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Literature summary extracted from
- Sulfation of tibolone metabolites by human postmenopausal liver and small intestinal sulfotransferases (SULTs) (2006), Steroids, 71, 343-351.
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 2.8.2.1 | 2,6-dichloro-4-nitrophenyl phosphate | i.e. DCNP; i.e. DCNP | Homo sapiens |  |
| 2.8.2.4 | 2,6-Dichloro-4-nitrophenol | DCNP | Homo sapiens | |
| 2.8.2.15 | DCNP | - |
Homo sapiens | |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 2.8.2.1 | additional information | - |
additional information | kinetics | Homo sapiens | |
| 2.8.2.1 | 0.00018 | - |
3alpha-tibolone | pH 7.5, 37°C, postmenopausal liver enzyme | Homo sapiens | |
| 2.8.2.1 | 0.00042 | - |
3beta-tibolone | pH 7.5, 37°C, postmenopausal liver enzyme | Homo sapiens | |
| 2.8.2.4 | additional information | - |
additional information | kinetics | Homo sapiens | |
| 2.8.2.4 | 0.00018 | - |
3alpha-tibolone | pH 6.5, 37°C, recombinant SULT1E1 | Homo sapiens | |
| 2.8.2.4 | 0.00048 | - |
3beta-tibolone | pH 6.5, 37°C, recombinant SULT1E1 | Homo sapiens | |
| 2.8.2.15 | additional information | - |
additional information | kinetics | Homo sapiens | |
| 2.8.2.15 | 0.00056 | - |
3beta-tibolone | pH 7.0, 37°C, recombinant SULT1A1 | Homo sapiens | |
| 2.8.2.15 | 0.00079 | - |
3alpha-tibolone | pH 6.0, 37°C, recombinant SULT1A1 | Homo sapiens | |
Metals/Ions
| EC Number | Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|---|
| 2.8.2.1 | Mg2+ | activates | Homo sapiens | |
| 2.8.2.1 | NaCl | activates | Homo sapiens | |
| 2.8.2.4 | Mg2+ | activates | Homo sapiens | |
| 2.8.2.4 | NaCl | activates | Homo sapiens | |
| 2.8.2.15 | Mg2+ | activates | Homo sapiens | |
| 2.8.2.15 | NaCl | activates | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 2.8.2.1 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | Homo sapiens | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | adenosine 3',5'-bisphosphate + 3alpha-sulfooxytibolone O-sulfate | - |
? | |
| 2.8.2.1 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | Homo sapiens | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | adenosine 3',5'-bisphosphate + 3beta-sulfooxytibolone O-sulfate | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | Homo sapiens | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | adenosine 3',5'-bisphosphate + ? | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | Homo sapiens | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | adenosine 3',5'-bisphosphate + ? | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + estrone | Homo sapiens | - |
adenosine 3',5'-bisphosphate + estrone 3-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | Homo sapiens | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | adenosine 3',5'-bisphosphate + 3alpha-hydroxytibolone 3-O-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | Homo sapiens | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | adenosine 3',5'-bisphosphate + 3beta-hydroxytibolone 3-O-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + dehydroepiandrosterone | Homo sapiens | - |
adenosine 3',5'-bisphosphate + dehydroepiandrosterone 3-O-sulfate | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 2.8.2.1 | Homo sapiens | P0DMM9 | SULT1A3 | - |
| 2.8.2.1 | Homo sapiens | P50225 | SULT1A1 | - |
| 2.8.2.4 | Homo sapiens | P49888 | SULT1E1 | - |
| 2.8.2.15 | Homo sapiens | - |
SULT2A1 | - |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 2.8.2.1 | liver | postmenopausal | Homo sapiens | - |
| 2.8.2.1 | small intestine | postmenopausal | Homo sapiens | - |
| 2.8.2.4 | liver | postmenopausal, SULT1E1 | Homo sapiens | - |
| 2.8.2.4 | small intestine | postmenopausal, SULT1E1 | Homo sapiens | - |
| 2.8.2.15 | liver | postmenopausal, SULT2A1 | Homo sapiens | - |
| 2.8.2.15 | small intestine | postmenopausal, SULT2A1 | Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 2.8.2.1 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + 3alpha-sulfooxytibolone O-sulfate | - |
? | |
| 2.8.2.1 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | Homo sapiens | adenosine 3',5'-bisphosphate + 3alpha-sulfooxytibolone O-sulfate | - |
? | |
| 2.8.2.1 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + 3beta-sulfooxytibolone O-sulfate | - |
? | |
| 2.8.2.1 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | Homo sapiens | adenosine 3',5'-bisphosphate + 3beta-sulfooxytibolone O-sulfate | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + ? | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | Homo sapiens | adenosine 3',5'-bisphosphate + ? | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + ? | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | Homo sapiens | adenosine 3',5'-bisphosphate + ? | - |
? | |
| 2.8.2.4 | 3'-phosphoadenylyl sulfate + estrone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + estrone 3-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + 3alpha-hydroxytibolone 3-O-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + 3alpha-hydroxytibolone | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | Homo sapiens | adenosine 3',5'-bisphosphate + 3alpha-hydroxytibolone 3-O-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + 3beta-hydroxytibolone 3-O-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + 3beta-hydroxytibolone | sulfation inactivates the hydroxylated metabolite of tibolone, a synthetic steroid used for the treatment for climacteric symptoms and postmenopausal osteoporosis | Homo sapiens | adenosine 3',5'-bisphosphate + 3beta-hydroxytibolone 3-O-sulfate | - |
? | |
| 2.8.2.15 | 3'-phosphoadenylyl sulfate + dehydroepiandrosterone | - |
Homo sapiens | adenosine 3',5'-bisphosphate + dehydroepiandrosterone 3-O-sulfate | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 2.8.2.1 | SULT1A1 | - |
Homo sapiens |
| 2.8.2.1 | SULT1A3 | - |
Homo sapiens |
| 2.8.2.4 | SULT1E1 | - |
Homo sapiens |
| 2.8.2.15 | SULT2A1 | - |
Homo sapiens |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 2.8.2.1 | 37 | - |
assay at | Homo sapiens |
| 2.8.2.4 | 37 | - |
assay at | Homo sapiens |
| 2.8.2.15 | 37 | - |
assay at | Homo sapiens |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 2.8.2.1 | 7.5 | - |
- |
Homo sapiens |
| 2.8.2.4 | 6.5 | - |
assay at | Homo sapiens |
| 2.8.2.15 | 6 | 7 | assay at | Homo sapiens |
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