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Literature summary for 1.4.3.1 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
Search for more literature for 1.4.3.1

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

Inhibitors Comment Organism Structure
(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
(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
malonate
-
 Homo sapiens
malonate competitive inhibition Mus musculus
meso-tartrate
-
 Homo sapiens
meso-tartrate competitive inhibition Mus musculus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-
Mus musculus
-
 male ICR mice
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
DAO
-
 Mus musculus
DAO
-
 Homo sapiens
DDO
-
 Mus musculus
DDO
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
FAD
-
 Mus musculus
FAD
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information inhibition kinetics Mus musculus
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
1.59
-
 malonate pH 8.3, 37°C Mus musculus
1.94
-
 meso-tartrate pH 8.3, 37°C Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
5.3
-
 pH 8.3, 37°C Mus musculus malonate
8.71
-
 pH 8.3, 37°C Mus musculus meso-tartrate