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(1-((5-(6-chloro-8-(((2-ethylpyridin-4-yl)methyl)amino)-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxyphenyl)sulfonyl)-piperidin-4-yl)methanol
-
(2-bromo-4,5-dimethoxyphenyl)(6,7-dimethoxyisoquinolin-1-yl)methanone
-
about 80% residual activity at 0.01 mM
1,10-phenanthroline-5,6-dione
-
about 35% residual activity at 0.01 mM
1,6-dimethyl-3-propylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
about 65% residual activity at 0.01 mM
1-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]-2-methylpropan-1-one
-
16% residual activity at 0.01 mM
1-[5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxybenzene-1-sulfonyl]piperidin-4-ol
-
2,3-Dihydroxybenzaldehyde
-
-
2-(3-chlorophenyl)-9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
67% residual activity at 0.01 mM
2-amino-1-(isopropylsulfonyl)-6-benzimidazole phenylketone oxime
-
i.e. enviroxime, inhibitor of the in vitro replication of rhinoviruses and enteroviruses, inhibits hepatitis C virus subgenomic replicon replication
2-[5-(1,3-benzodioxol-5-yl)-1,2,4-oxadiazol-3-yl]pyridine
-
about 18% residual activity at 0.01 mM
3-(3,4-dimethoxyphenyl)-2,5-dimethyl-N-[2-(morpholin-4-yl)ethyl]pyrazolo[1,5-a]pyrimidin-7-amine
3-(3,4-dimethoxyphenyl)-5-methyl-N-[2-(morpholin-4-yl)ethyl]-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-amine
-
31% residual activity at 0.01 mM
3-(3,4-dimethoxyphenyl)-N-[2-(morpholin-4-yl)ethyl]-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-amine
-
41% residual activity at 0.01 mM
3-(4-methylphenyl)-5H-indeno[1,2-c]pyridazin-5-one
-
about 55% residual activity at 0.01 mM
3-(6-chloro-2-methyl-8-[[(2-methylpyridin-4-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
-
3-(6-chloro-2-methyl-8-[[(pyridin-3-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
-
3-(6-chloro-2-methyl-8-[[(pyridin-4-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
-
3-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
-
4-(quinoxalin-2-yl)phenyl furan-2-carboxylate
-
about 75% residual activity at 0.01 mM
4-[9-(3,4-dimethoxyphenyl)-2-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-8-yl]benzonitrile
-
97% residual activity at 0.01 mM
4-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]benzonitrile
-
97% residual activity at 0.01 mM
4-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenol
-
18% residual activity at 0.01 mM
5'-AMP
-
0.5 mM, 10% inhibition
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxy-N,N-dimethylbenzene-1-sulfonamide
-
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxy-N-(2-methoxyethyl)benzene-1-sulfonamide
-
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxy-N-(prop-2-en-1-yl)benzene-1-sulfonamide
-
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxybenzene-1-sulfonyl chloride
-
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-(1-hydroxybutan-2-yl)-2-methoxybenzene-1-sulfonamide
-
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-(2-hydroxyethyl)-2-methoxybenzene-1-sulfonamide
-
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-cyclopropyl-2-methoxybenzene-1-sulfonamide
-
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-[2-(dimethylamino)ethyl]-2-methoxybenzene-1-sulfonamide
-
5-[8-[(2-acetamidoethyl)amino]-6-chloro-2-methylimidazo[1,2-b]pyridazin-3-yl]-2-methoxybenzene-1-sulfonyl chloride
-
6-chloro-3-iodo-2-methyl-N-((2-methylpyridin-4-yl)methyl)-imidazo[1,2-b]pyridazin-8-amine
-
6-chloro-3-iodo-2-methyl-N-(pyridin-2-ylmethyl)imidazo[1,2-b]-pyridazin-8-amine
-
6-chloro-3-iodo-2-methyl-N-(pyridin-3-ylmethyl)imidazo[1,2-b]-pyridazin-8-amine
-
6-chloro-3-iodo-2-methyl-N-(pyridin-4-ylmethyl)imidazo[1,2-b]-pyridazin-8-amine
-
6-chloro-N-((2-ethylpyr idin-4-yl)methyl)-3-iodo-2-methylimidazo[1,2-b]pyridazin-8-amine
-
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-(4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-amine
-
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-[4-methoxy-3-(1H-pyrazole-1-sulfonyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-amine
-
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-[4-methoxy-3-(morpholine-4-sulfonyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-amine
-
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-[4-methoxy-3-(piperidine-1-sulfonyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-amine
-
7-(3,4-dimethoxyphenyl)-N-[2-(morpholin-4-yl)ethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
-
74% residual activity at 0.01 mM
8-(cyclohex-3-en-1-yl)-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
75% residual activity at 0.01 mM
8-bromo-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
17% residual activity at 0.01 mM
8-cyclohexyl-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
79% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2,8-dimethyl-N-[2-(morpholin-4-yl)ethyl]-5,9-dihydro-4H-purin-6-amine
-
14% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-(4-fluorophenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
66% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-ethynyl-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
18% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-iodo-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
33% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-methoxy-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
15% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(3-phenylprop-1-yn-1-yl)-9H-purin-6-amine
-
96% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(propan-2-yl)-9H-purin-6-amine
-
65% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(thiophen-3-yl)-9H-purin-6-amine
-
94% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(trifluoromethyl)-9H-purin-6-amine
-
99% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
26% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-(4-fluorophenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
78% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-iodo-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
38% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-methoxy-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
86% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purine-2-carbonitrile
-
24% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-2-(3-phenylprop-1-yn-1-yl)-9H-purin-6-amine
-
58% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-2-(pyridin-3-yl)-9H-purin-6-amine
-
36% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-2-(thiophen-3-yl)-9H-purin-6-amine
-
46% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
-
13% residual activity at 0.01 mM
9-(3,4-dimethoxyphenyl)-8-methyl-N6-[2-(morpholin-4-yl)ethyl]-9H-purine-2,6-diamine
-
25% residual activity at 0.01 mM
amyloid beta
-
amino acids 1-42, inhibits type II phosphatidylinositol 4-kinase and enhances glutamate toxicity
-
amyloid beta protein
-
pathophysiological concentrations of amyloid beta proteins directly inhibit. Abeta25-35 inhibits in a non-competitive manner. Inhibition by 10 nM Abeta25-35 is reversible
-
arachidonic acid
-
0.5 mg/ml, 91.3% inhibition of mPIK-III
Caffeine
-
6.5 mM, 18% inhibition
cholesterol
-
cholesterol sensitivity of PI4KIIalpha
GDP
-
0.5 mM, 4% inhibition
MDL-860
-
irreversible inhibition. MDL-860 only affects in vivo isoform PI4KB activity
methyl N-[[(4-butyl-2-oxo-2H-1-benzopyran-7-yl)oxy]acetyl]-5-hydroxy-L-tryptophanate
-
-
N'-(4-methoxybenzoyl)pyridine-2-carbohydrazide
-
about 20% residual activity at 0.01 mM
N'-[(4-methoxybenzoyl)oxy]pyridine-2-carboximidamide
-
about 30% residual activity at 0.01 mM
N-(1H-benzimidazol-2-yl)-2-methoxybenzamide
-
about 65% residual activity at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[[5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazol-2-yl]sulfanyl]acetamide
-
about 40% residual activity at 0.01 mM
N-(2-((3-(3-((1H-pyrazol-1-yl)sulfonyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
-
N-(2-((3-(3-(N-(4-aminocyclohexyl)sulfamoyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
-
N-(2-((3-(3-(N-allylsulfamoyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
-
N-(2-((6-chloro-3-(3-((4-(hydroxymethyl)piperidin-1-yl)sulfonyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
-
N-(2-((6-chloro-3-(3-(N,N-dimethylsulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
-
N-(2-((6-chloro-3-(3-(N-(1-hydroxybutan-2-yl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
-
N-(2-((6-chloro-3-(3-(N-(2-(dimethylamino)ethyl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
-
N-(2-((6-chloro-3-(3-(N-(2-hydroxyethyl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
-
N-(2-((6-chloro-3-(3-(N-cyclopropylsulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
-
N-(2-((6-chloro-3-(4-methoxy-3-(morpholinosulfonyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
-
N-(2-((6-chloro-3-(4-methoxy-3-(N-(2-methoxyethyl)sulfamoyl)-phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
-
N-(2-((6-chloro-3-(4-methoxy-3-(N-methyl-N-(2-(methylamino)-ethyl)sulfamoyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)-amino)ethyl)acetamide
-
N-(2-((6-chloro-3-(4-methoxy-3-(piperidin-1-ylsulfonyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
-
N-(2-((6-chloro-3-(4-methoxyphenyl)-2-methylimidazo[1,2-b]-pyridazin-8-yl)amino)ethyl)acetamide
-
N-(2-((6-chloro-3-iodo-2-methylimidazo[1,2-b]pyridazin-8-yl)-amino)ethyl)acetamide
-
N-(4-aminocyclohexyl)-5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxybenzene-1-sulfonamide
-
N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide
-
i.e. PIK93, a phenylthiazole
N-[2-([6-chloro-3-[3-(dimethylsulfamoyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-yl]amino)ethyl]acetamide
-
N-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]acetamide
-
14% residual activity at 0.01 mM
N-[5-[4-(dimethylamino)phenyl]-3-oxo-2,3-dihydro-1H-pyrazol-4-yl]pyridine-2-carboxamide
-
about 95% residual activity at 0.01 mM
N-[[(4-butyl-2-oxo-2H-1-benzopyran-7-yl)oxy]acetyl]-5-hydroxy-L-tryptophan
-
about 20% residual activity at 0.01 mM
N6-dimethylamine-adenosine 5'-triphosphate
-
-
PCMB
-
0.01 mM, 74% inhibition
phosphatidylinositol 4,5-bisphosphate
-
50% inhibition when added in equimolar amounts to phosphatidylinositol
phosphatidylserine
-
0.5 mg/ml, 64.3% inhibition of mPIK-III
propan-2-yl N-[[(4-butyl-2-oxo-2H-1-benzopyran-7-yl)oxy]acetyl]-5-hydroxy-L-tryptophanate
-
-
quercetin
-
IC50: 0.004 mM
resveratrol
inhibition of PtdIns 4-kinase activity by resveratrol/phenylarsine oxide reduces Jurkat cell adhesion to matrigel/fibronectin coated surfaces
sodium cholate
-
inhibits activity of both mPIK-I and mPIK-III
tert-butyl N-[[8-(2-chlorophenyl)-4,5-dihydro[1,3]thiazolo[4,5-h]quinazolin-2-yl]carbamoyl]-beta-alaninate
-
i.e. Inhibitor A
theophylline
-
2 mM, 21% inhibition
Toyocamycin
-
IC50 is 0.0033 mg/ml
Triton X-100
-
inhibits activity of mPIK-I but rather weakly enhances mPIK-III activity
[5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol
[9-(3,4-dimethoxyphenyl)-2-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-8-yl]methanol
-
62% residual activity at 0.01 mM
3-(3,4-dimethoxyphenyl)-2,5-dimethyl-N-[2-(morpholin-4-yl)ethyl]pyrazolo[1,5-a]pyrimidin-7-amine
-
-
3-(3,4-dimethoxyphenyl)-2,5-dimethyl-N-[2-(morpholin-4-yl)ethyl]pyrazolo[1,5-a]pyrimidin-7-amine
-
adenosine
-
-
adenosine
-
IC50: 0.09 mM
adenosine
-
0.5 mM, 67% inhibition
ADP
-
-
ADP
-
0.5 mM, 58% inhibition
ADP
-
inhibition of mPIK-I and mPIK-III
Ca2+
-
inhibits in the presence of Mg2+
Ca2+
-
inhibition depends in Ca2+ concentration
cAMP
-
-
cAMP
-
0.5 mM, 32% inhibition
Phenylarsine oxide
-
0.1 mM, strong imhibition
Phenylarsine oxide
-
partial inhibition at 0.01 mM
PIK93
-
-
PIK93
-
90% inhibition at 250 nM
T-00127-HEV1
-
-
T-00127-HEV1
-
about 80% residual activity at 0.001 mM
Wortmannin
IC50: about 300 nM
Wortmannin
-
0.01 mM, significant inhibition
[5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol
-
i.e. AL-9
[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
additional information
-
some anti-viral molecules are isoform selective phosphatidylinositol 4-kinase inhibitors. Isozymes PI4KIIalpha and PI4KIIbeta are wortmannin-insensitive
-
additional information
-
MDL-860 does not affect in vitro isoform PI4KB activity
-
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1-phosphatidylinositol 4-kinase deficiency
PI4K2A deficiency in an intellectual disability, epilepsy, myoclonus, akathisia syndrome.
22q11 Deletion Syndrome
An association screen of myelin-related genes implicates the chromosome 22q11 PIK4CA gene in schizophrenia.
Adenocarcinoma
Membrane-associated phosphatidylinositol kinase of R3230AC mammary tumors and normal mammary glands and effects of insulin on tumor enzyme activity.
Alzheimer Disease
Effects of Alzheimer's disease-related beta amyloid protein fragments on enzymes metabolizing phosphoinositides in brain.
Alzheimer Disease
Evidence for a selective decrease in type 1 phosphatidylinositol kinase activity in brains of patients with Alzheimer's disease.
Alzheimer Disease
Pathophysiological concentrations of amyloid beta proteins directly inhibit rat brain and recombinant human type II phosphatidylinositol 4-kinase activity.
Alzheimer Disease
Phosphatidylinositol kinase is reduced in Alzheimer's disease.
Alzheimer Disease
Platelet phosphatidylinositol kinase activity is not altered in Alzheimer disease.
Alzheimer Disease
Reduced phosphatidylinositol kinase activity in Alzheimer's disease: effects of age and onset.
Alzheimer Disease
Reductions in brain phosphatidylinositol kinase activities in Alzheimer's disease.
Anemia
A Forward Genetic Screen Targeting the Endothelium Reveals a Regulatory Role for the Lipid Kinase Pi4ka in Myelo- and Erythropoiesis.
Anemia
Red cell membrane phosphatidylinositol kinase activity in hemolytic anemias and myeloproliferative diseases.
Anemia, Hemolytic, Congenital
Red cell membrane phosphatidylinositol kinase activity in hemolytic anemias and myeloproliferative diseases.
Arthrogryposis
Germline recessive mutations in PI4KA are associated with perisylvian polymicrogyria, cerebellar hypoplasia and arthrogryposis.
Breast Neoplasms
Amplification of Chromosome 1q Genes Encoding the Phosphoinositide Signalling Enzymes PI4KB, AKT3, PIP5K1A and PI3KC2B in Breast Cancer.
Breast Neoplasms
Coordinated increase in activities of the signal transduction enzymes PI kinase and PIP kinase in human cancer cells.
Breast Neoplasms
Quercetin down-regulates signal transduction in human breast carcinoma cells.
Breast Neoplasms
Therapeutic targeting of the PI4K2A/PKR lysosome network is critical for misfolded protein clearance and survival in cancer cells.
Breast Neoplasms
Using Phosphatidylinositol Phosphorylation as Markers for Hyperglycemic Related Breast Cancer.
Carcinogenesis
Murine pancreatic ductal adenocarcinoma produced by in vitro transduction of polyoma middle T oncogene into the islets of Langerhans.
Carcinogenesis
Oncogenic KRAS is dependent upon an EFR3A-PI4KA signaling axis for potent tumorigenic activity.
Carcinogenesis
Relationship between phosphatidylinositol 4-phosphate synthesis, membrane organisation and lateral diffusion of PI4KIIalpha at the trans-Golgi Network.
Carcinogenesis
Transforming protein of avian sarcoma virus UR2 is associated with phosphatidylinositol kinase activity: possible role in tumorigenesis.
Carcinoma
Coordinated increase in activities of the signal transduction enzymes PI kinase and PIP kinase in human cancer cells.
Carcinoma
Differential sensitization by orobol in proliferating and quiescent human ovarian carcinoma cells.
Carcinoma
Evidence for tight coupling of gonadotropin-releasing hormone receptors to phosphatidylinositol kinase in plasma membrane from ovarian carcinomas.
Carcinoma
Intracellular signalling: phosphatidylinositol lipid metabolism in cancer cells.
Carcinoma
Linkage of reduction in 1-phosphatidylinositol 4-kinase activity and inositol 1,4,5-trisphosphate concentration in human ovarian carcinoma cells treated with quercetin.
Carcinoma, Hepatocellular
1-Phosphatidylinositol 4-kinase: an enzyme linked with proliferation and malignancy.
Carcinoma, Hepatocellular
Current issues in the regulation of signal transduction.
Carcinoma, Hepatocellular
Enhanced phosphatidylinositol kinase activity is associated with early stages of hepatocarcinogenesis and hepatocellular carcinoma.
Carcinoma, Hepatocellular
Intracellular signalling: phosphatidylinositol lipid metabolism in cancer cells.
Carcinoma, Hepatocellular
The interaction of HAb18G/CD147 with integrin alpha6beta1 and its implications for the invasion potential of human hepatoma cells.
Carcinoma, Hepatocellular
Tuning a cellular lipid kinase activity adapts hepatitis C virus to replication in cell culture.
Cholera
Epidermal growth factor stimulates the production of phosphatidylinositol monophosphate and the breakdown of polyphosphoinositides in A431 cells.
Contracture
Dependence of cyclopiazonic-acid-induced muscle contractures on extracellular Ca2+.
Cutis Laxa
Novel defect in phosphatidylinositol 4-kinase type 2-alpha (PI4K2A) at the membrane-enzyme interface is associated with metabolic cutis laxa.
Deafness
Phosphatidylinositol 4-kinase ? mutations cause nonsyndromic sensorineural deafness and inner ear malformation.
DiGeorge Syndrome
Accurate diagnosis of spinal muscular atrophy and 22q11.2 deletion syndrome using limited deoxynucleotide triphosphates and high-resolution melting.
DiGeorge Syndrome
Association of the PIK4CA schizophrenia-susceptibility gene in adults with the 22q11.2 deletion syndrome.
DiGeorge Syndrome
Failure to confirm association between PIK4CA and psychosis in 22q11.2 deletion syndrome.
Dystonia
Recent genetic advances in early-onset dystonia.
Enterovirus Infections
ACBD3-mediated recruitment of PI4KB to picornavirus RNA replication sites.
Epilepsy
PI4K2A deficiency in an intellectual disability, epilepsy, myoclonus, akathisia syndrome.
Glioblastoma
Chromosomal Instability and Phosphoinositide Pathway Gene Signatures in Glioblastoma Multiforme.
Hemangioma
Induction of tumor formation and cell transformation by polyoma middle T antigen in the absence of Src.
Hepatitis A
ACBD3 interaction with TBC1 domain 22 protein is differentially affected by enteroviral and kobuviral 3A protein binding.
Hepatitis C
Activity-Based Phosphatidylinositol Kinase Probes Detect Changes to Protein-Protein Interactions During Hepatitis C Virus Replication.
Hepatitis C
Anti-Hepatitis C Virus Activity and Toxicity of Type III Phosphatidylinositol-4-Kinase Beta Inhibitors.
Hepatitis C
Discovery of Selective Small Molecule Type III Phosphatidylinositol 4-Kinase Alpha (PI4KIII?) Inhibitors as Anti Hepatitis C (HCV) Agents.
Hepatitis C
Evaluation of phosphatidylinositol-4-kinase III? as a hepatitis C virus drug target.
Hepatitis C
Hepatitis C virus NS5A competes with PI4KB for binding to ACBD3 in a genotype-dependent manner.
Hepatitis C
Hepatitis C Virus Stimulates the Phosphatidylinositol 4-Kinase III Alpha-Dependent Phosphatidylinositol 4-Phosphate Production That Is Essential for Its Replication.
Hepatitis C
Hepatitis C Virus Subverts Human Choline Kinase-? To Bridge Phosphatidylinositol-4-Kinase III? (PI4KIII?) and NS5A and Upregulates PI4KIII? Activation, Thereby Promoting the Translocation of the Ternary Complex to the Endoplasmic Reticulum for Viral Replication.
Hepatitis C
Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase III? (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology.
Hepatitis C
Roles for endocytic trafficking and phosphatidylinositol 4-kinase III alpha in hepatitis C virus replication.
Hepatitis C
The lipid kinase phosphatidylinositol-4 kinase III alpha regulates the phosphorylation status of hepatitis C virus NS5A.
Hepatitis C
The role of the phosphatidylinositol 4-kinase PI4KA in hepatitis C virus-induced host membrane rearrangement.
Hermanski-Pudlak Syndrome
Hermansky-Pudlak syndrome protein complexes associate with phosphatidylinositol 4-kinase type II alpha in neuronal and non-neuronal cells.
Hermanski-Pudlak Syndrome
The WASH complex, an endosomal Arp2/3 activator, interacts with the Hermansky-Pudlak syndrome complex BLOC-1 and its cargo phosphatidylinositol-4-kinase type II?.
Immune System Diseases
Biallelic PI4KA variants cause neurological, intestinal and immunological disease.
Infections
ANXA2 Facilitates Enterovirus 71 Infection by Interacting with 3D Polymerase and PI4KB to Assist the Assembly of Replication Organelles.
Infections
Class III phosphatidylinositol 4-kinase alpha and beta are novel host factor regulators of hepatitis C virus replication.
Infections
Enterovirus 3A facilitates viral replication by promoting PI4KB-ACBD3 interaction.
Infections
Hepatitis C Virus Stimulates the Phosphatidylinositol 4-Kinase III Alpha-Dependent Phosphatidylinositol 4-Phosphate Production That Is Essential for Its Replication.
Infections
Kinases required in hepatitis C virus entry and replication highlighted by small interference RNA screening.
Infections
Modulation of proteolytic polyprotein processing by coxsackievirus mutants resistant to inhibitors targeting phosphatidylinositol-4-kinase III? or oxysterol binding protein.
Infections
Phosphatidylinositol 4-Kinase III? Is Required for Severe Acute Respiratory Syndrome Coronavirus Spike-mediated Cell Entry.
Infections
Tetraspanin CD81 is required for Listeria monocytogenes invasion.
Infections
West Nile virus replication requires fatty acid synthesis but is independent on phosphatidylinositol-4-phosphate lipids.
Influenza, Human
Multiple roles for phosphatidylinositol 4-kinase in biosynthetic transport in polarized Madin-Darby canine kidney cells.
Insulin Resistance
Hepatic deletion of p110α and p85α results in insulin resistance despite sustained IRS1-associated phosphatidylinositol kinase activity.
Intellectual Disability
PI4K2A deficiency in an intellectual disability, epilepsy, myoclonus, akathisia syndrome.
Kidney Diseases
APOL1 C-Terminal Variants May Trigger Kidney Disease through Interference with APOL3 Control of Actomyosin.
Leukemia
Identification of phosphatidylinositol 4-kinase type II beta as HLA class II-restricted target in graft versus leukemia reactivity.
Leukemia
The role of phosphatidylinositol 4-kinase type IIalpha in degranulation of RBL-2H3 cells.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Puncta intended: connecting the dots between autophagy and cell stress networks.
Malaria
Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.
Medulloblastoma
A Sensitized RNA Interference Screen Identifies a Novel Role for the PI3K p110{gamma} Isoform in Medulloblastoma Cell Proliferation and Chemoresistance.
Myeloproliferative Disorders
Red cell membrane phosphatidylinositol kinase activity in hemolytic anemias and myeloproliferative diseases.
Myocardial Ischemia
Association of the phosphatidylinositol signal pathway with prolonged myocardial ischemia.
Myoclonus
PI4K2A deficiency in an intellectual disability, epilepsy, myoclonus, akathisia syndrome.
Neoplasm Metastasis
Identification of genes related to invasion and metastasis in pancreatic cancer by cDNA representational difference analysis.
Neoplasms
1-Phosphatidylinositol 4-kinase: an enzyme linked with proliferation and malignancy.
Neoplasms
A complex between phosphatidylinositol 4 kinase II? and integrin ?3?1 is required for N-glycan sialylation in cancer cells.
Neoplasms
A Forward Genetic Screen Targeting the Endothelium Reveals a Regulatory Role for the Lipid Kinase Pi4ka in Myelo- and Erythropoiesis.
Neoplasms
Aegle marmelos differentially affects hepatic markers of glycolysis, insulin signalling pathway, hypoxia, and inflammation in HepG2 cells grown in fructose versus glucose-rich environment.
Neoplasms
Amplification of Chromosome 1q Genes Encoding the Phosphoinositide Signalling Enzymes PI4KB, AKT3, PIP5K1A and PI3KC2B in Breast Cancer.
Neoplasms
Amplification of signal transduction capacity and down-regulation by drugs.
Neoplasms
Amplified increase in signal transduction activity in cancer cells.
Neoplasms
Analysis of the microarray gene expression for breast cancer progression after the application modified logistic regression.
Neoplasms
Chromosomal Instability and Phosphoinositide Pathway Gene Signatures in Glioblastoma Multiforme.
Neoplasms
Coordinated increase in activities of the signal transduction enzymes PI kinase and PIP kinase in human cancer cells.
Neoplasms
Current issues in the regulation of signal transduction.
Neoplasms
Down-regulation of increased signal transduction capacity in human cancer cells.
Neoplasms
Enhanced phosphatidylinositol kinase activity is associated with early stages of hepatocarcinogenesis and hepatocellular carcinoma.
Neoplasms
Enzymatic synthesis and hydrolysis of [32P]phosphatidylinositol phosphate.
Neoplasms
Membrane-associated phosphatidylinositol kinase of R3230AC mammary tumors and normal mammary glands and effects of insulin on tumor enzyme activity.
Neoplasms
Oncogenic pathways implicated in ovarian epithelial cancer.
Neoplasms
PI4KIIalpha is a novel regulator of tumor growth by its action on angiogenesis and HIF-1alpha regulation.
Neoplasms
Polyoma virus middle tumor antigen stimulates membrane-associated protein kinase C at lower levels than required for phosphatidylinositol kinase activation and neoplastic transformation.
Neoplasms
Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase ?- but not ?-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation.
Neoplasms
Silencing of type II phosphatidylinositol 4-kinase ? stabilizes prostate apoptosis response-4 and induces apoptosis in cancer cells.
Neoplasms
The Many Roles of Type II Phosphatidylinositol 4-Kinases in Membrane Trafficking: New Tricks for Old Dogs.
Neoplasms
Therapeutic targeting of the PI4K2A/PKR lysosome network is critical for misfolded protein clearance and survival in cancer cells.
Neoplasms
Tyrosine phosphorylation is a signal for the trafficking of pp85, an 85-kDa phosphorylated polypeptide associated with phosphatidylinositol kinase activity.
Nervous System Diseases
PI4K2A deficiency in an intellectual disability, epilepsy, myoclonus, akathisia syndrome.
Ovarian Neoplasms
Phosphatidylinositol Kinase Activity in Ovarian Cancer Cells.
Ovarian Neoplasms
Puncta intended: connecting the dots between autophagy and cell stress networks.
Paramyxoviridae Infections
PI4KB on Inclusion Bodies Formed by ER Membrane Remodeling Facilitates Replication of Human Parainfluenza Virus Type 3.
Paraplegia
Biallelic PI4KA variants cause a novel neurodevelopmental syndrome with hypomyelinating leukodystrophy.
Paraplegia
Mouse models for hereditary spastic paraplegia uncover a role of PI4K2A in autophagic lysosome reformation.
Parkinson Disease
Effects of Alzheimer's disease-related beta amyloid protein fragments on enzymes metabolizing phosphoinositides in brain.
Polycystic Kidney Diseases
Overexpression of kidney phosphatidylinositol 4-kinasebeta and phospholipase C(gamma1) proteins in two rodent models of polycystic kidney disease.
Polymicrogyria
Germline recessive mutations in PI4KA are associated with perisylvian polymicrogyria, cerebellar hypoplasia and arthrogryposis.
Psychomotor Agitation
PI4K2A deficiency in an intellectual disability, epilepsy, myoclonus, akathisia syndrome.
Sarcoma
1-Phosphatidylinositol 4-kinase: an enzyme linked with proliferation and malignancy.
Sarcoma
Phosphatidylinositol kinase activity in virus-transformed and nontransformed cells.
Sarcoma, Avian
Elevated phosphatidylinositol kinase activity in Rous sarcoma virus-transformed cells. Lack of evidence for enzyme translocation.
Sarcoma, Avian
Phosphatidylinositol kinase activities in normal and Rous sarcoma virus-transformed cells.
Sarcoma, Avian
Phosphatidylinositol kinase activity in virus-transformed and nontransformed cells.
Sarcoma, Avian
Transforming protein of avian sarcoma virus UR2 is associated with phosphatidylinositol kinase activity: possible role in tumorigenesis.
Spastic Paraplegia, Hereditary
Mouse models for hereditary spastic paraplegia uncover a role of PI4K2A in autophagic lysosome reformation.
Starvation
Microautophagy in the yeast vacuole depends on the activities of phosphatidylinositol 4-kinases, Stt4p and Pik1p.
Starvation
Regulation of phosphatidylinositol 4-kinase from the yeast Saccharomyces cerevisiae by CDP-diacylglycerol.
Triple Negative Breast Neoplasms
Puncta intended: connecting the dots between autophagy and cell stress networks.
Vesicular Stomatitis
Multiple roles for phosphatidylinositol 4-kinase in biosynthetic transport in polarized Madin-Darby canine kidney cells.
Vesicular Stomatitis
Phosphatidylinositol 4-kinasebeta is critical for functional association of rab11 with the Golgi complex.
Vesicular Stomatitis
Protein kinase D regulates vesicular transport by phosphorylating and activating phosphatidylinositol-4 kinase IIIbeta at the Golgi complex.
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0.0000415
(1-((5-(6-chloro-8-(((2-ethylpyridin-4-yl)methyl)amino)-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxyphenyl)sulfonyl)-piperidin-4-yl)methanol
Homo sapiens
pH and temperature not specified in the publication
0.00109
1-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]-2-methylpropan-1-one
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.0000062
1-[5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxybenzene-1-sulfonyl]piperidin-4-ol
Homo sapiens
pH and temperature not specified in the publication
0.00012 - 0.0014
2-amino-1-(isopropylsulfonyl)-6-benzimidazole phenylketone oxime
0.0000337
3-(6-chloro-2-methyl-8-[[(2-methylpyridin-4-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000746 - 0.0001454
3-(6-chloro-2-methyl-8-[[(pyridin-3-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
0.0000264
3-(6-chloro-2-methyl-8-[[(pyridin-4-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000125
3-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.00237
4-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenol
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.0000273
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxy-N,N-dimethylbenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000172
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxy-N-(2-methoxyethyl)benzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000086
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxy-N-(prop-2-en-1-yl)benzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000053
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-(1-hydroxybutan-2-yl)-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000061 - 0.0134
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-(2-hydroxyethyl)-2-methoxybenzene-1-sulfonamide
0.000056
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-cyclopropyl-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.000009 - 0.001128
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-[2-(dimethylamino)ethyl]-2-methoxybenzene-1-sulfonamide
0.000441
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-(4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-amine
Homo sapiens
pH and temperature not specified in the publication
0.0000191
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-[4-methoxy-3-(1H-pyrazole-1-sulfonyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-amine
Homo sapiens
pH and temperature not specified in the publication
0.000176
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-[4-methoxy-3-(morpholine-4-sulfonyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-amine
Homo sapiens
pH and temperature not specified in the publication
0.0000592
6-chloro-N-[(2-ethylpyridin-4-yl)methyl]-3-[4-methoxy-3-(piperidine-1-sulfonyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-amine
Homo sapiens
pH and temperature not specified in the publication
0.0052
8-bromo-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.00091
9-(3,4-dimethoxyphenyl)-2,8-dimethyl-N-[2-(morpholin-4-yl)ethyl]-5,9-dihydro-4H-purin-6-amine
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.00191
9-(3,4-dimethoxyphenyl)-2-ethynyl-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.00299
9-(3,4-dimethoxyphenyl)-2-methoxy-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.00207
9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purine-2-carbonitrile
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.00161
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.00144
9-(3,4-dimethoxyphenyl)-8-methyl-N6-[2-(morpholin-4-yl)ethyl]-9H-purine-2,6-diamine
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.09
adenosine
Homo sapiens
-
IC50: 0.09 mM
0.000024
Cpd 6
Homo sapiens
-
isozyme PI4KIIIbeta, pH and temperature not specified in the publication
-
0.000054
MI14
Homo sapiens
pH and temperature not specified in the publication
0.0001633
N-(2-((3-(3-((1H-pyrazol-1-yl)sulfonyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0000269 - 0.00066
N-(2-((3-(3-(N-(4-aminocyclohexyl)sulfamoyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
0.0000199
N-(2-((3-(3-(N-allylsulfamoyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0000149 - 0.00819
N-(2-((6-chloro-3-(3-((4-(hydroxymethyl)piperidin-1-yl)sulfonyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
0.0000024
N-(2-((6-chloro-3-(3-(N,N-dimethylsulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00000723 - 0.01228
N-(2-((6-chloro-3-(3-(N-(1-hydroxybutan-2-yl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
0.00486 - 0.0935
N-(2-((6-chloro-3-(3-(N-(2-(dimethylamino)ethyl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
0.000022
N-(2-((6-chloro-3-(3-(N-(2-hydroxyethyl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0001058
N-(2-((6-chloro-3-(3-(N-cyclopropylsulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00000098 - 0.048
N-(2-((6-chloro-3-(4-methoxy-3-(morpholinosulfonyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
0.0001348
N-(2-((6-chloro-3-(4-methoxy-3-(N-(2-methoxyethyl)sulfamoyl)-phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0001469 - 0.01707
N-(2-((6-chloro-3-(4-methoxy-3-(N-methyl-N-(2-(methylamino)-ethyl)sulfamoyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)-amino)ethyl)acetamide
0.0001894
N-(2-((6-chloro-3-(4-methoxy-3-(piperidin-1-ylsulfonyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0000157 - 0.000553
N-(4-aminocyclohexyl)-5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxybenzene-1-sulfonamide
0.000019 - 0.0011
N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide
0.000054 - 0.1
N-[2-([6-chloro-3-[3-(dimethylsulfamoyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-yl]amino)ethyl]acetamide
0.00214
N-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]acetamide
Homo sapiens
-
isoform PI4K IIIbeta, pH and temperature not specified in the publication
0.004
quercetin
Homo sapiens
-
IC50: 0.004 mM
0.00045
tert-butyl N-[[8-(2-chlorophenyl)-4,5-dihydro[1,3]thiazolo[4,5-h]quinazolin-2-yl]carbamoyl]-beta-alaninate
Homo sapiens
-
isozyme PI4KIIIalpha, pH and temperature not specified in the publication
0.0003
Wortmannin
Homo sapiens
IC50: about 300 nM
0.00057 - 0.0031
[5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol
0.00012
2-amino-1-(isopropylsulfonyl)-6-benzimidazole phenylketone oxime
Homo sapiens
-
isozyme PI4KIIIbeta, pH and temperature not specified in the publication
0.0014
2-amino-1-(isopropylsulfonyl)-6-benzimidazole phenylketone oxime
Homo sapiens
-
isozyme PI4KIIIalpha, pH and temperature not specified in the publication
0.0000746
3-(6-chloro-2-methyl-8-[[(pyridin-3-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0001454
3-(6-chloro-2-methyl-8-[[(pyridin-3-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl)-N,N-dimethylbenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000061
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-(2-hydroxyethyl)-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0134
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-(2-hydroxyethyl)-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.000009
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-[2-(dimethylamino)ethyl]-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.001128
5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-N-[2-(dimethylamino)ethyl]-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.0000269
N-(2-((3-(3-(N-(4-aminocyclohexyl)sulfamoyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00066
N-(2-((3-(3-(N-(4-aminocyclohexyl)sulfamoyl)-4-methoxyphenyl)-6-chloro-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0000149
N-(2-((6-chloro-3-(3-((4-(hydroxymethyl)piperidin-1-yl)sulfonyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0000438
N-(2-((6-chloro-3-(3-((4-(hydroxymethyl)piperidin-1-yl)sulfonyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00819
N-(2-((6-chloro-3-(3-((4-(hydroxymethyl)piperidin-1-yl)sulfonyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00000723
N-(2-((6-chloro-3-(3-(N-(1-hydroxybutan-2-yl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
Homo sapiens
pH and temperature not specified in the publication
0.01228
N-(2-((6-chloro-3-(3-(N-(1-hydroxybutan-2-yl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)-acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00486
N-(2-((6-chloro-3-(3-(N-(2-(dimethylamino)ethyl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0935
N-(2-((6-chloro-3-(3-(N-(2-(dimethylamino)ethyl)sulfamoyl)-4-methoxyphenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)-ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00000098
N-(2-((6-chloro-3-(4-methoxy-3-(morpholinosulfonyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.048
N-(2-((6-chloro-3-(4-methoxy-3-(morpholinosulfonyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0001469
N-(2-((6-chloro-3-(4-methoxy-3-(N-methyl-N-(2-(methylamino)-ethyl)sulfamoyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)-amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.01707
N-(2-((6-chloro-3-(4-methoxy-3-(N-methyl-N-(2-(methylamino)-ethyl)sulfamoyl)phenyl)-2-methylimidazo[1,2-b]pyridazin-8-yl)-amino)ethyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.0000157
N-(4-aminocyclohexyl)-5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.000553
N-(4-aminocyclohexyl)-5-(6-chloro-8-[[(2-ethylpyridin-4-yl)methyl]amino]-2-methylimidazo[1,2-b]pyridazin-3-yl)-2-methoxybenzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.000019
N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide
Homo sapiens
-
isozyme PI4KIIIbeta, pH and temperature not specified in the publication
0.0011
N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide
Homo sapiens
-
isozyme PI4KIIIalpha, pH and temperature not specified in the publication
0.000054
N-[2-([6-chloro-3-[3-(dimethylsulfamoyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-yl]amino)ethyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.1
N-[2-([6-chloro-3-[3-(dimethylsulfamoyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-yl]amino)ethyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.1
N-[2-([6-chloro-3-[3-(dimethylsulfamoyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-yl]amino)ethyl]acetamide
Homo sapiens
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.00057
[5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol
Homo sapiens
-
isozyme PI4KIIIalpha, pH 7.5, 22°C
0.0031
[5-(4-[[4-(morpholin-4-yl)phenyl]amino]quinazolin-6-yl)furan-2-yl]methanol
Homo sapiens
-
isozyme PI4KIIIbeta, pH 7.5, 22°C
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evolution
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in vertebrates, PtdIns4P is synthesized by four distinct PI4K enzymes that belong to either the type-II or type-III family, each having alpha- and beta-forms. The type-III PI4Ks are relatives of the PI 3-kinase family, while the smaller type-II enzymes form a separate family
malfunction
-
depletion of PI4KIIalpha by siRNA-mediated knockdown reduces Wnt5a-triggered uptake and/or sorting of Fz4-eGFP into EEA1-positive endosomes. This effect is fully rescued by re-expression of siRNA-resistant PI4KIIalpha
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
malfunction
-
PI4KIIalpha knockdown causes enlarged LAMP-1-positive endosomal structures in fixed cells. Acute depletion of phosphatidylinositol 4-phosphate in the Golgi causes accumulation of LIMP-2 in this compartment, and PI4KIIIbeta is responsible for controlling the exit of LIMP-2 from the Golgi. In contrast, depletion of PI4KIIalpha blocks trafficking at a post-Golgi compartment, leading to accumulation of LIMP-2 in enlarged endosomal vesicles. PI4KIIalpha depletion also causes secretion of missorted GBA into the medium, which is attenuated by limiting LIMP-2/GBA exit from the Golgi by PI4KIIIbeta inhibitors, overview
malfunction
-
silencing of isozyme PI4KIIIbeta, but not ofisozyme PI4KIIIa strongly inhibits SARS CoV spike-mediated entry
malfunction
-
silencing of the PI 4-kinase PI4KA leads to abberrant membranous web morphology, and PI4KB silencing inhibits HCV infection, overview. PI4KA silencing-induced membrane clustering depends on HCV polyprotein cleavage but does not require integrity of the endoplasmic reticulum-Golgi secretory pathway
malfunction
-
siRNAs that reduce PI4KA accumulation appear to perturb membranous web formation. Cell viral polyprotein expression results in enhanced cytoplasmic phosphatidylinositol 4-phosphate production. Increased phosphatidylinositol 4-phosphate accumulation following hepatitis C virus protein expression is precluded by silencing the expression of isozyme PI4KA, but not the related isozyme PI4KB. Silencing PI4KA also results in aberrant agglomeration of viral replicase proteins, including NS5A, NS5B, and NS3. NS5A alone, but not other viral proteins, stimulates phosphatidylinositol 4-phosphate production in vivo and enhanced PI4KA kinase activity in vitro
malfunction
-
loss of the PI4K2B allele and underexpression of isoform PI4KIIbeta mRNA are associated with human cancers. Depletion of isoform PI4KIIbeta is sufficient to confer an aggressive invasive phenotype on minimally invasive HeLa and MCF-7 cell lines. Loss of isoform PI4KIIbeta induces the formation of invadopodia and leads to increased exocytic trafficking of membrane type I matrix metalloproteinase
metabolism
-
alterations to phosphatidylinositol 4-kinase expression levels can modulate MAP kinase and Akt signalling, and are important for chemoresistance, tumour angiogenesis and the suppression of apoptosis and metastases
metabolism
-
regulation of the Golgi system and 1-phosphatidyl-1D-myo-inositol 4-phosphate levels involving the enzyme, overview
metabolism
-
the enzyme interacts with hepatitis C virus nonstructural protein 5A
metabolism
-
the enzyme interacts with peroxiredoxin-1, Nedd4-1, and vesicle-mediated transport proteins such as clathrin heavy chain and the pallidin subunit of BLOC-1
physiological function
-
distinct phosphatidylinositol 4-kinases play important roles at multiple steps in the trafficking pathway of the LIMP-2/GBA complex. The phosphatidylinositol 4-kinases control lysosomal delivery of the Gaucher disease enzyme, beta-glucocerebrosidase, overview. Catalytic activity of PI4KIIIbeta in Golgi exit of the LIMP-2/GBA complex, which is followed by PI4KIIalpha-mediated trafficking to lysosomes. PI4KIalpha is involved in post-Golgi trafficking of LIMP-2 along the degradative pathway
physiological function
-
isozyme phosphatidylinositol 4-kinase IIIbeta is required for severe acute respiratory syndrome coronavirus spike-mediated cell entry. PI4P plays an essential role in SARS-CoV spike-mediated entry, which is regulated by the PI4P lipid microenvironment, overview
physiological function
-
isozyme PI4KA plays an essential role in hepatitis C virus membranous webs formation and colocalizes with the hepatitis C virus membranous webs, which show phosphatidylinositol 4-phosphate enrichment, while isozyme PI4KB supports the HCV life cycle but does not localize to or generate phosphatidylinositol 4-phosphate at membranous webs
physiological function
-
key role of isozyme PI4KIIalpha in TGN/endosomal membrane traffic, isozyme PI4KIIalpha regulates Wnt signalling, endosomal sorting of signalling receptors, and promotes adaptor protein recruitment to endosomes and the trans-Golgi network. E3 ubiquitin ligase Itch is a binding partner and regulator of PI4KIIa function. Itch directly associates with and ubiquitinates PI4KIIalpha, and both proteins co-localize on endosomes containing Wnt-activated frizzled 4 receptor. Itch and PI4KIIalpha reciprocally regulate each other
physiological function
-
phosphatidylinositol 4-kinase IIalpha is required for oxysterol binding protein-dependent activation of sphingomyelin synthesis in the Golgi apparatus, overview
physiological function
-
phosphatidylinositol 4-kinases regulate vesicle mediate export from the Golgi apparatus via phosphatidylinositol 4-phosphate binding effector proteins that control vesicle budding reactions and regulate membrane dynamics. Function of phosphatidylinositol 4-phosphate at the Golgi Membrane biogenesis and lipid homeostasis
physiological function
-
PI4KIIalpha recruits clathrin adaptors AP1, AP3 and GGAs to the trans-Golgi network, and controls fate of endocytic vesicles, PI4KIIalpha promotes EGF receptor degradation, and supports Wnt signaling. PI4KIIIbeta regulates exit of certain cargos from the Golgi, and supports CERT-mediated ceramide transport to the trans-Golgi. PI4KIIIalpha supplies PtdIns(4,5)P2 for the plasma membrane and regulates the endoplasmic reticulum exit. Phosphatidylinositide 4-phosphate lipids are involved in viral replications. They can be used as replication platforms in the host membranes that are hijacked by RNA viruses including the endoplasmic reticulum, Golgi apparatus, trans-Golgi network, endosomes, plasma membrane and mitochondrial outer membrane. Viral replication machinery is assembled on these platforms as a supramolecular complex and PtdIns4P lipids regulate viral RNA synthesis, detailed overview. Throughout infection, the viral replication membrane platforms contain high levels of the host enzyme phosphatidylinositol 4-kinase IIIbeta, PI4KIIIbeta, that generates PtdIns4P at these membranes. PI4KIIIbeta or PI4KIIIalpha, independently from making PtdIns4P lipids, can also serve as scaffolds to recruit other host proteins to the replication platform
physiological function
-
PI4KIIIalpha is a host factor for hepatitis C virus. Isozyme PI4KIIIbet is involved in the entry of SARS coronavirus. PI4KIIIbeta is not required for virus binding and internalization, but plays a role at, or before, virus fusion with the late endosomes. Modes of recruitment of PI4KIIIs to the replication complexes of hepattis C virus, enteroviruses, and the Aichi virus, overview
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
physiological function
-
PI4KIIIbeta localised to the Golgi complex through GTP-bound Arf1 binding, can be activated by protein kinase D phosphorylation, and also through interactions with neuronal calcium sensor 1. 1-Phosphatidyl-1D-myo-inositol 4-phosphate PI4P is an essential phospholipid substrate for two phosphoinositide-dependent signalling pathways that control cell migration and proliferation. It induces expression of Girdin in several cancers, and its translocation to the plasma membrane where it activates heterotrimeric Gai proteins to stimulate PI(3,4,5)P3 synthesis by PI 3-kinase, overview. The enzyme shows a potential role for a plasma membrane pool of PI4P in regulating Girdin targeting and EGFR signalling. PI4KIIIa may have an underappreciated function in the constitutive chemoresistance of cancers which are recalcitrant to apoptotic induction. PI4KIIbeta isoform migh exhibit an anti-metastatic role in hepatocellular carcinoma
physiological function
-
whereas the palmitoylated membrane-bound pool is catalytically active, the cytosolic kinase is inactive
physiological function
-
the enzyme is associated with actin cytoskeleton and cell adhesion, required for CD3 receptor induced calcium release, and a key component in early T cell activation signaling cascades
physiological function
-
isoform PI4KIIbeta synthesizes a pool of 1-phosphatidyl-1D-myo-inositol 4-phosphate that maintains membrane type I matrix metalloproteinase traffic in the degradative pathway and suppresses the formation of invadopodia
additional information
-
hepatitis C virus stimulates the phosphatidylinositol 4-kinase III alpha-dependent phosphatidylinositol 4-phosphate production that is essential for its replication, overview. PI4KA is also implicated in HCV replication complex formation
additional information
-
molecular chaperone Hsp90 is a binding partner of isozyme PI4KIIbeta, PI4KIIbeta contains an Hsp90 interaction site, which most likely resides in the N-terminal lobe of the catalytic domain. PI4KIIbeta must bind to Hsp90 and is highly sensitive to its release, perhaps because a substantial portion of this isoform is cytosolic. Hsp90 selectively stabilizes the cytosolic pool of PI4KIIbeta.. Hsp90 protects PI4KIIbeta from degradation by the proteasome. Geldanamycin, a specific Hsp90 inhibitor, disrupts the Hsp90-PI4KIIbeta interaction and destabilizes PI4KIIbeta, reducing its half-life by 40% and increasing its susceptibility to ubiquitylation and proteasomal degradation. Cytosolic PI4KIIbeta is much more sensitive to geldanamycin treatment than is the integrally membrane-associated species. Stimuli such as PDGF receptor activation that also induce recruitment of the kinase to membranes disrupt the Hsp90-PI4KIIbeta interaction to a similar extent as inhibitor treatment. Dissociation of PI4KIIbeta from Hsp90 by exposure to geldanamycin results in transient translocation to membranes and increased kinase activity
additional information
-
PI4KA interacts with viral protein NS5A in hepatitis C virus-infected cells
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Walker, D.H.; Dougherty, N.; Pike, L.J.
Purification and characterization of a phosphatidylinositol kinase from A431 cells
Biochemistry
27
6504-6511
1988
Homo sapiens
brenda
Vogel, S.; Hoppe, J.
Polyamines stimulate the phosphorylation of phosphatidylinositol in membranes from A431 cells
Eur. J. Biochem.
154
253-257
1986
Homo sapiens
brenda
Graziani, A.; Ling, L.E.; Endemann, G.; Carpenter, C.L.; Cantley, L.C.
Purification and characterization of human erythrocyte phosphatidylinositol 4-kinase. Phosphatidylinositol 4-kinase and phosphatidylinositol 3-monophosphate 4-kinase are distinct enzymes
Biochem. J.
284
39-45
1992
Homo sapiens
-
brenda
Nishioka, H.; Sawa, T.; Hamada, M.; Shimura, N.; Imoto, M.; Umezawa, K.
Inhibition of phosphatidylinositol kinase by toyocamycin
J. Antibiot.
43
1586-1589
1990
Homo sapiens
brenda
Suga, K.; Kambayashi, J.; Tsujinaka, T.; Sakon, M.; Mori, T.
Properties of phosphatidylinositol kinase of human platelets
Biochem. Int.
15
769-777
1987
Homo sapiens
brenda
Buckley, J.T.
Properties of human erythrocyte phosphatidylinositol kinase and inhibition by adenosine, ADP and related compounds
Biochim. Biophys. Acta
498
1-9
1977
Homo sapiens
brenda
Jenkins, G.H.; Subrahmanyam, G.; Anderson, R.A.
Purification and reconstitution of phosphatidylinositol 4-kinase from human erythrocytes
Biochim. Biophys. Acta
1080
11-18
1991
Homo sapiens
brenda
Wetzker, R.; Klinger, R.; Hsuan, J.; Fry, M.J.; Kauffmann-Zeh, A.; Mller, E.; Frunder, H.; Waterfield, M.
Purification and characterization of phosphatidylinositol 4-kinase from human erythrocyte membranes
Eur. J. Biochem.
200
179-185
1991
Homo sapiens
brenda
Kanoh, H.; Banno, Y.; Hirata, M.; Nozawa, Y.
Partial purification and characterization of phosphatidylinositol kinases from human platelets
Biochim. Biophys. Acta
1046
120-126
1990
Homo sapiens
brenda
Heilmeyer, L.Jr.; Vereb, G.Jr.; Vereb, G.; Kakuk, A.; Szivak, I.
Mammalian phosphatidylinositol 4-kinases
IUBMB Life
55
59-65
2003
Bos taurus, Homo sapiens, Mus musculus, Rattus norvegicus
brenda
Suer, S.; Sickmann, A.; Meyer, H.E.; Herberg, F.W.; Heilmeyer, L.M., Jr.
Human phosphatidylinositol 4-kinase isoform PI4K92. Expression of the recombinant enzyme and determination of multiple phosphorylation sites
Eur. J. Biochem.
268
2099-2106
2001
Homo sapiens (Q9UBF8), Homo sapiens
brenda
Waugh, M.G.; Minogue, S.; Anderson, J.S.; Balinger, A.; Blumenkrantz, D.; Calnan, D.P.; Cramer, R.; Hsuan, J.J.
Localization of a highly active pool of type II phosphatidylinositol 4-kinase in a p97/valosin-containing-protein-rich fraction of the endoplasmic reticulum
Biochem. J.
373
57-63
2003
Homo sapiens
brenda
Wei, Y.J.; Sun, H.Q.; Yamamoto, M.; Wlodarski, P.; Kunii, K.; Martinez, M.; Barylko, B.; Albanesi, J.P.; Yin, H.L.
Type II phosphatidylinositol 4-kinase beta is a cytosolic and peripheral membrane protein that is recruited to the plasma membrane and activated by Rac-GTP
J. Biol. Chem.
277
46586-46593
2002
Homo sapiens (Q8TCG2)
brenda
Balla, A.; Tuymetova, G.; Barshishat, M.; Geiszt, M.; Balla, T.
Characterization of type II phosphatidylinositol 4-kinase isoforms reveals association of the enzymes with endosomal vesicular compartments
J. Biol. Chem.
277
20041-20050
2002
Homo sapiens (Q8TCG2)
brenda
Prajda, N.; Singhal, R.L.; Yeh, Y.A.; Olah, E.; Look, K.Y.; Weber, G.
Linkage of reduction in 1-phosphatidylinositol 4-kinase activity and inositol 1,4,5-trisphosphate concentration in human ovarian carcinoma cells treated with quercetin
Life Sci.
56
1587-1593
1995
Homo sapiens
brenda
Waugh, M.G.; Minogue, S.; Blumenkrantz, D.; Anderson, J.S.; Hsuan, J.J.
Identification and characterization of differentially active pools of type IIalpha phosphatidylinositol 4-kinase activity in unstimulated A431 cells
Biochem. J.
376
497-503
2003
Homo sapiens
brenda
Srivastava, R.; Ratheesh, A.; Gude, R.K.; Rao, K.V.K.; Panda, D.; Subrahmanyam, G.
Resveratrol inhibits type II phosphatidylinositol 4-kinase: A key component in pathways of phosphoinositide turn over
Biochem. Pharmacol.
70
1048-1055
2005
Homo sapiens (Q8TCG2)
brenda
Souza, M.S.; Magnarelli de Potas, G.; Pechen de D'Angelo, A.M.
Organophosphorous and organochlorine pesticides affect human placental phosphoinositides metabolism and PI-4 kinase activity
J. Biochem. Mol. Toxicol.
18
30-36
2004
Homo sapiens
brenda
Wu, B.; Kitagawa, K.; Zhang, N.Y.; Liu, B.; Inagaki, C.
Pathophysiological concentrations of amyloid beta proteins directly inhibit rat brain and recombinant human type II phosphatidylinositol 4-kinase activity
J. Neurochem.
91
1164-1170
2004
Homo sapiens
brenda
Balla, A.; Tuymetova, G.; Tsiomenko, A.; Varnai, P.; Balla, T.
A plasma membrane pool of phosphatidylinositol 4-phosphate is generated by phosphatidylinositol 4-kinase type-III alpha: studies with the PH domains of the oxysterol binding protein and FAPP1
Mol. Biol. Cell
16
1282-1295
2005
Homo sapiens
brenda
Pizarro-Cerda, J.; Payrastre, B.; Wang, Y.J.; Veiga, E.; Yin, H.L.; Cossart, P.
Type II phosphatidylinositol 4-kinases promote Listeria monocytogenes entry into target cells
Cell. Microbiol.
9
2381-2390
2007
Homo sapiens
brenda
Kakuk, A.; Friedlaender, E.; Vereb, G.; Kasa, A.; Balla, A.; Balla, T.; Heilmeyer, L.M.; Gergely, P.; Vereb, G.
Nucleolar localization of phosphatidylinositol 4-kinase PI4K230 in various mammalian cells
Cytometry A
69
1174-1183
2006
Homo sapiens, Rattus norvegicus
brenda
Szivak, I.; Lamb, N.; Heilmeyer, L.M.
Subcellular localization and structural function of endogenous phosphorylated phosphatidylinositol 4-kinase (PI4K92)
J. Biol. Chem.
281
16740-16749
2006
Homo sapiens
brenda
Toth, B.; Balla, A.; Ma, H.; Knight, Z.A.; Shokat, K.M.; Balla, T.
Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi
J. Biol. Chem.
281
36369-36377
2006
Homo sapiens
brenda
Waugh, M.G.; Minogue, S.; Chotai, D.; Berditchevski, F.; Hsuan, J.J.
Lipid and peptide control of phosphatidylinositol 4-kinase IIalpha activity on Golgi-endosomal rafts
J. Biol. Chem.
281
3757-3763
2006
Homo sapiens
brenda
Jeganathan, S.; Lee, J.M.
Binding of elongation factor eEF1A2 to phosphatidylinositol 4-kinase beta stimulates lipid kinase activity and phosphatidylinositol 4-phosphate generation
J. Biol. Chem.
282
372-380
2007
Homo sapiens
brenda
Minogue, S.; Waugh, M.G.; De Matteis, M.A.; Stephens, D.J.; Berditchevski, F.; Hsuan, J.J.
Phosphatidylinositol 4-kinase is required for endosomal trafficking and degradation of the EGF receptor
J. Cell Sci.
119
571-580
2006
Homo sapiens
brenda
Xiong, Z.M.; Kitagawa, K.; Nishiuchi, Y.; Kimura, T.; Inagaki, C.
Protective effects of Abeta-derived tripeptide, Abeta(32-34), on Abeta(1-42)-induced phosphatidylinositol 4-kinase inhibition and neurotoxicity
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419
247-252
2007
Homo sapiens
brenda
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The role of phosphatidylinositol 4-kinases and phosphatidylinositol 4-phosphate during viral replication
Biochem. Pharmacol.
84
1400-1408
2012
Homo sapiens
brenda
Szentpetery, Z.; Szakacs, G.; Bojjireddy, N.; Tai, A.W.; Balla, T.
Genetic and functional studies of phosphatidyl-inositol 4-kinase type IIIalpha
Biochim. Biophys. Acta
1811
476-483
2011
Homo sapiens
brenda
Waugh, M.G.
Phosphatidylinositol 4-kinases, phosphatidylinositol 4-phosphate and cancer
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325
125-131
2012
Homo sapiens
brenda
Moessinger, J.; Wieffer, M.; Krause, E.; Freund, C.; Gerth, F.; Krauss, M.; Haucke, V.
Phosphatidylinositol 4-kinase IIalpha function at endosomes is regulated by the ubiquitin ligase Itch
EMBO Rep.
13
1087-1094
2012
Homo sapiens
brenda
Jung, G.; Barylko, B.; Lu, D.; Shu, H.; Yin, H.; Albanesi, J.P.
Stabilization of phosphatidylinositol 4-kinase type IIbeta by interaction with Hsp90
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286
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2011
Homo sapiens, Rattus norvegicus
brenda
Yang, N.; Ma, P.; Lang, J.; Zhang, Y.; Deng, J.; Ju, X.; Zhang, G.; Jiang, C.
Phosphatidylinositol 4-kinase IIIbeta is required for severe acute respiratory syndrome coronavirus spike-mediated cell entry
J. Biol. Chem.
287
8457-8467
2012
Chlorocebus sabaeus, Homo sapiens
brenda
Berger, K.L.; Kelly, S.M.; Jordan, T.X.; Tartell, M.A.; Randall, G.
Hepatitis C virus stimulates the phosphatidylinositol 4-kinase III alpha-dependent phosphatidylinositol 4-phosphate production that is essential for its replication
J. Virol.
85
8870-8883
2011
Homo sapiens
brenda
Banerji, S.; Ngo, M.; Lane, C.F.; Robinson, C.A.; Minogue, S.; Ridgway, N.D.
Oxysterol binding protein-dependent activation of sphingomyelin synthesis in the Golgi apparatus requires phosphatidylinositol 4-kinase IIalpha
Mol. Biol. Cell
21
4141-4150
2010
Cricetulus griseus, Homo sapiens
brenda
Jovic, M.; Kean, M.J.; Szentpetery, Z.; Polevoy, G.; Gingras, A.C.; Brill, J.A.; Balla, T.
Two phosphatidylinositol 4-kinases control lysosomal delivery of the Gaucher disease enzyme, beta-glucocerebrosidase
Mol. Biol. Cell
23
1533-1545
2012
Homo sapiens
brenda
Tai, A.W.; Salloum, S.
The role of the phosphatidylinositol 4-kinase PI4KA in hepatitis C virus-induced host membrane rearrangement
PLoS ONE
6
e26300
2011
Homo sapiens
brenda
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
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8
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2012
Homo sapiens
brenda
Altan-Bonnet, N.; Balla, T.
Phosphatidylinositol 4-kinases: hostages harnessed to build panviral replication platforms
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2012
Saccharomyces cerevisiae, Homo sapiens
brenda
Graham, T.R.; Burd, C.G.
Coordination of Golgi functions by phosphatidylinositol 4-kinases
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21
113-121
2011
Saccharomyces cerevisiae, Homo sapiens
brenda
Klima, M.; Baumlova, A.; Chalupska, D.; Hrebabecky, H.; Dejmek, M.; Nencka, R.; Boura, E.
The high-resolution crystal structure of phosphatidylinositol 4-kinase IIbeta and the crystal structure of phosphatidylinositol 4-kinase IIalpha containing a nucleoside analogue provide a structural basis for isoform-specific inhibitor design
Acta Crystallogr. Sect. D
71
1555-1563
2015
Homo sapiens (Q8TCG2), Homo sapiens (Q9BTU6)
brenda
Sinha, R.K.; Bojjireddy, N.; Kulkarni, D.; Ratheesh, A.; Chiplunkar, S.V.; Gude, R.; Subrahmanyam, G.
Type II phosphatidylinositol 4-kinase beta is an integral signaling component of early T cell activation mechanisms
Biochimie
95
1560-1566
2013
Homo sapiens
brenda
Baumlova, A.; Chalupska, D.; Rozycki, B.; Jovic, M.; Wisniewski, E.; Klima, M.; Dubankova, A.; Kloer, D.P.; Nencka, R.; Balla, T.; Boura, E.
The crystal structure of the phosphatidylinositol 4-kinase IIalpha
EMBO Rep.
15
1085-1092
2014
Homo sapiens (Q9BTU6)
brenda
Rutaganira, F.U.; Fowler, M.L.; McPhail, J.A.; Gelman, M.A.; Nguyen, K.; Xiong, A.; Dornan, G.L.; Tavshanjian, B.; Glenn, J.S.; Shokat, K.M.; Burke, J.E.
Design and structural characterization of potent and selective inhibitors of phosphatidylinositol 4 kinase IIIbeta
J. Med. Chem.
59
1830-1839
2016
Homo sapiens
brenda
Harak, C.; Radujkovic, D.; Taveneau, C.; Reiss, S.; Klein, R.; Bressanelli, S.; Lohmann, V.
Mapping of functional domains of the lipid kinase phosphatidylinositol 4-kinase type III alpha involved in enzymatic activity and hepatitis C virus replication
J. Virol.
88
9909-9926
2014
Homo sapiens
brenda
Ryder, P.V.; Vistein, R.; Gokhale, A.; Seaman, M.N.; Puthenveedu, M.A.; Faundez, V.
The WASH complex, an endosomal Arp2/3 activator, interacts with the Hermansky-Pudlak syndrome complex BLOC-1 and its cargo phosphatidylinositol-4-kinase type IIalpha
Mol. Biol. Cell
24
2269-2284
2013
Homo sapiens
brenda
Arita, M.; Dobrikov, G.; Puerstinger, G.; Galabov, A.S.
Allosteric Regulation of Phosphatidylinositol 4-Kinase III Beta by an Antipicornavirus Compound MDL-860
ACS Infect. Dis.
3
585-594
2017
Homo sapiens
brenda
Sala, M.; Koegler, M.; Plackova, P.; Mejdrova, I.; Hrebabecky, H.; Prochazkova, E.; Strunin, D.; Lee, G.; Birkus, G.; Weber, J.; Mertlikova-Kaiserova, H.; Nencka, R.
Purine analogs as phosphatidylinositol 4-kinase IIIbeta inhibitors
Bioorg. Med. Chem. Lett.
26
2706-2712
2016
Homo sapiens
brenda
Mohamed, M.; Gardeitchik, T.; Balasubramaniam, S.; Guerrero-Castillo, S.; Dalloyaux, D.; van Kraaij, S.; Venselaar, H.; Hoischen, A.; Urban, Z.; Brandt, U.; Al-Shawi, R.; Simons, J.P.; Frison, M.; Ngu, L.H.; Callewaert, B.; Spelbrink, H.; Kallemeijn, W.W.; Aerts, J.M.F.G.; Waugh, M.G.; Morava, E.; We, W.e.v.
Novel defect in phosphatidylinositol 4-kinase type 2-alpha (PI4K2A) at the membrane-enzyme interface is associated with metabolic cutis laxa
J. Inherit. Metab. Dis.
43
1382-1391
2020
Homo sapiens
brenda
Sengupta, N.; Jovic, M.; Barnaeva, E.; Kim, D.W.; Hu, X.; Southall, N.; Dejmek, M.; Mejdrova, I.; Nencka, R.; Baumlova, A.; Chalupska, D.; Boura, E.; Ferrer, M.; Marugan, J.; Balla, T.
A large scale high-throughput screen identifies chemical inhibitors of phosphatidylinositol 4-kinase type II alpha
J. Lipid Res.
60
683-693
2019
Homo sapiens
brenda
Mejdrova, I.; Chalupska, D.; Plackova, P.; Mueller, C.; Sala, M.; Klima, M.; Baumlova, A.; Hrebabecky, H.; Prochazkova, E.; Dejmek, M.; Strunin, D.; Weber, J.; Lee, G.; Matousova, M.; Mertlikova-Kaiserova, H.; Ziebuhr, J.; Birkus, G.; Boura, E.; Nencka, R.
Rational design of novel highly potent and selective phosphatidylinositol 4-kinase IIIbeta (PI4KB) inhibitors as broad-spectrum antiviral agents and tools for chemical biology
J. Med. Chem.
60
100-118
2017
Homo sapiens, Homo sapiens (Q9UBF8)
brenda
Chalupska, D.; Eisenreichova, A.; Rozycki, B.; Rezabkova, L.; Humpolickova, J.; Klima, M.; Boura, E.
Structural analysis of phosphatidylinositol 4-kinase IIIbeta (PI4KB) - 14-3-3 protein complex reveals internal flexibility and explains 14-3-3 mediated protection from degradation in vitro
J. Struct. Biol.
200
36-44
2017
Homo sapiens (Q9UBF8)
brenda
Alli-Balogun, G.O.; Gewinner, C.A.; Jacobs, R.; Kriston-Vizi, J.; Waugh, M.G.; Minogue, S.
Phosphatidylinositol 4-kinase IIbeta negatively regulates invadopodia formation and suppresses an invasive cellular phenotype
Mol. Biol. Cell
27
4033-4042
2016
Homo sapiens
brenda
Daboussi, L.; Costaguta, G.; Ghukasyan, R.; Payne, G.S.
Conserved role for Gga proteins in phosphatidylinositol 4-kinase localization to the trans-Golgi network
Proc. Natl. Acad. Sci. USA
114
3433-3438
2017
Saccharomyces cerevisiae, Homo sapiens
brenda
Chalupska, D.; Rozycki, B.; Humpolickova, J.; Faltova, L.; Klima, M.; Boura, E.
Phosphatidylinositol 4-kinase IIIbeta (PI4KB) forms highly flexible heterocomplexes that include ACBD3, 14-3-3, and Rab11 proteins
Sci. Rep.
9
567
2019
Homo sapiens (Q9UBF8)
brenda