indoleamine 2,3-dioxygenase 2 | 1.13.11.- Dioxygenases | IUPHAR/BPS Guide to PHARMACOLOGY

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indoleamine 2,3-dioxygenase 2

target has curated data in GtoImmuPdb

Target id: 3019

Nomenclature: indoleamine 2,3-dioxygenase 2

Abbreviated Name: IDO2

Family: 1.13.11.- Dioxygenases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 420 8p11.21 IDO2 indoleamine 2,3-dioxygenase 2
Mouse - 405 8 A2 Ido2 indoleamine 2,3-dioxygenase 2
Rat - 403 16q12.5 Ido2 indoleamine 2,3-dioxygenase 2
Previous and Unofficial Names
indoleamine 2 | INDOL1 | indoleamine-pyrrole 2,3 dioxygenase-like 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.13.11.52
Description Reaction Reference
D-tryptophan + O(2) <=> N-formyl-D-kynurenine
L-tryptophan + O(2) <=> N-formyl-L-kynurenine

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
tryptanthrin 5i Hs Inhibition 6.0 pKi 1
pKi 6.0 (Ki 9.7x10-7 M) [1]
tryptanthrin 5i Hs Inhibition 5.7 – 6.3 pIC50 1
pIC50 6.3 (IC50 4.5x10-7 M) [1]
Description: Inhibition of enzyme activity when hIDO2 is expressed in U87 human glioblastoma cells.
pIC50 5.7 (IC50 1.8x10-6 M) [1]
Description: Inhibition of enzymatic activity of recombinant human IDO2.
Immunopharmacology Comments
IDO2 is an enzyme in the tryptophan-kynurenine pathway. It is expressed in immune cells (e.g. dendritic cells and monocytes) which suggests that it plays some role in immune function, but its precise function remains to be fully elucidated. Mice lacking Ido2 produce greater amounts of interleukin-6 (IL-6) and have elevated levels of activated (phosphorylated) Stat3 compared to wild type mice in response to LPS exposure [2]. Overexpression of Ido2 (in mouse macrophages) has the opposite effect, i.e. suppression of IL-6 production and Stat3 activation. These results suggest that pharmacological modulation of Ido2 could be exploited to regulate IL-6/Stat3 signalling as a mechanism to treat immune disorders.
Physiological Consequences of Altering Gene Expression
Ido2 knockout mice are more susceptible to LPS endotoxin-induced shock and death than wild type mice.
Species:  Mouse
Tissue: 
Technique: 
References:  2

References

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1. Li J, Li Y, Yang D, Hu N, Guo Z, Kuang C, Yang Q. (2016) Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors. Eur J Med Chem, 123: 171-179. [PMID:27475108]

2. Yamamoto Y, Yamasuge W, Imai S, Kunisawa K, Hoshi M, Fujigaki H, Mouri A, Nabeshima T, Saito K. (2018) Lipopolysaccharide shock reveals the immune function of indoleamine 2,3-dioxygenase 2 through the regulation of IL-6/stat3 signalling. Sci Rep, 8 (1): 15917. [PMID:30374077]

How to cite this page

1.13.11.- Dioxygenases: indoleamine 2,3-dioxygenase 2. Last modified on 05/11/2018. Accessed on 23/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3019.