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Literature summary for 2.7.1.67 extracted from

  • Bianco, A.; Reghellin, V.; Donnici, L.; Fenu, S.; Alvarez, R.; Baruffa, C.; Peri, F.; Pagani, M.; Abrignani, S.; Neddermann, P.; De Francesco, R.
    Metabolism of phosphatidylinositol 4-kinase IIIalpha-dependent PI4P is subverted by HCV and is targeted by a 4-anilino quinazoline with antiviral activity (2012), PLoS Pathog., 8, e1002576.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.67

Cloned(Commentary)

Cloned (Comment) Organism
isolated catalytic domain of isozyme PI4KIIIalpha as His-tagged protein in Spodoptera frugiperda Sf9 cells via transfection by recombinant baculovirus Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
[5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol i.e. AL-9, a 4-anilino quinazoline, inhibits purified PI4KIIIalpha and, to a lesser extent, PI4KIIIbeta, and inhibits PI4KIIIalpha in vivo Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
Golgi membrane isozyme PI4KIIIbeta Homo sapiens 139
-
plasma membrane isozyme PI4KIIIalpha Homo sapiens 5886
-

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 + 1-phosphatidyl-1D-myo-inositol Homo sapiens
-
 ADP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged catalytic domain of isozyme PI4KIIIalpha from Sf9 cells by nickel affinity chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
Huh-7.5 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 1-phosphatidyl-1D-myo-inositol
-
 Homo sapiens ADP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
-
 ?

Synonyms

Synonyms Comment Organism
PI4KIIIalpha
-
 Homo sapiens
PI4KIIIbeta
-
 Homo sapiens
type III phosphatidylinositol 4-kinase alpha
-
 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
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
0.00057
-
 isozyme PI4KIIIalpha, pH 7.5, 22°C Homo sapiens [5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol
0.0031
-
 isozyme PI4KIIIbeta, pH 7.5, 22°C Homo sapiens [5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol

General Information

General Information Comment Organism
malfunction hepatitis C virus, by recruiting PI4KIIIa in the RNA replication complex, hijacks phosphatidylinositol-4 phosphate metabolism, ultimately resulting in a markedly altered subcellular distribution of the PI4KIIIalpha product. Antiviral effect of 4-anilino quinazoline compounds is mediated by the inhibition of PI4KIIIalpha and the consequent depletion of 1-phosphatidyl-1D-myo-inositol 4-phosphate required for the HCV membranous web. Inhibition of PI4KIIIalpha by AL-9 induces the formation of large viral NS5A protein clusters Homo sapiens
physiological function PI4KIIIalpha is responsible for the phosphatidylinositol-4 phosphate pool present in the plasma membrane. Antiviral effect of 4-anilino quinazoline compounds is mediated by the inhibition of PI4KIIIalpha and the consequent depletion of 1-phosphatidyl-1D-myo-inositol 4-phosphate required for the HCV membranous web Homo sapiens