Literature summary for 2.8.2.2 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.

Crystallization (Commentary)

Crystallization (Comment)	Organism
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

Protein Variants	Comment	Organism
M137I	site-directed mutagenesis, substrate binding structure, the Ki for androsterone is increased 28.6fold compared to the wild-type enzyme, overview	Homo sapiens
M137K	site-directed mutagenesis, inactive mutant	Homo sapiens
M137K/Y238A	site-directed mutagenesis, inactive mutant	Homo sapiens
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
M137V/Y238A	site-directed mutagenesis, the mutant shows no substrate inhibition by dehydroepiandrosterone	Homo sapiens
M137W	site-directed mutagenesis, substrate binding structure, the Ki for androsterone is increased 11.1fold compared to the wild-type enzyme, overview	Homo sapiens
M137W/Y238A	site-directed mutagenesis, the mutant shows no substrate inhibition by dehydroepiandrosterone	Homo sapiens
V260A	site-directed mutagenesis, a monomeric mutant	Homo sapiens
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
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
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
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

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

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q06520	-	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
dehydroepiandrosterone sulfotransferase	-	Homo sapiens
SULT2A1	-	Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

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