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Literature summary extracted from

  • Squirewell, E.J.; Qin, X.; Duffel, M.W.
    Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1) (2014), Drug Metab. Dispos., 42, 1843-1850.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.8.2.15 expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.8.2.15 4-hydroxytamoxifen noncompetitive inhibition Homo sapiens
2.8.2.15 endoxifen i.e. 4-hydroxy-N-desmethyltamoxifen, potent noncompetitive inhibition Homo sapiens
2.8.2.15 N-demethyltamoxifen competitive inhibition Homo sapiens
2.8.2.15 tamoxifen N-oxide noncompetitive inhibition Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.8.2.15 3'-phosphoadenylyl sulfate + dehydroepiandrosterone Homo sapiens
-
 adenosine 3',5'-bisphosphate + dehydroepiandrosterone sulfate
-
 ?
2.8.2.15 3'-phosphoadenylyl sulfate + pregnenolone Homo sapiens
-
 adenosine 3',5'-bisphosphate + pregnenolone sulfate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.8.2.15 Homo sapiens Q06520
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.8.2.15 DE-52 column chromatography and hydroxyapatite column chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.8.2.15 3'-phosphoadenylyl sulfate + dehydroepiandrosterone
-
 Homo sapiens adenosine 3',5'-bisphosphate + dehydroepiandrosterone sulfate
-
 ?
2.8.2.15 3'-phosphoadenylyl sulfate + pregnenolone
-
 Homo sapiens adenosine 3',5'-bisphosphate + pregnenolone sulfate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.8.2.15 human hydroxysteroid sulfotransferase 2A1
-
 Homo sapiens
2.8.2.15 SULT2A1
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.8.2.15 0.0028
-
 endoxifen with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens
2.8.2.15 0.0035
-
 endoxifen with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens
2.8.2.15 0.0096
-
 tamoxifen N-oxide with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens
2.8.2.15 0.0098
-
 N-demethyltamoxifen with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens
2.8.2.15 0.0127
-
 4-hydroxytamoxifen with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens
2.8.2.15 0.0169
-
 tamoxifen N-oxide with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens
2.8.2.15 0.0172
-
 N-demethyltamoxifen with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens
2.8.2.15 0.0194
-
 4-hydroxytamoxifen with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.8.2.15 0.0017
-
 with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens endoxifen
2.8.2.15 0.0027
-
 with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens endoxifen
2.8.2.15 0.0083
-
 with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens N-demethyltamoxifen
2.8.2.15 0.01
-
 with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens 4-hydroxytamoxifen
2.8.2.15 0.0111
-
 with dehydroepiandrosterone as substrate, at pH 7.4 and 37°C Homo sapiens tamoxifen N-oxide
2.8.2.15 0.015
-
 with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens N-demethyltamoxifen
2.8.2.15 0.0161
-
 with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens tamoxifen N-oxide
2.8.2.15 0.0167
-
 with pregnenolone as substrate, at pH 7.4 and 37°C Homo sapiens 4-hydroxytamoxifen