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Literature summary for 1.21.99.3 extracted from

  • Auf'mkolk, M.; Koehrle, J.; Hesch, R.D.; Cody, V.
    Inhibition of rat liver iodothyronine deiodinase. Interaction of aurones with the iodothyronine ligand-binding site (1986), J. Biol. Chem., 261, 11623-11630.
    View publication on PubMed
Search for more literature for 1.21.99.3

Inhibitors

Inhibitors Comment Organism Structure
(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
(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
(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
(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
(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
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
3',4',4,6-tetrahydroxyaurone inhibition kinetics; very potent naturally occuring plant-derived inhibitor, conformation study Rattus norvegicus
3,3',5'-triiodo-L-thyronine substrate inhibition Rattus norvegicus
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
ellagic acid
-
 Rattus norvegicus
luteolin-7-beta-glucoside
-
 Rattus norvegicus
rosmarinic acid
-
 Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Rattus norvegicus
-
-
microsome 5'-deiodinase and 5-deiodinase activity Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-thyroxine + AH2 Rattus norvegicus 5-deiodinase activity 3,3',5'-triiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2 Rattus norvegicus 5'-deiodinase activity 3,3',5-triiodo-L-thyronine + iodide + A + H+
-
 ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-
Rattus norvegicus
-
 isozyme type I
-

Reaction

Reaction Comment Organism Reaction ID
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
a

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3,3',5'-triiodo-L-thyronine + AH2 preferred substrate Rattus norvegicus 3,3'-diiodo-L-thyronine + iodide + A + H+
-
 ?
3,3',5'-triiodo-L-thyronine + AH2 type I isozyme Rattus norvegicus 3,3'-diiodo-L-thyronine + iodide + A + H+
-
 ?
3,3',5-triiodo-L-thyronine + AH2
-
 Rattus norvegicus 3,3'-diiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2
-
 Rattus norvegicus 3,3',5'-triiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2 type I isozyme Rattus norvegicus 3,3',5'-triiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2 5-deiodinase activity Rattus norvegicus 3,3',5'-triiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2 i.e. 3,3',5,5'-tetraiodo-L-thyronine Rattus norvegicus 3,3',5'-triiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2 preferred substrate Rattus norvegicus 3,3',5-triiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2 5'-deiodinase activity Rattus norvegicus 3,3',5-triiodo-L-thyronine + iodide + A + H+
-
 ?
L-thyroxine + AH2 isozyme type I Rattus norvegicus 3,3',5-triiodo-L-thyronine + iodide + A + H+
-
 ?

Synonyms

Synonyms Comment Organism
iodothyronine monodeiodinase
-
 Rattus norvegicus
ITHD
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
dithioerythritol i.e. DTE Rattus norvegicus
dithioerythritol cofactor, influences the kinetic parameters Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information
-
 Rattus norvegicus
0.00014
-
 4',4,6-trihydroxyaurone at 2-20 mM dithioerythreitol, pH 7.4, 37°C Rattus norvegicus
0.00017
-
 4',4,6-trihydroxyaurone at 1.8 mM dithioerythreitol, pH 7.4, 37°C Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0005
-
 pH 7.4, 37°C Rattus norvegicus (2E)-4,6-dihydroxy-2-(4-hydroxy-3-iodobenzylidene)-1-benzofuran-3(2H)-one
0.001
-
 pH 7.4, 37°C Rattus norvegicus (2E)-2-(3,4-dihydroxybenzylidene)-4,6-dihydroxy-1-benzofuran-3(2H)-one
0.001
-
 pH 7.4, 37°C Rattus norvegicus (2E)-4,6-dihydroxy-2-(4-hydroxybenzylidene)-1-benzofuran-3(2H)-one
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