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Literature summary for 2.8.2.1 extracted from

  • Rohn, K.J.; Cook, I.T.; Leyh, T.S.; Kadlubar, S.A.; Falany, C.N.
    Potent inhibition of human sulfotransferase 1A1 by 17alpha-ethinylestradiol: role of 3-phosphoadenosine 5-phosphosulfate binding and structural rearrangements in regulating inhibition and activity (2012), Drug Metab. Dispos., 40, 1588-1595.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli as fusion protein with maltose-binding protein Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
17alpha-ethinylestradiol potent inhibitor, 17alpha-ethinylestradiol binds and inhibits isoform SULT1A1 activity toward 4-nitrophenol and 2-naphthol at low nanomolar concentrations, whereas the compound is not sulfated until significantly higher concentrations are reached Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0024
-
17beta-estradiol pH not specified in the publication, at 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3'-phosphoadenylyl sulfate + 17alpha-ethinylestradiol Homo sapiens
-
?
-
?
3'-phosphoadenylyl sulfate + 17beta-estradiol Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
DEAE-Sepharose column chromatography and amylose affinity column chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3'-phosphoadenylyl sulfate + 17alpha-ethinylestradiol
-
Homo sapiens ?
-
?
3'-phosphoadenylyl sulfate + 17beta-estradiol
-
Homo sapiens ?
-
?
3'-phosphoadenylyl sulfate + 4-nitrophenol
-
Homo sapiens adenosine 3',5'-bisphosphate + 4-nitrophenyl sulfate
-
?

Synonyms

Synonyms Comment Organism
sulfotransferase 1A1
-
Homo sapiens
SULT1A1
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000089
-
17alpha-ethinylestradiol for 4-nitrophenol sulfation, pH not specified in the publication, at 37°C Homo sapiens
0.0000149
-
17alpha-ethinylestradiol for 17beta-estradiol sulfation, pH not specified in the publication, at 37°C Homo sapiens
0.000019
-
17alpha-ethinylestradiol for 2-naphthol sulfation, pH not specified in the publication, at 37°C Homo sapiens