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Literature summary for 1.1.1.21 extracted from
- 6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2 (2010), Bioorg. Med. Chem. Lett., 20, 5630-5633.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3-hydroxycoumarin | - |
Rattus norvegicus |  |
| 4-Hydroxycoumarin | - |
Rattus norvegicus | |
| 6,7-dihydroxy-4-methylcoumarin | - |
Rattus norvegicus | |
| 6,7-dihydroxy-4-phenylcoumarin | binds to ALR2 in a different manner from epalrestat, molecular docking, overview. Suppresses galactitol accumulation | Rattus norvegicus | |
| 6,7-dihydroxycoumarin | - |
Rattus norvegicus | |
| 6-hydroxy-7-methoxycoumarin | - |
Rattus norvegicus | |
| 6-hydroxycoumarin | - |
Rattus norvegicus | |
| 7-hydroxy-4-methylcoumarin | - |
Rattus norvegicus | |
| 7-hydroxy-4-phenylcoumarin | - |
Rattus norvegicus | |
| 7-hydroxy-6-methoxycoumarin | - |
Rattus norvegicus | |
| 7-hydroxycoumarin | - |
Rattus norvegicus | |
| 7-hydroxylcoumarin-4-acetic acid | - |
Rattus norvegicus | |
| 7-hydroxylcoumarinyl-4-acetic acid | - |
Rattus norvegicus | |
| 7-methoxycoumarin | - |
Rattus norvegicus | |
| coumarin | - |
Rattus norvegicus | |
| epalrestat | - |
Rattus norvegicus | |
| additional information | structure-activity relationship of a series of coumarins as ALR1 inhibitors, overview. The C6 OH group interferes with ALR1 inhibition activity; structure-activity relationship of a series of coumarins as ALR2 inhibitors and their suppressive effect on the accumulation of galactitol in the rat lens, overview. Substitutions in the C7 OH group enhanced the potency toward ALR2 | Rattus norvegicus |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| D-glucose + NADPH + H+ | Rattus norvegicus | aldose reductase, ALR2 | sorbitol + NADP+ | - |
? | |
| sorbitol + NAD+ | Rattus norvegicus | aldehyde reductase, ALR1 | D-fructose + NADH + H+ | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| lens | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| D-glucose + NADPH + H+ | aldose reductase, ALR2 | Rattus norvegicus | sorbitol + NADP+ | - |
? | |
| sorbitol + NAD+ | aldehyde reductase, ALR1 | Rattus norvegicus | D-fructose + NADH + H+ | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| aldehyde reductase | - |
Rattus norvegicus |
| aldose reductase 2 | - |
Rattus norvegicus |
| ALR1 | - |
Rattus norvegicus |
| ALR2 | - |
Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NAD+ | - |
Rattus norvegicus | |
| NADP+ | - |
Rattus norvegicus | |
| NADPH | - |
Rattus norvegicus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0014 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | epalrestat | |
| 0.0024 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxy-4-phenylcoumarin | |
| 0.0096 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6,7-dihydroxy-4-phenylcoumarin | |
| 0.0125 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | epalrestat | |
| 0.021 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxylcoumarinyl-4-acetic acid | |
| 0.023 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxycoumarin | |
| 0.0245 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxy-4-methylcoumarin | |
| 0.0365 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6,7-dihydroxycoumarin | |
| 0.037 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxy-4-phenylcoumarin | |
| 0.038 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6,7-dihydroxy-4-methylcoumarin | |
| 0.045 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 4-Hydroxycoumarin | |
| 0.046 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxy-6-methoxycoumarin | |
| 0.053 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxylcoumarin-4-acetic acid | |
| 0.056 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6-hydroxy-7-methoxycoumarin | |
| 0.062 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 3-hydroxycoumarin | |
| 0.063 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxylcoumarin-4-acetic acid | |
| 0.064 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6,7-dihydroxy-4-methylcoumarin | |
| 0.066 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6,7-dihydroxy-4-phenylcoumarin | |
| 0.067 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6,7-dihydroxycoumarin | |
| 0.0675 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-methoxycoumarin | |
| 0.074 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxy-6-methoxycoumarin | |
| 0.086 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxycoumarin | |
| 0.09 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxy-4-methylcoumarin | |
| 0.101 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6-hydroxy-7-methoxycoumarin | |
| 0.131 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-methoxycoumarin | |
| 0.142 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 7-hydroxylcoumarinyl-4-acetic acid | |
| 0.156 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6-hydroxycoumarin | |
| 0.171 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 6-hydroxycoumarin | |
| 0.172 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 3-hydroxycoumarin | |
| 0.4 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | 4-Hydroxycoumarin | |
| 0.4 | - |
ALR2, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | coumarin | |
| 0.5 | - |
ALR1, pH not specified in the publication, temperature not specified in the publication | Rattus norvegicus | coumarin | |
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