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Literature summary for 1.13.11.52 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

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

Inhibitors

Inhibitors Comment Organism Structure
(10Z,13Z)-nonadecadienoic acid 32% inhibition at 0.02 mM Homo sapiens
(11Z,14Z)-eicosadienoic acid 42% inhibition at 0.02 mM Homo sapiens
(11Z,14Z,17Z)-eisosatrienoic acid 19% inhibition at 0.02 mM Homo sapiens
(12Z,15Z)-heneicosadienoic acid 39% inhibition at 0.02 mM Homo sapiens
(13Z,16Z)-docosadienoic acid 39% inhibition at 0.02 mM Homo sapiens
(13Z,16Z,19Z)-docosatrienoic acid 52% inhibition at 0.02 mM Homo sapiens
(4Z,7Z,10Z,13Z,16Z)-docosapentaenoic acid 48% inhibition at 0.02 mM Homo sapiens
(4Z,7Z,10Z,13Z,16Z,19Z)-Docosahexaenoic acid 35% inhibition at 0.02 mM Homo sapiens
(5Z,8Z)-7,7-dimethyl-5,8-eicosadienoic acid 29% inhibition at 0.02 mM Homo sapiens
(5Z,8Z)-eicosadienoic acid 42% inhibition at 0.02 mM Homo sapiens
(5Z,8Z,11Z)-eisosatrienoic acid 45% inhibition at 0.02 mM Homo sapiens
(5Z,8Z,11Z,14Z)-eicosatetraenoic acid 55% inhibition at 0.02 mM; 80% inhibition at 0.02 mM Homo sapiens
(5Z,8Z,11Z,14Z,17Z)-eicosapentaenoic acid 19% inhibition at 0.02 mM Homo sapiens
(7Z,10Z,13Z,16Z)-docosatetraenoic acid 42% inhibition at 0.02 mM Homo sapiens
(8Z,11Z,14Z)-eisosatrienoic acid 68% inhibition at 0.02 mM Homo sapiens
(9E,11Z)-octadecadienoic acid 26% inhibition at 0.02 mM Homo sapiens
(9E,12E)-octadecadienoic acid 23% inhibition at 0.02 mM Homo sapiens
(9Z,12Z)-octadecadienoic acid 16% inhibition at 0.02 mM Homo sapiens
(9Z,12Z,15Z)-octadecatrienoic acid 23% inhibition at 0.02 mM Homo sapiens
15-deoxy-DELTA12,14-prostaglandin
-
Homo sapiens
arachidonate
-
Homo sapiens
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
prostaglandin (19R)-hydroxy-PGE2
-
Homo sapiens
prostaglandin 13,14-dihydro-15-oxo-PGE2
-
Homo sapiens
prostaglandin 15-oxo-PGE2
-
Homo sapiens
prostaglandin 15-oxo-PGF2alpha
-
Homo sapiens
prostaglandin 20-hydroxy PGE2
-
Homo sapiens
prostaglandin DELTA12-PGJ2
-
Homo sapiens
prostaglandin PGA2
-
Homo sapiens
prostaglandin PGD2
-
Homo sapiens
prostaglandin PGD2 ethanolamide
-
Homo sapiens
prostaglandin PGE2
-
Homo sapiens
prostaglandin PGE2 ethanolamide
-
Homo sapiens
prostaglandin PGF2beta
-
Homo sapiens
prostaglandin PGG2
-
Homo sapiens
prostaglandin PGH2
-
Homo sapiens
prostaglandin PGJ2
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

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

Temperature Optimum [°C]

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

Cofactor

Cofactor Comment Organism Structure
heme
-
Homo sapiens

IC50 Value

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

Organism Comment Expression
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

General Information Comment Organism
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