Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.8.2.20 extracted from

  • Zhou, W.; Wang, Y.; Xie, J.; Geraghty, R.J.
    A fluorescence-based high-throughput assay to identify inhibitors of tyrosylprotein sulfotransferase activity (2017), Biochem. Biophys. Res. Commun., 482, 1207-1212 .
    View publication on PubMed
Search for more literature for 2.8.2.20

Cloned(Commentary)

Cloned (Comment) Organism
gene TPST1, recombinant expression in Spodoptera frugiperda cells using the baculovirus transfection method Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
aurintricarboxylic acid 95% inhibition at 0.02 mM; complete inhibition at 0.02 mM Homo sapiens
fluphenazine
-
 Homo sapiens
guanidinyl-naltrindole di-trifluoroacetate 74% inhibition at 0.02 mM; 77% inhibition at 0.02 mM Homo sapiens
additional information development of a fluorescent peptide assay for TPST2 activity, inhibitor screening using the LOPAC library in a high-throughput screening, overview. The assay method is sensitive, reproducible and can identify valid TPST inhibitors under high-throughput screening (HTS) conditions. Sodium chlorate inhibits TPST activity via competitive inhibition of PAPS synthetases; development of a fluorescent peptide assay for TPST2 activity, inhibitor screening using the LOPAC library in a high-throughput screening, overview. The assay method is sensitive, reproducible and can identify valid TPST inhibitors under high-throughput screening (HTS) conditions. Sodium chlorate inhibits TPST activity via competitive inhibition of PAPS synthetases. Molecular docking using the crystal structure of TPST2 (PDB 3AP1) Homo sapiens
suramin possesses inhibitory properties consistent with a competitive inhibitor of substrate binding, molecular docking reveals a good fit of suramin into the TPST2 substrate-binding pocket, inhibition kinetic mechanism, overview. 96% inhibition at 0.02 mM; possesses inhibitory properties consistent with a competitive inhibitor of substrate binding, molecular docking reveals a good fit of suramin into the TPST2 substrate-binding pocket, inhibition kinetic mechanism, overview. Complete inhibition at 0.02 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information Michaelis-Menten kinetics Homo sapiens
0.002
-
 peptide Y+1 tyrosine pH 6.5, 22°C, recombinant TPST in presence of 0.001 mM suramin Homo sapiens
0.0044
-
 peptide Y+1 tyrosine pH 6.5, 22°C, recombinant TPST Homo sapiens
0.0051
-
 3'-phosphoadenylyl sulfate pH 6.5, 22°C, recombinant TPST Homo sapiens
0.0054
-
 3'-phosphoadenylyl sulfate pH 6.5, 22°C, recombinant TPST in presence of 0.001 mM suramin Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
Golgi membrane TPST is a Golgi-resident type II transmembrane Homo sapiens 139
-

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens O60507
-
-
Homo sapiens O60704
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant TPST1 from Spodoptera frugiperda cells Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3'-phosphoadenylyl sulfate + peptide Y+1 tyrosine
-
 Homo sapiens adenosine 3',5'-bisphosphate + peptide Y+1 tyrosine-O-sulfate
-
 ?
3'-phosphoadenylyl sulfate + peptide Y+1 tyrosine i.e. peptide Glu-Leu-Asp-Tyr-Dap-Gly-Glu-Ala Homo sapiens adenosine 3',5'-bisphosphate + peptide Y+1 tyrosine-O-sulfate
-
 ?
3'-phosphoadenylyl sulfate + protein tyrosine
-
 Homo sapiens adenosine 3',5'-bisphosphate + protein tyrosine-O-sulfate
-
 ?
additional information development of a fluorescent peptide assay, termed TPST2/Y+1 peptide assay, for TPST1 and 2 activity, substrate screening using the LOPAC library in a high-throughput screening, overview Homo sapiens ?
-
-

Synonyms

Synonyms Comment Organism
TPST
-
 Homo sapiens
TPST1
-
 Homo sapiens
TPST2
-
 Homo sapiens
tyrosylprotein sulfotransferase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00045
-
 pH 6.5, 22°C, recombinant TPST1 Homo sapiens aurintricarboxylic acid
0.00046
-
 pH 6.5, 22°C, recombinant TPST1 Homo sapiens aurintricarboxylic acid
0.0014
-
 pH 6.5, 22°C, recombinant TPST1 Homo sapiens suramin
0.0016
-
 pH 6.5, 22°C, recombinant TPST1 Homo sapiens guanidinyl-naltrindole di-trifluoroacetate
0.0024
-
 pH 6.5, 22°C, recombinant TPST1 Homo sapiens guanidinyl-naltrindole di-trifluoroacetate

General Information

General Information Comment Organism
physiological function tyrosylprotein sulfotransferases (TPSTs) are Golgi-resident type II transmembrane proteins that catalyze the transfer of a sulfuryl group from the 3'-phosphoadenosine-5'-phosphosulfate (PAPS) donor to the side chain of select tyrosine residues of proteins translocating the secretory pathway. Proteins with modified sulfotyrosine residues often reside in the extracellular space and participate in protein-protein interactions. TPST-modified proteins are involved in processes such as immune cell trafficking, complement function and coagulation regulation Homo sapiens