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Literature summary for 2.8.2.1 extracted from

  • Wang, T.; Cook, I.; Leyh, T.S.
    The NSAID allosteric site of human cytosolic sulfotransferases (2017), J. Biol. Chem., 292, 20305-20312 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.8.2.1

Crystallization (Commentary)

Crystallization (Comment) Organism
structure of the Mefenamic acid-binding site of SULT1A1, using spin-label triangulation NMR Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Acetylsalicylic acid
-
 Homo sapiens
Mefenamic acid inhibits SULT1A1 turnover through an indirect (helix-mediated) stabilization of the closed form of the active-site cap of the enzyme, which traps the nucleotide and slows its release. Residues Tyr140, His141, His144, and Trp155 at the binding site directly contact mefenamic acid Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000022
-
 1-hydroxypyrene wild-type, initial rate value, pH 7.5, 25°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P50225 isoform SULT1A1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3'-phosphoadenylyl sulfate + 1-hydroxypyrene
-
 Homo sapiens adenosine 3',5'-bisphosphate + 1-hydroxypyrene sulfate
-
 ?

Synonyms

Synonyms Comment Organism
SULT1A1
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2
-
 1-hydroxypyrene wild-type, initial rate value, pH 7.5, 25°C Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000027
-
 Mefenamic acid wild-type, pH 7.5, 25°C Homo sapiens
0.000044
-
 Mefenamic acid mutant Y140L, pH 7.5, 25°C Homo sapiens
0.000093
-
 Mefenamic acid mutant H144R, pH 7.5, 25°C Homo sapiens
0.00014
-
 Mefenamic acid mutant W155R, pH 7.5, 25°C Homo sapiens
0.000148
-
 Mefenamic acid mutant H141S, pH 7.5, 25°C Homo sapiens
0.00026
-
 Acetylsalicylic acid wild-type, pH 7.5, 25°C Homo sapiens
0.00044
-
 Acetylsalicylic acid mutant W155R, pH 7.5, 25°C Homo sapiens
0.00045
-
 Acetylsalicylic acid mutant Y140L, pH 7.5, 25°C Homo sapiens
0.00556
-
 Acetylsalicylic acid mutant H141S, pH 7.5, 25°C Homo sapiens
0.00751
-
 Acetylsalicylic acid mutant H144R, pH 7.5, 25°C Homo sapiens