3.1 D-aspartate + H2O + O2
-
 Mus musculus oxaloacetate + NH3 + H2O2
-
 ?
1.4.3.1 D-aspartate + H2O + O2
-
 Homo sapiens oxaloacetate + NH3 + H2O2
-
 ?
1.4.3.1 additional information structure-function relationships of DDO, overview Mus musculus ?
-
 ?
1.4.3.1 additional information structure-function relationships of DDO, overview Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.4.3.1 DAO
-
 Mus musculus
1.4.3.1 DAO
-
 Homo sapiens
1.4.3.1 DDO
-
 Mus musculus
1.4.3.1 DDO
-
 Homo sapiens
1.4.3.3 DAO
-
 Sus scrofa

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.4.3.1 37
-
 assay at Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.4.3.1 8.3
-
 assay at Mus musculus

Cofactor

EC Number Cofactor Comment Organism Structure
1.4.3.1 FAD
-
 Mus musculus
1.4.3.1 FAD
-
 Homo sapiens
1.4.3.3 FAD
-
 Sus scrofa

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.4.3.1 additional information
-
 additional information inhibition kinetics Mus musculus
1.4.3.1 0.66
-
 (5R)-4-hydroxy-3,5-dimethyl-5-[(1E)-2-methyl-1,3-butadienyl]-2(5H)-thiophenone pH 8.3, 37°C Mus musculus
1.4.3.1 1.59
-
 malonate pH 8.3, 37°C Mus musculus
1.4.3.1 1.94
-
 meso-tartrate pH 8.3, 37°C Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.4.3.1 1.86
-
 pH 8.3, 37°C Mus musculus (5R)-4-hydroxy-3,5-dimethyl-5-[(1E)-2-methyl-1,3-butadienyl]-2(5H)-thiophenone
1.4.3.1 5.3
-
 pH 8.3, 37°C Mus musculus malonate
1.4.3.1 8.71
-
 pH 8.3, 37°C Mus musculus meso-tartrate