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Literature summary for 1.13.11.52 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
Search for more literature for 1.13.11.52

Application

Application Comment Organism
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)

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

Inhibitors

Inhibitors Comment Organism Structure
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
methyl thiohydantoin-Trp
-
 Homo sapiens
additional information no inhibition by phenylthiohydantoin-Trp; no inhibition by phenylthiohydantoin-Trp 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 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
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
N-methyl-L-Trp
-
 Homo sapiens

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens F5H5G0 IDO2
-
Homo sapiens P14902 IDO1
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

Turnover Number [1/s]

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

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
0.0216
-
 pH 7.0, 22°C, IDO1 Homo sapiens methyl thiohydantoin-Trp
0.0826
-
 pH 7.0, 22°C, IDO2 Homo sapiens methyl thiohydantoin-Trp
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
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
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
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
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

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

kcat/KM [mM/s]

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