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Literature summary for 2.7.1.127 extracted from

  • Schroeder, D.; Rehbach, C.; Seyffarth, C.; Neuenschwander, M.; Kries, J.V.; Windhorst, S.
    Identification of a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A (2013), Biochem. Biophys. Res. Commun., 439, 228-234.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene ITPKA, recombinant expression in Escherichia coli strain BL21 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
7-methylsulfanyl-3-phenyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 55% inhibition at 0.04 mM Homo sapiens
additional information in order to inhibit the metastasis-promoting activity of ITPKA, both its actin bundling and its InsP3kinase activity has to be blocked, inhibitor library screening, overview Homo sapiens
N-(1,2-benzoxazol-3-yl)-4-methylbenzamide 68% inhibition at 0.04 mM, mixed type inhibitor, that is nearly completely taken up by H1299 cells and remains stable after cellular uptake, the compound exhibits a robust stability and a high membrane permeability. The inhibitor provides the possibility to partly inhibit the metastasis-promoting effect of ITPKA in lung tumor cells. Inhibition mechanism of BAMB-4, overview Homo sapiens
N-(4-ethoxyphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide 87% inhibition at 0.04 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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + 1D-myo-inositol 1,4,5-trisphosphate Homo sapiens
-
ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P23677 isozyme/gene ITPKA
-

Purification (Commentary)

Purification (Comment) Organism
recombinant isozyme ITPKA from Escherichia coli strain BL21 by phosphocellulose chromatography and calmodulin affinity chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
carcinoma cell
-
Homo sapiens
-
H-1299 cell
-
Homo sapiens
-
neuron neuron-specific isozyme Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 1D-myo-inositol 1,4,5-trisphosphate
-
Homo sapiens ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate
-
?

Synonyms

Synonyms Comment Organism
inositol-1,4,5-trisphosphate-3-kinase A
-
Homo sapiens
ITPKA
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.017
-
pH 7.5, 30°C, recombinant enzyme Homo sapiens N-(4-ethoxyphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide
0.036
-
pH 7.5, 30°C, recombinant enzyme Homo sapiens 7-methylsulfanyl-3-phenyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one
0.037
-
pH 7.5, 30°C, recombinant enzyme Homo sapiens N-(1,2-benzoxazol-3-yl)-4-methylbenzamide

General Information

General Information Comment Organism
physiological function ectopic expression of the neuron-specific inositol-1,4,5-trisphosphate-3-kinase A in lung cancer cells increases their metastatic potential because the protein exhibits two actin regulating activities. The isozyme ITPKA bundles actin filaments and regulates inositol-1,4,5-trisphosphate (InsP3)-mediated calcium signals by phosphorylating InsP3 Homo sapiens