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Literature summary extracted from

  • Costabile, M.; Bassal, N.K.; Gerber, J.P.; Hughes, B.P.
    Inhibition of indoleamine 2,3-dioxygenase activity by fatty acids and prostaglandins A structure function analysis (2017), Prostaglandins Leukot. Essent. Fatty Acids, 122, 7-15 .
    View publication on PubMed

Application

EC Number Application Comment Organism
1.13.11.52 pharmacology IDO-1 is a target for pharmacological inhibition in the treatment of cancer Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.13.11.52 (10Z,13Z)-nonadecadienoic acid 32% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (11Z,14Z)-eicosadienoic acid 42% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (11Z,14Z,17Z)-eisosatrienoic acid 19% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (12Z,15Z)-heneicosadienoic acid 39% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (13Z,16Z)-docosadienoic acid 39% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (13Z,16Z,19Z)-docosatrienoic acid 52% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (4Z,7Z,10Z,13Z,16Z)-docosapentaenoic acid 48% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (4Z,7Z,10Z,13Z,16Z,19Z)-Docosahexaenoic acid 35% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (5Z,8Z)-7,7-dimethyl-5,8-eicosadienoic acid 29% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (5Z,8Z)-eicosadienoic acid 42% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (5Z,8Z,11Z)-eisosatrienoic acid 45% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (5Z,8Z,11Z,14Z)-eicosatetraenoic acid 55% inhibition at 0.02 mM; 80% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (5Z,8Z,11Z,14Z,17Z)-eicosapentaenoic acid 19% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (7Z,10Z,13Z,16Z)-docosatetraenoic acid 42% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (8Z,11Z,14Z)-eisosatrienoic acid 68% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (9E,11Z)-octadecadienoic acid 26% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (9E,12E)-octadecadienoic acid 23% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (9Z,12Z)-octadecadienoic acid 16% inhibition at 0.02 mM Homo sapiens
1.13.11.52 (9Z,12Z,15Z)-octadecatrienoic acid 23% inhibition at 0.02 mM Homo sapiens
1.13.11.52 15-deoxy-DELTA12,14-prostaglandin
-
 Homo sapiens
1.13.11.52 arachidonate
-
 Homo sapiens
1.13.11.52 additional information inhibition of indoleamine 2,3-dioxygenase activity by fatty acids, eicosanoids and prostaglandins, structure-function-analysis, overview. No inhibition by (6Z,9Z,12Z)-octadecatrienoic and (6Z,9Z,12Z,15Z)-octadecatetraenoic Homo sapiens
1.13.11.52 prostaglandin (19R)-hydroxy-PGE2
-
 Homo sapiens
1.13.11.52 prostaglandin 13,14-dihydro-15-oxo-PGE2
-
 Homo sapiens
1.13.11.52 prostaglandin 15-oxo-PGE2
-
 Homo sapiens
1.13.11.52 prostaglandin 15-oxo-PGF2alpha
-
 Homo sapiens
1.13.11.52 prostaglandin 20-hydroxy PGE2
-
 Homo sapiens
1.13.11.52 prostaglandin DELTA12-PGJ2
-
 Homo sapiens
1.13.11.52 prostaglandin PGA2
-
 Homo sapiens
1.13.11.52 prostaglandin PGD2
-
 Homo sapiens
1.13.11.52 prostaglandin PGD2 ethanolamide
-
 Homo sapiens
1.13.11.52 prostaglandin PGE2
-
 Homo sapiens
1.13.11.52 prostaglandin PGE2 ethanolamide
-
 Homo sapiens
1.13.11.52 prostaglandin PGF2beta
-
 Homo sapiens
1.13.11.52 prostaglandin PGG2
-
 Homo sapiens
1.13.11.52 prostaglandin PGH2
-
 Homo sapiens
1.13.11.52 prostaglandin PGJ2
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.13.11.52 Homo sapiens
-
-
-

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.13.11.52 37
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.13.11.52 heme
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.13.11.52 0.0041
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGD2
1.13.11.52 0.0042
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGJ2
1.13.11.52 0.0044
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens 15-deoxy-DELTA12,14-prostaglandin
1.13.11.52 0.0046
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin DELTA12-PGJ2
1.13.11.52 0.0046
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGE2 ethanolamide
1.13.11.52 0.0047
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGD2 ethanolamide
1.13.11.52 0.0049
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGA2
1.13.11.52 0.0057
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGD2 ethanolamide
1.13.11.52 0.006
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin (19R)-hydroxy-PGE2
1.13.11.52 0.0063
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGE2 ethanolamide
1.13.11.52 0.0067
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin 13,14-dihydro-15-oxo-PGE2
1.13.11.52 0.0067
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGJ2
1.13.11.52 0.0068
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin 15-oxo-PGE2
1.13.11.52 0.0071
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGF2beta
1.13.11.52 0.0071
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin DELTA12-PGJ2
1.13.11.52 0.0072
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGH2
1.13.11.52 0.0074
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGD2
1.13.11.52 0.0074
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGF2beta
1.13.11.52 0.0074
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin 20-hydroxy PGE2
1.13.11.52 0.0076
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin 15-oxo-PGF2alpha
1.13.11.52 0.0078
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGA2
1.13.11.52 0.009
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin 15-oxo-PGE2
1.13.11.52 0.0092
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGG2
1.13.11.52 0.0095
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin (19R)-hydroxy-PGE2
1.13.11.52 0.0096
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGH2
1.13.11.52 0.01
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin PGE2
1.13.11.52 0.0112
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGG2
1.13.11.52 0.0112
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin 20-hydroxy PGE2
1.13.11.52 0.013
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens 15-deoxy-DELTA12,14-prostaglandin
1.13.11.52 0.0221
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin PGE2
1.13.11.52 0.0231
-
 pH not specified in the publication, 37°C, inhibition of human monocytes Homo sapiens prostaglandin 15-oxo-PGF2alpha
1.13.11.52 0.03
-
 pH not specified in the publication, 37°C, inhibition of human THP-1 cells Homo sapiens prostaglandin 13,14-dihydro-15-oxo-PGE2

Expression

EC Number Organism Comment Expression
1.13.11.52 Homo sapiens arachinoate and the prostaglandin metabolite, PGD2, repress the IFNgamma mediated activity of IDO-1 in THP-1 cells and human monocytes down

General Information

EC Number General Information Comment Organism
1.13.11.52 physiological function the enzyme catalyses the first and rate-limiting step in the metabolism of L-tryptophan. Degradation of L-Trp leads to the production of several immunosuppressive metabolites, including N-formyl kynurenine and kynurenine. Enzyme IDO-1 also plays a crucial role in immune suppression and tumour induced tolerance. IDO-1 acts as an inducible negative regulator of T cell viability, proliferation and activation Homo sapiens