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Literature summary extracted from
- Reprint of in vitro and in vivo evaluation of a 3beta-androsterone derivative as inhibitor of 17beta-hydroxysteroid dehydrogenase type 3 (2015), J. Steroid Biochem. Mol. Biol., 153, 170-178.
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 1.1.1.51 | gene HSD17B3, recombinant expression in HEK-293 cells | Homo sapiens |
| 1.1.1.64 | gene HSD17B3, recombinant expression in HEK-293 cells | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.1.1.51 | (3alpha,5alpha)-3-[(2,5-dimethyl-4-{[2-(trifluoromethyl)phenyl]sulfonyl}piperazin-1-yl)methyl]-3-hydroxyandrostan-17-one | the inhibitor RM-532-105 seems to have difficulties in penetrating inside the testis and is concentrated in the testicular capsule. Therefore it is unable to inhibit the 17bets-HSD3 located inside the testis. At a higher concentration, RM-532-105 significantly decreases the level of testosterone and dihydrotestosterone in rat plasma, in vivo effects of the inhibitor in testis and plasma, detailed overview | Rattus norvegicus |  |
| 1.1.1.51 | 1-[(3R,5S,8R,9S,10S,13S,14S)-10,13-dimethyl-2',17-dioxohexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-3,5'-[1,3]oxazolidin]-3'-yl]-3-(morpholin-4-yl)propan-2-yl cyclohexanecarboxylate | - |
Homo sapiens | |
| 1.1.1.51 | RM-532-105 | - |
Homo sapiens | |
| 1.1.1.64 | (3alpha,5alpha)-3-[(2,5-dimethyl-4-{[2-(trifluoromethyl)phenyl]sulfonyl}piperazin-1-yl)methyl]-3-hydroxyandrostan-17-one | the inhibitor RM-532-105 seems to have difficulties in penetrating inside the testis and is concentrated in the testicular capsule. Therefore it is unable to inhibit the 17bets-HSD3 located inside the testis. At a higher concentration, RM-532-105 significantly decreases the level of testosterone and dihydrotestosterone in rat plasma, in vivo effects of the inhibitor in testis and plasma, detailed overview | Rattus norvegicus | |
| 1.1.1.64 | 1-[(3R,5S,8R,9S,10S,13S,14S)-10,13-dimethyl-2',17-dioxohexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-3,5'-[1,3]oxazolidin]-3'-yl]-3-(morpholin-4-yl)propan-2-yl cyclohexanecarboxylate | - |
Homo sapiens | |
| 1.1.1.64 | RM-532-105 | - |
Homo sapiens | |
Localization
| EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|---|
| 1.1.1.51 | microsome | - |
Rattus norvegicus | - |
- |
| 1.1.1.64 | microsome | - |
Rattus norvegicus | - |
- |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.1.1.51 | testosterone + NADP+ | Rattus norvegicus | - |
androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.51 | testosterone + NADP+ | Homo sapiens | - |
androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.51 | testosterone + NADP+ | Rattus norvegicus Sprague-Dawley | - |
androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.64 | testosterone + NADP+ | Rattus norvegicus | - |
androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.64 | testosterone + NADP+ | Homo sapiens | - |
androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.64 | testosterone + NADP+ | Rattus norvegicus Sprague-Dawley | - |
androstenedione + NADPH + H+ | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.1.1.51 | Homo sapiens | P37058 | - |
- |
| 1.1.1.51 | Rattus norvegicus | O54939 | - |
- |
| 1.1.1.51 | Rattus norvegicus Sprague-Dawley | O54939 | - |
- |
| 1.1.1.64 | Homo sapiens | P37058 | - |
- |
| 1.1.1.64 | Rattus norvegicus | O54939 | - |
- |
| 1.1.1.64 | Rattus norvegicus Sprague-Dawley | O54939 | - |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 1.1.1.51 | testis | - |
Rattus norvegicus | - |
| 1.1.1.64 | testis | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.1.1.51 | testosterone + NADP+ | - |
Rattus norvegicus | androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.51 | testosterone + NADP+ | - |
Homo sapiens | androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.51 | testosterone + NADP+ | - |
Rattus norvegicus Sprague-Dawley | androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.64 | testosterone + NADP+ | - |
Rattus norvegicus | androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.64 | testosterone + NADP+ | - |
Homo sapiens | androstenedione + NADPH + H+ | - |
? | |
| 1.1.1.64 | testosterone + NADP+ | - |
Rattus norvegicus Sprague-Dawley | androstenedione + NADPH + H+ | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.1.1.51 | 17beta-HSD3 | - |
Rattus norvegicus |
| 1.1.1.51 | 17beta-HSD3 | - |
Homo sapiens |
| 1.1.1.51 | 17beta-hydroxysteroid dehydrogenase type 3 | - |
Rattus norvegicus |
| 1.1.1.51 | 17beta-hydroxysteroid dehydrogenase type 3 | - |
Homo sapiens |
| 1.1.1.51 | HSD17B3 | - |
Rattus norvegicus |
| 1.1.1.51 | HSD17B3 | - |
Homo sapiens |
| 1.1.1.64 | 17beta-HSD3 | - |
Rattus norvegicus |
| 1.1.1.64 | 17beta-HSD3 | - |
Homo sapiens |
| 1.1.1.64 | 17beta-hydroxysteroid dehydrogenase type 3 | - |
Rattus norvegicus |
| 1.1.1.64 | 17beta-hydroxysteroid dehydrogenase type 3 | - |
Homo sapiens |
| 1.1.1.64 | HSD17B3 | - |
Rattus norvegicus |
| 1.1.1.64 | HSD17B3 | - |
Homo sapiens |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 1.1.1.51 | 37 | - |
assay at | Rattus norvegicus |
| 1.1.1.64 | 37 | - |
assay at | Rattus norvegicus |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 1.1.1.51 | 7.4 | - |
assay at | Rattus norvegicus |
| 1.1.1.64 | 7.4 | - |
assay at | Rattus norvegicus |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.1.1.51 | NADP+ | - |
Rattus norvegicus | |
| 1.1.1.51 | NADP+ | - |
Homo sapiens | |
| 1.1.1.51 | NADPH | - |
Rattus norvegicus | |
| 1.1.1.51 | NADPH | - |
Homo sapiens | |
| 1.1.1.64 | NADP+ | - |
Rattus norvegicus | |
| 1.1.1.64 | NADP+ | - |
Homo sapiens | |
| 1.1.1.64 | NADPH | - |
Rattus norvegicus | |
| 1.1.1.64 | NADPH | - |
Homo sapiens | |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 1.1.1.51 | metabolism | the enzyme catalyzes the last step in the biosynthesis of the potent androgen testosterone (T), by stereoselectively reducing the C17 ketone of 4-androstene-3,17-dione (4-dione), with NADPH as cofactor | Rattus norvegicus |
| 1.1.1.51 | metabolism | the enzyme catalyzes the last step in the biosynthesis of the potent androgen testosterone (T), by stereoselectively reducing the C17 ketone of 4-androstene-3,17-dione (4-dione), with NADPH as cofactor | Homo sapiens |
| 1.1.1.64 | metabolism | the enzyme catalyzes the last step in the biosynthesis of the potent androgen testosterone (T), by stereoselectively reducing the C17 ketone of 4-androstene-3,17-dione (4-dione), with NADPH as cofactor | Rattus norvegicus |
| 1.1.1.64 | metabolism | the enzyme catalyzes the last step in the biosynthesis of the potent androgen testosterone (T), by stereoselectively reducing the C17 ketone of 4-androstene-3,17-dione (4-dione), with NADPH as cofactor | Homo sapiens |
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