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Literature summary for 1.1.1.146 extracted from
- Recent advances in the study of 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) inhibitors (2017), Environ. Toxicol. Pharmacol., 52, 47-53 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane | - |
Homo sapiens |  |
| 2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane | - |
Rattus norvegicus | |
| 3-monoglucuronyl-glycyrrhetinic acid | - |
Homo sapiens | |
| 3-monoglucuronyl-glycyrrhetinic acid | - |
Rattus norvegicus | |
| bisphenol A | weak inhibition of isoform 11beta-HSD2, 51.16% inhibition at 0.1 mM | Homo sapiens | |
| bisphenol A | weak inhibition of isoform 11beta-HSD2, 41.61% inhibition at 0.1 mM | Rattus norvegicus | |
| bortezomib | - |
Homo sapiens | |
| butylated hydroxyanisole | highly selective inhibitor of isoform 11beta-HSD2 | Homo sapiens | |
| butylated hydroxyanisole | highly selective inhibitor of isoform 11beta-HSD2 | Rattus norvegicus | |
| danazol | competitive inhibition | Homo sapiens | |
| dibutyltin | - |
Homo sapiens | |
| diethyldithiocarbamate | uncompetitive inhibition of isoform 11beta-HSD2 | Homo sapiens | |
| diphenyltin | - |
Homo sapiens | |
| Disulfiram | potent inhibitor of isoform 11beta-HSD2 | Homo sapiens | |
| fluoxymesterone | potent inhibitor of isoform 11beta-HSD2 | Homo sapiens | |
| glycyrrhetinic acid | - |
Homo sapiens | |
| glycyrrhizin | - |
Homo sapiens | |
| glycyrrhizin | - |
Rattus norvegicus | |
| maneb | - |
Homo sapiens | |
| additional information | not inhibited by perfluorobutane sulfonic acid | Homo sapiens | |
| additional information | not inhibited by perfluorobutane sulfonic acid | Rattus norvegicus | |
| oxymesterone | - |
Homo sapiens | |
| oxymetholone | - |
Homo sapiens | |
| perfluorohexane sulfonate | - |
Homo sapiens | |
| perfluorohexane sulfonate | - |
Rattus norvegicus | |
| perfluorooctane sulfonate | - |
Homo sapiens | |
| perfluorooctane sulfonate | - |
Rattus norvegicus | |
| Perfluorooctanoic acid | - |
Homo sapiens | |
| Perfluorooctanoic acid | - |
Rattus norvegicus | |
| pyrrolidine dithiocarbamate | - |
Homo sapiens | |
| testosterone | - |
Homo sapiens | |
| thiram | potent inhibitor of isoform 11beta-HSD2 | Homo sapiens | |
| tributyltin | - |
Homo sapiens | |
| Triphenyltin | - |
Homo sapiens | |
| zearalenone | selective inhibitor of isoform 11beta-HSD2 | Homo sapiens | |
| zearalenone | selective inhibitor of isoform 11beta-HSD2 | Rattus norvegicus | |
| zineb | - |
Homo sapiens | |
| ziram | - |
Homo sapiens | |
| ziram | - |
Rattus norvegicus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
| microsome | - |
Rattus norvegicus | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| corticosterone + NAD+ | Homo sapiens | - |
11-dehydrocorticosterone + NADH + H+ | - |
? | |
| corticosterone + NAD+ | Rattus norvegicus | - |
11-dehydrocorticosterone + NADH + H+ | - |
? | |
| cortisol + NAD+ | Homo sapiens | - |
cortisone + NADH + H+ | - |
? | |
| cortisol + NAD+ | Rattus norvegicus | - |
cortisone + NADH + H+ | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P80365 | - |
- |
| Rattus norvegicus | A0A1B0GWP2 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HEK-293 cell | - |
Homo sapiens | - |
| JURKAT cell | - |
Homo sapiens | - |
| kidney | - |
Homo sapiens | - |
| kidney | - |
Rattus norvegicus | - |
| placenta | - |
Homo sapiens | - |
| placenta | - |
Rattus norvegicus | - |
| testis | - |
Homo sapiens | - |
| testis | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| corticosterone + NAD+ | - |
Homo sapiens | 11-dehydrocorticosterone + NADH + H+ | - |
? | |
| corticosterone + NAD+ | - |
Rattus norvegicus | 11-dehydrocorticosterone + NADH + H+ | - |
? | |
| cortisol + NAD+ | - |
Homo sapiens | cortisone + NADH + H+ | - |
? | |
| cortisol + NAD+ | - |
Rattus norvegicus | cortisone + NADH + H+ | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| 11beta-HSD2 | - |
Homo sapiens |
| 11beta-HSD2 | - |
Rattus norvegicus |
| 11beta-hydroxysteroid dehydrogenase type 2 | - |
Homo sapiens |
| 11beta-hydroxysteroid dehydrogenase type 2 | - |
Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NAD+ | - |
Homo sapiens | |
| NAD+ | - |
Rattus norvegicus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000000048 | - |
pH and temperature not specified in the publication | Homo sapiens | perfluorooctane sulfonate | |
| 0.000000293 | - |
pH and temperature not specified in the publication | Rattus norvegicus | perfluorooctane sulfonate | |
| 0.0000038 | - |
pH and temperature not specified in the publication | Rattus norvegicus | Perfluorooctanoic acid | |
| 0.00001897 | - |
pH and temperature not specified in the publication | Homo sapiens | perfluorohexane sulfonate | |
| 0.00002441 | - |
pH and temperature not specified in the publication | Homo sapiens | Perfluorooctanoic acid | |
| 0.00006 | - |
pH and temperature not specified in the publication | Homo sapiens | fluoxymesterone | |
| 0.00006287 | - |
pH and temperature not specified in the publication | Rattus norvegicus | perfluorohexane sulfonate | |
| 0.000128 | - |
pH and temperature not specified in the publication | Homo sapiens | Disulfiram | |
| 0.000132 | - |
pH and temperature not specified in the publication | Homo sapiens | thiram | |
| 0.000256 | - |
pH and temperature not specified in the publication | Homo sapiens | glycyrrhetinic acid | |
| 0.00071 | - |
pH and temperature not specified in the publication | Homo sapiens | oxymetholone | |
| 0.00074 | - |
pH and temperature not specified in the publication | Homo sapiens | danazol | |
| 0.000753 | - |
pH and temperature not specified in the publication | Homo sapiens | maneb | |
| 0.00096 | - |
pH and temperature not specified in the publication | Homo sapiens | oxymesterone | |
| 0.00137 | - |
pH and temperature not specified in the publication | Homo sapiens | testosterone | |
| 0.00142 | - |
pH and temperature not specified in the publication | Homo sapiens | diphenyltin | |
| 0.0017 | - |
pH and temperature not specified in the publication | Homo sapiens | diethyldithiocarbamate | |
| 0.0019 | - |
pH and temperature not specified in the publication | Homo sapiens | tributyltin | |
| 0.00195 | - |
pH and temperature not specified in the publication | Homo sapiens | dibutyltin | |
| 0.00319 | - |
pH and temperature not specified in the publication | Homo sapiens | Triphenyltin | |
| 0.0063 | - |
pH and temperature not specified in the publication | Homo sapiens | pyrrolidine dithiocarbamate | |
| 0.01296 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane | |
| 0.01399 | - |
pH and temperature not specified in the publication | Homo sapiens | butylated hydroxyanisole | |
| 0.01481 | - |
pH and temperature not specified in the publication | Homo sapiens | bisphenol A | |
| 0.01939 | - |
pH and temperature not specified in the publication | Rattus norvegicus | bisphenol A | |
| 0.031 | - |
pH and temperature not specified in the publication | Homo sapiens | zineb | |
| 0.05557 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane | |
| 0.06925 | - |
pH and temperature not specified in the publication | Rattus norvegicus | butylated hydroxyanisole | |
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