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Literature summary extracted from

  • Meininger, D.; Zalameda, L.; Liu, Y.; Stepan, L.P.; Borges, L.; McCarter, J.D.; Sutherland, C.L.
    Purification and kinetic characterization of human indoleamine 2,3-dioxygenases 1 and 2 (IDO1 and IDO2) and discovery of selective IDO1 inhibitors (2011), Biochim. Biophys. Acta, 1814, 1947-1954.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.13.11.52 drug development therapeutic inhibition of IDO1 is receiving much attention due to its proposed role in the pathogenesis of several diseases including cancer, hypotension and neurodegenerative disorders Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.13.11.52 expression of His6-tagged IDO1 in Escherichia coli strain BL21 Star Homo sapiens
1.13.11.52 expression of His6-tagged IDO2 in Escherichia coli strain BL21 Star Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.13.11.52 2-([5-(3-methoxyphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)-N-(5-methyl-1,3-thiazol-2-yl)acetamide poor inhibitor; poor inhibitor Homo sapiens
1.13.11.52 methyl thiohydantoin-Trp
-
 Homo sapiens
1.13.11.52 additional information no inhibition by phenylthiohydantoin-Trp; no inhibition by phenylthiohydantoin-Trp Homo sapiens
1.13.11.52 N-(1,3-benzodioxol-5-yl)-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide a reversible inhibitor of IDO1. highly specific for IDO1 compared to IDO2, docking analysis with IDO1 and IDO2; a reversible inhibitor of IDO1. highly specific for IDO1 compared to IDO2, docking analysis with IDO1 and IDO2 Homo sapiens
1.13.11.52 N-carbamoyl-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide poor inhibitor; poor inhibitor Homo sapiens
1.13.11.52 N-methyl-L-Trp
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.13.11.52 0.0141
-
 L-tryptophan pH 7.0, 22°C, IDO2 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.13.11.52 D-tryptophan + O2 Homo sapiens
-
 N-formyl-D-kynurenine
-
 ?
1.13.11.52 L-tryptophan + O2 Homo sapiens
-
 N-formyl-L-kynurenine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.13.11.52 Homo sapiens F5H5G0 IDO2
-
1.13.11.52 Homo sapiens P14902 IDO1
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.13.11.52 recombinant His6-tagged IDO1 from Escherichia coli strain BL21 Star by nickel affinity chromatography and gel filtration Homo sapiens
1.13.11.52 recombinant His6-tagged IDO2 from Escherichia coli strain BL21 Star by nickel affinity chromatography and gel filtration Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.13.11.52 D-tryptophan + O2
-
 Homo sapiens N-formyl-D-kynurenine
-
 ?
1.13.11.52 L-tryptophan + O2
-
 Homo sapiens N-formyl-L-kynurenine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.13.11.52 IDO1
-
 Homo sapiens
1.13.11.52 IDO2
-
 Homo sapiens
1.13.11.52 indoleamine 2,3-dioxygenase 1
-
 Homo sapiens
1.13.11.52 indoleamine 2,3-dioxygenase 2
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.13.11.52 22
-
 assay at room temperature Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.13.11.52 1
-
 L-tryptophan pH 7.0, 22°C, IDO2 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.13.11.52 7
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.13.11.52 0.003
-
 pH 7.0, 22°C, IDO1 Homo sapiens N-(1,3-benzodioxol-5-yl)-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
1.13.11.52 0.0216
-
 pH 7.0, 22°C, IDO1 Homo sapiens methyl thiohydantoin-Trp
1.13.11.52 0.0826
-
 pH 7.0, 22°C, IDO2 Homo sapiens methyl thiohydantoin-Trp
1.13.11.52 0.25
-
 above, pH 7.0, 22°C, IDO1 Homo sapiens N-carbamoyl-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
1.13.11.52 0.25
-
 above, pH 7.0, 22°C, IDO1 Homo sapiens 2-([5-(3-methoxyphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)-N-(5-methyl-1,3-thiazol-2-yl)acetamide
1.13.11.52 0.25
-
 above, pH 7.0, 22°C, IDO2 Homo sapiens N-(1,3-benzodioxol-5-yl)-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
1.13.11.52 0.25
-
 above, pH 7.0, 22°C, IDO2 Homo sapiens N-carbamoyl-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
1.13.11.52 0.25
-
 above, pH 7.0, 22°C, IDO2 Homo sapiens 2-([5-(3-methoxyphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)-N-(5-methyl-1,3-thiazol-2-yl)acetamide

General Information

EC Number General Information Comment Organism
1.13.11.52 metabolism indoleamine 2,3-dioxygenase catalyzes the first step in tryptophan breakdown along the kynurenine pathway Homo sapiens
1.13.11.52 additional information IDO1 and IDO2 have different kinetic parameters and different inhibition profiles Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.13.11.52 4.5
-
 L-tryptophan pH 7.0, 22°C, IDO2 Homo sapiens
1.13.11.52 70.9
-
 L-tryptophan pH 7.0, 22°C, IDO1 Homo sapiens