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Literature summary for 1.13.11.11 extracted from
- Indoleamine and tryptophan 2,3-dioxygenases as important future therapeutic targets (2021), Pharmacol. Ther., 221, 107746 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-(3-chlorophenyl)-imidazole | - |
Homo sapiens | |
| 4-chlorophenyl-1,2,3-triazol-4-amine | - |
Homo sapiens | |
| 4-phenylimidazole | - |
Homo sapiens |  |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| L-tryptophan + O2 | Homo sapiens | - |
N-formyl-L-kynurenine | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Homo sapiens | P14902 | - |
- |
| Homo sapiens | Q6ZQW0 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| A-172 cell | - |
Homo sapiens | - |
| HeLa cell | - |
Homo sapiens | - |
| lung | endothelial cell expression in lung | Homo sapiens | - |
| MDA-MB-231 cell | - |
Homo sapiens | - |
| placenta | endothelial cell expression in placenta | Homo sapiens | - |
| U-87MG cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 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 |
| TDO | - |
Homo sapiens |
| tryptophan-2,3-dioxygenase | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00011 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-chlorophenyl-1,2,3-triazol-4-amine | |
| 0.00033 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(3-chlorophenyl)-imidazole | |
| 0.00048 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-phenylimidazole | |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Homo sapiens | treated with interferon gamma stimulates hIDO1 expression | up |
General Information
| General Information | Comment | Organism |
|---|---|---|
| drug target | conversion of tryptophan to N-formylkynurenine is the first and rate-limiting step of the tryptophan metabolic pathway (i.e., the kynurenine pathway). This conversion is catalyzed by three enzyme isoforms: indoleamine 2,3-dioxygenase 1 (IDO1), indoleamine 2,3-dioxygenase 2 (IDO2), and tryptophan-2,3-dioxygenase (TDO). As this pathway generates numerous metabolites that are involved in various pathological conditions, IDOs and TDO represent important targets for therapeutic intervention. Despite their poor sequence similarities, their active sites are highly conserved, and therefore allow the design of inhibitors with multiple activities that can target at least two isoforms | Homo sapiens |
| physiological function | conversion of tryptophan to N-formylkynurenine is the first and rate-limiting step of the tryptophan metabolic pathway (i.e., the kynurenine pathway). This conversion is catalyzed by three enzyme isoforms: indoleamine 2,3-dioxygenase 1 (IDO1), indoleamine 2,3-dioxygenase 2 (IDO2), and tryptophan-2,3-dioxygenase (TDO) | Homo sapiens |
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