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Literature summary extracted from
- Inhibition of rat liver iodothyronine deiodinase. Interaction of aurones with the iodothyronine ligand-binding site (1986), J. Biol. Chem., 261, 11623-11630.
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.21.99.3 | (2E)-2-(3,4-dihydroxybenzylidene)-4,6-dihydroxy-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5'-deiodinase EC 1.97.1.10 | Rattus norvegicus |  |
| 1.21.99.3 | (2E)-2-(3,4-dihydroxybenzylidene)-6-hydroxy-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5'-deiodinase EC 1.97.1.10 | Rattus norvegicus | |
| 1.21.99.3 | (2E)-4,6-dihydroxy-2-(4-hydroxy-3-iodobenzylidene)-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5'-deiodinase EC 1.97.1.10 | Rattus norvegicus | |
| 1.21.99.3 | (2E)-4,6-dihydroxy-2-(4-hydroxybenzylidene)-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5'-deiodinase EC 1.97.1.10 | Rattus norvegicus | |
| 1.21.99.3 | (4-[(E)-(4,6-dihydroxy-3-oxo-1-benzofuran-2(3H)-ylidene)methyl]phenoxy)acetic acid | aurone derivative isolated from plant extract. Comparison with inhibition of 5'-deiodinase EC 1.97.1.10 | Rattus norvegicus | |
| 1.21.99.3 | 2-(3,4-dihydroxybenzyl)-4,6-dihydroxy-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5'-deiodinase EC 1.97.1.10 | Rattus norvegicus | |
| 1.21.99.3 | 3',4',4,6-tetrahydroxyaurone | inhibition kinetics; very potent naturally occuring plant-derived inhibitor, conformation study | Rattus norvegicus | |
| 1.21.99.3 | 3,3',5'-triiodo-L-thyronine | substrate inhibition | Rattus norvegicus | |
| 1.21.99.3 | 4',4,6-trihydroxyaurone | cofactor competitive mechanism, displacement of thyroxine from the binding site of thyroxine-binding prealbumin; inhibition kinetics; very potent naturally occuring plant-derived inhibitor | Rattus norvegicus | |
| 1.21.99.3 | ellagic acid | - |
Rattus norvegicus | |
| 1.21.99.3 | luteolin-7-beta-glucoside | - |
Rattus norvegicus | |
| 1.21.99.3 | rosmarinic acid | - |
Rattus norvegicus | |
| 1.21.99.4 | (2E)-2-(3,4-dihydroxybenzylidene)-4,6-dihydroxy-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5-deiodinase EC 1.97.1.11 | Rattus norvegicus | |
| 1.21.99.4 | (2E)-2-(3,4-dihydroxybenzylidene)-6-hydroxy-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5-deiodinase EC 1.97.1.11 | Rattus norvegicus | |
| 1.21.99.4 | (2E)-4,6-dihydroxy-2-(4-hydroxy-3-iodobenzylidene)-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5-deiodinase EC 1.97.1.11 | Rattus norvegicus | |
| 1.21.99.4 | (2E)-4,6-dihydroxy-2-(4-hydroxybenzylidene)-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5-deiodinase EC 1.97.1.11 | Rattus norvegicus | |
| 1.21.99.4 | (4-[(E)-(4,6-dihydroxy-3-oxo-1-benzofuran-2(3H)-ylidene)methyl]phenoxy)acetic acid | aurone derivative isolated from plant extract. Comparison with inhibition of 5-deiodinase EC 1.97.1.11 | Rattus norvegicus | |
| 1.21.99.4 | 2-(3,4-dihydroxybenzyl)-4,6-dihydroxy-1-benzofuran-3(2H)-one | aurone derivative isolated from plant extract. Comparison with inhibition of 5-deiodinase EC 1.97.1.11 | Rattus norvegicus | |
Localization
| EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|---|
| 1.21.99.3 | microsome | - |
Rattus norvegicus | - |
- |
| 1.21.99.3 | microsome | 5'-deiodinase and 5-deiodinase activity | Rattus norvegicus | - |
- |
| 1.21.99.4 | microsome | - |
Rattus norvegicus | - |
- |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.21.99.3 | L-thyroxine + AH2 | Rattus norvegicus | 5-deiodinase activity | 3,3',5'-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | Rattus norvegicus | 5'-deiodinase activity | 3,3',5-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.21.99.3 | Rattus norvegicus | - |
- |
- |
| 1.21.99.3 | Rattus norvegicus | - |
isozyme type I | - |
| 1.21.99.4 | Rattus norvegicus | - |
- |
- |
Reaction
| EC Number | Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|---|
| 1.21.99.3 | 3,3',5'-triiodo-L-thyronine + iodide + acceptor + H+ = L-thyroxine + reduced acceptor | enzyme has both thyroxine 5-deiodinase and thyroxine 5'-deiodinase activities | Rattus norvegicus |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 1.21.99.3 | liver | - |
Rattus norvegicus | - |
| 1.21.99.4 | liver | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.21.99.3 | 3,3',5'-triiodo-L-thyronine + AH2 | preferred substrate | Rattus norvegicus | 3,3'-diiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | 3,3',5'-triiodo-L-thyronine + AH2 | type I isozyme | Rattus norvegicus | 3,3'-diiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | 3,3',5-triiodo-L-thyronine + AH2 | - |
Rattus norvegicus | 3,3'-diiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | - |
Rattus norvegicus | 3,3',5'-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | type I isozyme | Rattus norvegicus | 3,3',5'-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | 5-deiodinase activity | Rattus norvegicus | 3,3',5'-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | i.e. 3,3',5,5'-tetraiodo-L-thyronine | Rattus norvegicus | 3,3',5'-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | preferred substrate | Rattus norvegicus | 3,3',5-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | 5'-deiodinase activity | Rattus norvegicus | 3,3',5-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.3 | L-thyroxine + AH2 | isozyme type I | Rattus norvegicus | 3,3',5-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
| 1.21.99.4 | 3,3',5'-triiodo-L-thyronine + AH2 | - |
Rattus norvegicus | 3,3'-diiodothyronine + iodide + A + H+ | - |
? | |
| 1.21.99.4 | L-thyroxine + AH2 | - |
Rattus norvegicus | 3,5,3'-triiodo-L-thyronine + iodide + A + H+ | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.21.99.3 | iodothyronine monodeiodinase | - |
Rattus norvegicus |
| 1.21.99.3 | ITHD | - |
Rattus norvegicus |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 1.21.99.3 | 37 | - |
assay at | Rattus norvegicus |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 1.21.99.3 | 7.4 | - |
assay at | Rattus norvegicus |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.21.99.3 | dithioerythritol | i.e. DTE | Rattus norvegicus | |
| 1.21.99.3 | dithioerythritol | cofactor, influences the kinetic parameters | Rattus norvegicus | |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.21.99.3 | additional information | - |
additional information | - |
Rattus norvegicus | |
| 1.21.99.3 | 0.00014 | - |
4',4,6-trihydroxyaurone | at 2-20 mM dithioerythreitol, pH 7.4, 37°C | Rattus norvegicus | |
| 1.21.99.3 | 0.00017 | - |
4',4,6-trihydroxyaurone | at 1.8 mM dithioerythreitol, pH 7.4, 37°C | Rattus norvegicus | |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 1.21.99.3 | 0.0005 | - |
pH 7.4, 37°C | Rattus norvegicus | (2E)-4,6-dihydroxy-2-(4-hydroxy-3-iodobenzylidene)-1-benzofuran-3(2H)-one | |
| 1.21.99.3 | 0.001 | - |
pH 7.4, 37°C | Rattus norvegicus | (2E)-2-(3,4-dihydroxybenzylidene)-4,6-dihydroxy-1-benzofuran-3(2H)-one | |
| 1.21.99.3 | 0.001 | - |
pH 7.4, 37°C | Rattus norvegicus | (2E)-4,6-dihydroxy-2-(4-hydroxybenzylidene)-1-benzofuran-3(2H)-one | |
| 1.21.99.3 | 0.005 | - |
pH 7.4, 37°C | Rattus norvegicus | (4-[(E)-(4,6-dihydroxy-3-oxo-1-benzofuran-2(3H)-ylidene)methyl]phenoxy)acetic acid | |
| 1.21.99.4 | 0.0005 | - |
pH 7.4, 37°C | Rattus norvegicus | (2E)-4,6-dihydroxy-2-(4-hydroxy-3-iodobenzylidene)-1-benzofuran-3(2H)-one | |
| 1.21.99.4 | 0.001 | - |
pH 7.4, 37°C | Rattus norvegicus | (2E)-2-(3,4-dihydroxybenzylidene)-4,6-dihydroxy-1-benzofuran-3(2H)-one | |
| 1.21.99.4 | 0.001 | - |
pH 7.4, 37°C | Rattus norvegicus | (2E)-4,6-dihydroxy-2-(4-hydroxybenzylidene)-1-benzofuran-3(2H)-one | |
| 1.21.99.4 | 0.005 | - |
pH 7.4, 37°C | Rattus norvegicus | (4-[(E)-(4,6-dihydroxy-3-oxo-1-benzofuran-2(3H)-ylidene)methyl]phenoxy)acetic acid | |
| 1.21.99.4 | 0.008 | - |
pH 7.4, 37°C | Rattus norvegicus | 2-(3,4-dihydroxybenzyl)-4,6-dihydroxy-1-benzofuran-3(2H)-one | |
| 1.21.99.4 | 0.01 | - |
pH 7.4, 37°C | Rattus norvegicus | (2E)-2-(3,4-dihydroxybenzylidene)-6-hydroxy-1-benzofuran-3(2H)-one | |
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