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Literature summary extracted from

  • Lu, L.Y.; Hsieh, Y.C.; Liu, M.Y.; Lin, Y.H.; Chen, C.J.; Yang, Y.S.
    Identification and characterization of two amino acids critical for the substrate inhibition of human dehydroepiandrosterone sulfotransferase (SULT2A1) (2008), Mol. Pharmacol., 73, 660-668.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.8.2.2 purified recombinant mutants M137I and M137W, hanging drop vapor diffusion method at 18°C, 0.002 ml hanging drops by mixing equal volumes of protein solution and a reservoir solution containing 1.6 M (NH4)2SO4, 100 mM NaCl, and 0.1 M HEPES at pH 7.5, 3-7 days, X-ray diffraction structure determination and analysis at 2.6 and 3.0 A resolution, respectively, modeling Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.8.2.2 M137I site-directed mutagenesis, substrate binding structure, the Ki for androsterone is increased 28.6fold compared to the wild-type enzyme, overview Homo sapiens
2.8.2.2 M137K site-directed mutagenesis, inactive mutant Homo sapiens
2.8.2.2 M137K/Y238A site-directed mutagenesis, inactive mutant Homo sapiens
2.8.2.2 M137V site-directed mutagenesis, substrate binding structure, the Ki for androsterone is increased 5fold and for dehydroepiandrosterone 9fold compared to the wild-type enzyme, overview Homo sapiens
2.8.2.2 M137V/Y238A site-directed mutagenesis, the mutant shows no substrate inhibition by dehydroepiandrosterone Homo sapiens
2.8.2.2 M137W site-directed mutagenesis, substrate binding structure, the Ki for androsterone is increased 11.1fold compared to the wild-type enzyme, overview Homo sapiens
2.8.2.2 M137W/Y238A site-directed mutagenesis, the mutant shows no substrate inhibition by dehydroepiandrosterone Homo sapiens
2.8.2.2 V260A site-directed mutagenesis, a monomeric mutant Homo sapiens
2.8.2.2 V260A/Y238A site-directed mutagenesis, a monomeric mutant, shows increased Ki for dehydroepiandosterone compared to the wild-type enzyme, no inhibition by androsterone Homo sapiens
2.8.2.2 Y238A site-directed mutagenesis, exhibits no substrate inhibition with ADT as substrate, the Ki value of DHEA increases 7.4fold compared with that of wild-type SULT2A1, no inhibition by androsterone Homo sapiens
2.8.2.2 Y238F site-directed mutagenesis, the Ki values of DHEA and ADT for Y238F SULT2A1 mutant increase for approximately 2 to 3fold compared with those of the wild type enzyme Homo sapiens
2.8.2.2 Y238W site-directed mutagenesis, the Ki values of DHEA and ADT for Y238W SULT2A1 mutant increase for approximately 2 to 3fold compared with those of the wild type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.8.2.2 3'-phosphoadenylyl sulfate substrate inhibition of SULT2A1, structure analysis of SULT2A1/DHEA and SULT2A1/PAP or SULT2A1/ADT, overview Homo sapiens
2.8.2.2 androsterone
-
 Homo sapiens
2.8.2.2 dehydroepiandrosterone substrate inhibition of SULT2A1, structure analysis of SULT2A1/DHEA and SULT2A1/PAP or SULT2A1/ADT, overview Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.8.2.2 additional information
-
 additional information substrate binding kinetics Homo sapiens
2.8.2.2 0.0002
-
 androsterone pH 7.0, 25°C, recombinant mutant M137I Homo sapiens
2.8.2.2 0.0007
-
 androsterone pH 7.0, 25°C, recombinant mutant M137V Homo sapiens
2.8.2.2 0.0007
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant Y238W Homo sapiens
2.8.2.2 0.0007
-
 androsterone pH 7.0, 25°C, recombinant mutant Y238W Homo sapiens
2.8.2.2 0.0011
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant Y238F Homo sapiens
2.8.2.2 0.0013
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137I Homo sapiens
2.8.2.2 0.0013
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137W Homo sapiens
2.8.2.2 0.0014
-
 androsterone pH 7.0, 25°C, recombinant wild-type enzyme Homo sapiens
2.8.2.2 0.0014
-
 androsterone pH 7.0, 25°C, recombinant mutant M137I/Y238A Homo sapiens
2.8.2.2 0.0014
-
 androsterone pH 7.0, 25°C, recombinant mutant Y238A Homo sapiens
2.8.2.2 0.0015
-
 androsterone pH 7.0, 25°C, recombinant mutant Y238F Homo sapiens
2.8.2.2 0.0019
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137V Homo sapiens
2.8.2.2 0.002
-
 androsterone pH 7.0, 25°C, recombinant mutant M137W/Y238A Homo sapiens
2.8.2.2 0.0025
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant wild-type enzyme Homo sapiens
2.8.2.2 0.0033
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant Y238A Homo sapiens
2.8.2.2 0.0036
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137I/Y238A Homo sapiens
2.8.2.2 0.0036
-
 androsterone pH 7.0, 25°C, recombinant mutant M137V/Y238A Homo sapiens
2.8.2.2 0.0042
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137V/Y238A Homo sapiens
2.8.2.2 0.0065
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137V/Y238A Homo sapiens
2.8.2.2 0.0096
-
 androsterone pH 7.0, 25°C, recombinant mutant M137W Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.8.2.2 3'-phosphoadenylyl sulfate + androsterone Homo sapiens
-
 adenosine 3',5'-bisphosphate + androsterone 3-sulfate
-
 ?
2.8.2.2 3'-phosphoadenylyl sulfate + dehydroepiandrosterone Homo sapiens
-
 adenosine 3',5'-bisphosphate + dehydroepiandrosterone 3-sulfate
-
 ?

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.8.2.2 3'-phosphoadenylyl sulfate + androsterone
-
 Homo sapiens adenosine 3',5'-bisphosphate + androsterone 3-sulfate
-
 ?
2.8.2.2 3'-phosphoadenylyl sulfate + dehydroepiandrosterone
-
 Homo sapiens adenosine 3',5'-bisphosphate + dehydroepiandrosterone 3-sulfate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.8.2.2 dehydroepiandrosterone sulfotransferase
-
 Homo sapiens
2.8.2.2 SULT2A1
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.8.2.2 25
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.8.2.2 7
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.8.2.2 0.0007
-
 androsterone pH 7.0, 25°C, recombinant wild-type enzyme Homo sapiens
2.8.2.2 0.0012
-
 androsterone pH 7.0, 25°C, recombinant mutant Y238W Homo sapiens
2.8.2.2 0.0022
-
 androsterone pH 7.0, 25°C, recombinant mutant Y238F Homo sapiens
2.8.2.2 0.0038
-
 androsterone pH 7.0, 25°C, recombinant mutant M137W Homo sapiens
2.8.2.2 0.0061
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant wild-type enzyme Homo sapiens
2.8.2.2 0.0071
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137W Homo sapiens
2.8.2.2 0.0078
-
 androsterone pH 7.0, 25°C, recombinant mutant M137V Homo sapiens
2.8.2.2 0.012
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant Y238F Homo sapiens
2.8.2.2 0.015
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant Y238W Homo sapiens
2.8.2.2 0.02
-
 androsterone pH 7.0, 25°C, recombinant mutant M137I Homo sapiens
2.8.2.2 0.036
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137I Homo sapiens
2.8.2.2 0.045
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant Y238A Homo sapiens
2.8.2.2 0.053
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137V Homo sapiens
2.8.2.2 0.159
-
 androsterone pH 7.0, 25°C, recombinant mutant M137I/Y238A Homo sapiens
2.8.2.2 0.17
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137I/Y238A Homo sapiens
2.8.2.2 0.466
-
 dehydroepiandrosterone pH 7.0, 25°C, recombinant mutant M137V/Y238A Homo sapiens