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Literature summary for 5.3.3.12 extracted from
- Macrophage migration inhibitory factor (MIF) tautomerase inhibitors as potential novel anti-inflammatory agents: current developments (2009), Curr. Med. Chem., 16, 1091-1114.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-oxo-4-phenyl-3-butynoate | a potent site-directed irreversible inhibitor of the phenyl pyruvate tautomerase activity | Homo sapiens |  |
| 3,6-dihydroxy-1-methyl-5-oxo-3,5-dihydro-2H-indolium | a dopachrome derivative, 98% inhibition at 0.5 mM, mechanism of action, overview | Homo sapiens | |
| 3,6-dihydroxy-2-methyl-2,3-dihydro-5H-indol-5-one | a dopachrome derivative, 92% inhibition at 0.5 mM, mechanism of action, overview | Homo sapiens | |
| 3,6-dihydroxy-5-oxo-3,5-dihydro-2H-indole-2-carboxylic acid | a dopachrome derivative, complete inhibition at 0.5 mM, mechanism of action, overview | Homo sapiens | |
| 6-hydroxy-2-methyl-5-oxo-3,5-dihydro-2H-indole-2-carboxylic acid | a dopachrome derivative, 35% inhibition at 0.5 mM, mechanism of action, overview; a dopachrome derivative, L-derivative, 29% inhibition at 0.5 mM, mechanism of action, overview | Homo sapiens | |
| methyl 6-hydroxy-2-methyl-5-oxo-3,5-dihydro-2H-indole-2-carboxylate | a dopachrome derivative, 34% inhibition at 0.5 mM, mechanism of action, overview; a dopachrome derivative, 45% inhibition at 0.5 mM, mechanism of action, overview | Homo sapiens | |
| additional information | there exist several classes of inhibitors that are active against MIF tautomerase activity, overview | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | the MIF protein is multifunctional, exhibiting besides its L-dopachrome tautomerase activity, e.g. also phenylpyruvate tautomerase activity, EC 5.3.2.1, and thioredoxin-like function, or its cytokine function, overview | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| endothelial cell | - |
Homo sapiens | - |
| eosinophil | - |
Homo sapiens | - |
| macrophage | - |
Homo sapiens | - |
| pituitary gland | corticotrop cells | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| L-dopachrome | i.e. 2-carboxy-2,3-dihydroindole-5,6-quinone, the enzyme is strictly specific for the L-enantiomer. The N-terminal Pro is crucial for tautomerase activity | Homo sapiens | 5,6-dihydroxyindole-2-carboxylic acid | - |
? | |
| additional information | the MIF protein is multifunctional, exhibiting besides its L-dopachrome tautomerase activity, e.g. also phenylpyruvate tautomerase activity, EC 5.3.2.1, and thioredoxin-like function, or its cytokine function, overview | Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| trimer | the tertiary structure is stabilized by hydrogen bonds and a hydrophobic core, three beta-sheets and six alpha-helices surround a traversing channel with dominant positive charge in the middle of the trimer, structure, overview. The enzyme contains a Cys-Xaa-Xaa-Cys motif required for oxido-reductase activity and MIF-like activities like glucorticoid overriding and cell proliferation | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| D-dopachrome tautomerase | - |
Homo sapiens |
| DDT | - |
Homo sapiens |
| Macrophage migration inhibitory factor | - |
Homo sapiens |
| MIF | - |
Homo sapiens |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Homo sapiens | MIF expression is upregulated by cytokines, TNF-alpha and interleukin-I, and by bacterial endotoxins, such as lipopolysaccharides, and exotoxins | up |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | MIF expression contributes to cell proliferation, invasiveness and neo-angiogenesis of neuroblastoma, gastric, hepatocellular, bladder, and breast carcinomas. MIF takes part in the pathogenesis of Alzheimer's disease and multiple sklerosis | Homo sapiens |
| physiological function | MIF plays an essential role in both, innate and adaptive immune response. It is implicated in tumor growth and angiogenesis, an exerts an antagonistic effect against glucocorticoid immunosuppressive action, and shows glucorticoid overriding activity | Homo sapiens |
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