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1-alkyl-2-lyso-sn-glycero-3-phosphocholine acetyltransferase
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acetyl-CoA: lyso-PAF acetyltransferase
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acetyl-CoA:1-alkyl-2-lyso-sn-glycero-3-phosphocholine 2-O-acetyltransferase
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acetyl-CoA:1-O-alkyl-2-lyso-sn-glycero-3-phosphocholine acetyltransferase
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acetyl-CoA:1-O-alkyl-sn-glycero-3-phosphocholine acetyltransferase
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acetyl-CoA:lyso-PAF acetyltransferase
acetyl-CoA:lysoPAF acetyltransferase
acetyl-coenzymeA:lysoPAF acetyltransferase
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acetyltransferase, 1-alkyl-2-lysolecithin
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acetyltransferase, 1-alkylglycerophosphocholine
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acyl-CoA:1-alkyl-sn-glycero-3-phosphocholine acyltransferase
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blood platelet-activating factor acetyltransferase
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lyso-GPC:acetyl CoA acetyltransferase
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lyso-PAF acetyltransferase
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lyso-PAF acetyltransferase:LPC acyltransferase 1
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Lyso-PAF ATC
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inflammatory isoform
Lyso-PAF ATE
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non-inflammatory isoform
lyso-PAF-acetyltransferase
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lyso-PAF:acetyl-CoA acetyltransferase
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lyso-platelet activating factor:acetyl-CoA acetyltransferase
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lyso-platelet-activating factor acetyltransferase
lyso-platelet-activating factor:acetyl-CoA acetyltransferase
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lysoPAF:acetyl CoA acetyltransferase
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PAF acetyltransferase
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platelet-activating factor acylhydrolase
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platelet-activating factor-synthesizing enzyme
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acetyl-CoA:lyso-PAF acetyltransferase
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acetyl-CoA:lyso-PAF acetyltransferase
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acetyl-CoA:lyso-PAF acetyltransferase
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acetyl-CoA:lysoPAF acetyltransferase
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acetyl-CoA:lysoPAF acetyltransferase
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lyso-PAF AT
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lyso-platelet-activating factor acetyltransferase
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lyso-platelet-activating factor acetyltransferase
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1-O-hexadecyl-sn-glycero-3-phosphocholine + acetyl-CoA
1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine + CoA
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lyso-PAF, lyso-platelet-activating factor
PAF, platelet-activating factor
-
?
acetyl-CoA + 1-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
acetyl-CoA + 1-hexadecyl-2-lyso-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-hexadecyl-sn-glycero-3-phosphocholine
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40% higher activity respect to the C18 analogue
-
?
acetyl-CoA + 1-O-alkyl-sn-glycero-3-phosphocholine
?
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-
?
acetyl-CoA + 1-O-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-6-phosphocholine
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final step in remodelling pathway of PAF biosynthesis
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?
acetyl-CoA + 1-octadecyl-2-lyso-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-octadecyl-sn-glycero-3-phosphocholine
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?
acetyl-CoA + acetyl-phosphatidylcholine
?
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-
?
acetyl-CoA + acyl-lyso-glycero-3-phosphocholine
CoA + acetyl-acyl-glycero-3-phosphocholine
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-
?
acetyl-CoA + alk-1-enyl-lyso-glycero-3-phosphoethanolamine
CoA + acetyl-alk-1-enyl-glycero-3-phosphoethanolamine
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-
-
?
acetyl-CoA + alkyl-lyso-glycero-3-phosphoethanolamine
CoA + 2-acetyl-alkyl-glycero-3-phosphoethanolamine
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-
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?
acetyl-CoA + alkyl-lyso-monomethylethanamine
?
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-
?
acetyl-CoA + alkyl-lyso-N',N'-dimethylethanamine
?
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-
?
acetyl-CoA + alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
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alkyl-lyso-sn-glycero-3-phosphocholine is preferred to its saturated counterpart as substrate
-
?
acetyl-CoA + hexadecyl-lyso-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-hexadecyl-sn-glycero-3-phosphocholine
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-
-
?
acetyl-CoA + lyso-phosphatidylcholine
CoA + 2-acetyl-1-acylphosphatidylcholine
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-
-
?
acetyl-CoA + lyso-phosphatidylethanolamine
CoA + 2-acetyl-1-acyl-phosphatidylethanolamine
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-
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?
acetyl-CoA + lyso-platelet activating factor
CoA + platelet activating factor
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?
acetyl-CoA + lyso-platelet-activating factor
?
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-
?
acetyl-CoA + lyso-platelet-activating factor
platelet-activating factor + CoA
acetyl-CoA + octadecyl-lyso-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-octadecyl-sn-glycero-3-phosphocholine
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-
-
?
acetyl-CoA + phosphatidylcholine
?
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?
lyso-platelt activating factor + acetyl-CoA
?
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?
propionyl-CoA + alkyl-lyso-glycero-phosphocholine
CoA + 2-propionyl-1-alkyl-sn-glycero-3-phosphocholine
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?
additional information
?
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enzyme is induced by bacterial endotoxin. The enzyme catalyzes not only biosynthesis of PAF from lyso-PAF but also incorporation of arachidonoyl-CoA to produce PAF precursor membrane glycerophospholipids (lysophosphatidylcholine acyltransferase activity). Under resting conditions, the enzyme prefers arachidonoyl-CoA and contributes to membrane biogenesis. Upon acute inflammatory stimulation with lipopolysaccharide, the activated enzyme utilizes acetyl-CoA more efficiently and produces PAF
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-
?
acetyl-CoA + 1-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
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-
-
-
?
acetyl-CoA + 1-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
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-
-
?
acetyl-CoA + 1-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
substrates are d31-16:0 LPC or d4-lyso-PAF
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-
?
acetyl-CoA + lyso-platelet-activating factor
platelet-activating factor + CoA
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?
acetyl-CoA + lyso-platelet-activating factor
platelet-activating factor + CoA
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?
acetyl-CoA + lyso-platelet-activating factor
platelet-activating factor + CoA
intracellular redox state involved in regulating synthesis of platelet-activating factor (PAF)
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?
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1-O-hexadecyl-sn-glycero-3-phosphocholine + acetyl-CoA
1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine + CoA
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lyso-PAF, lyso-platelet-activating factor
PAF, platelet-activating factor
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?
acetyl-CoA + 1-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
acetyl-CoA + 1-O-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-6-phosphocholine
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final step in remodelling pathway of PAF biosynthesis
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?
acetyl-CoA + lyso-platelet activating factor
CoA + platelet activating factor
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?
acetyl-CoA + lyso-platelet-activating factor
?
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?
acetyl-CoA + lyso-platelet-activating factor
platelet-activating factor + CoA
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?
additional information
?
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enzyme is induced by bacterial endotoxin. The enzyme catalyzes not only biosynthesis of PAF from lyso-PAF but also incorporation of arachidonoyl-CoA to produce PAF precursor membrane glycerophospholipids (lysophosphatidylcholine acyltransferase activity). Under resting conditions, the enzyme prefers arachidonoyl-CoA and contributes to membrane biogenesis. Upon acute inflammatory stimulation with lipopolysaccharide, the activated enzyme utilizes acetyl-CoA more efficiently and produces PAF
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-
?
acetyl-CoA + 1-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
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?
acetyl-CoA + 1-alkyl-sn-glycero-3-phosphocholine
CoA + 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine
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-
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?
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1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine
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irreversible inhibition dependent of both 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine and enzyme concentration
1-O-alkyl-sn-glycero-3-phosphocholine
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inhibition at high concentrations due to its detergent effect
3,4-dichloro-1-(4,5-dichloro-2-methoxyphenyl)-1H-pyrrole-2,5-dione
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3-chloro-1-(3-chloro-4-methoxyphenyl)-4-(2-methoxyphenoxy)-1H-pyrrole-2,5-dione
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3-chloro-1-(4,5-dichloro-2-methoxyphenyl)-4-(2-hydroxyanilino)-1H-pyrrole-2,5-dione
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3-chloro-4-(morpholin-4-yl)-1-(4-phenoxyphenyl)-1H-pyrrole-2,5-dione
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6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
i.e. Trolox, reduces production of platelet-activating factor (PAF) in H2O2-treated HUVEC cells
butyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
80.4% inhibition at 0.02 mM
CaCl2
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10 mM, 46% inhibition
diisopropylfluorophosphate
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EDTA
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1 mM, 47% inhibition
honokiol
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IC50: 0.06 mM, reversible inhibition
lopinavir-r
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remaining activity in human mesangial cells: 76%. By contrast no effect on activity is observed in blood of naiive patients treated with the drug
lysophosphatidylcholine
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inhibition at high concentrations due to its detergent effect
magnolol
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IC50: 0.07 mM, reversible inhibition
methyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
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methyl 4-[3-chloro-2,5-dioxo-4-(4-sulfamoylanilino)-2,5-dihydro-1H-pyrrol-1-yl]benzoate
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N-acetylcysteine
reduces production of platelet-activating factor (PAF) in H2O2-treated HUVEC cells
nordihydroguaiaretic acid
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IC50: 0.06 mM
p-bromophenacyl bromide
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p-chloromercuribenzoate
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palmitoyllyso-glycero-3-phosphocholine
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phenylmethylsulfonyl fluoride
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30% inhibition at 50 mM
propan-2-yl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
95.2% inhibition at 0.02 mM
propan-2-yl 4-(3-chloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
competitively inhibits the lyso-PAFAT activity with acetyl-CoA
propan-2-yl 4-[3-chloro-4-(2-hydroxyanilino)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
83.1% inhibition at 0.02 mM
propan-2-yl 4-[3-chloro-4-(morpholin-4-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
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propyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
85.4% inhibition at 0.02 mM
pyrrolidinecarbodithioic acid
i.e. PDTC, reduces production of platelet-activating factor (PAF) in H2O2-treated HUVEC cells
resveratrol
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0.157 microM, results in 50% inhibition in interleukin 1beta effect on catalytic activity
tenofovir-DF
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remaining activity in human mesangial cells: 32%. By contrast no effect on activity is observed in blood of naiive patients treated with the drug
tyrosol
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0.048 microM, results in 50% inhibition in interleukin 1beta effect on catalytic activity
additional information
500 ml/day of low-fat milk fortified with phytosterols, linoleic and alpha linolenic acids, vitamin C, vitamin E, vitamin A, vitamin B6, vitamin B12, folic acid, magnesium and selenium has no effect on the enzyme activity in vivo
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additional information
identification of LPCAT2-specific inhibitors in order to ameliorate platelet-activating factor-related inflammatory diseases: N-phenylmaleimide derivatives are selected from a 174000-compound library using fluorescence-based high-throughput screening followed by the evaluation of the effects on LPCAT1 and LPCAT2 activities, cell viability, and cellular platelet-activating factor production. The selected compounds have low inhibitory effects on enzyme LPCAT1 activity which is mostly expressed in the lungs where it produces platelet-activating factor, indicating that adverse effects on respiratory functions may be avoided. Structure-activity relationship, overview
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AMP-dependent protein kinase
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bovine serum albumin
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optimal concentration of 1-1.5 mg/ml at short incubation periods and 2-2.5 mg bovine serum albumin/ml during longer incubation periods
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calcium calmodulin-dependent protein kinase
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-
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diethyl maleate
enhanced 3-fold upon treatment with 5 mM H2O2
EDTA
-
isoform Lyso-PAF ATE is activated by 1.4 mM EDTA in assay conditions
H2O2
increased in concentration-dependent manner, fast but transitory activation, concentrations of H2O2 ranging from 1 to 10 mM, maximal effect at 10 mM, maximum reached within 20 min
interleukin 1beta
-
2.5 ng/ml, induces 2fold increase in intracellular platelet activating factor levels against non-stimulated cells, as well as in the specific activity of acetyl-CoA:lyso-PAF acetyltransferase at 3 h. Effect is inhibited in presence of tyrosol or resveratrol
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mitogen-activated protein p38
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MAP kinase p38
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N-formyl-methionyl-leucyl-phenylalanine
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stimulation is dependent on the preincubation of cells with cytochalasin B, addition of tumor necrosis factor increases 50% alkyl-2-acetyl-sn-glycero-3-phosphocholine production
NaF
-
slightly increases activity
additional information
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membrane-permeable oxidants more effective to provoke synthesis of platelet-activating factor (PAF), no effect on synthesis of platelet-activating factor (PAF) observed in cells treated with 10 mM 2,2'-azobis(2-amidinopropane) dihydrochloride or with 5 mM hydrophobic cumen hydroperoxide
-
additional information
membrane-permeable oxidants more effective to provoke synthesis of platelet-activating factor (PAF), no effect on synthesis of platelet-activating factor (PAF) observed in cells treated with 10 mM 2,2'-azobis(2-amidinopropane) dihydrochloride or with 5 mM hydrophobic cumen hydroperoxide
-
additional information
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activated by a phosphorylation mechanism
-
additional information
500 ml/day of low-fat milk fortified with phytosterols, linoleic and alpha linolenic acids, vitamin C, vitamin E, vitamin A, vitamin B6, vitamin B12, folic acid, magnesium and selenium has no effect on the enzyme activity in vivo
-
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0.0171
3,4-dichloro-1-(4,5-dichloro-2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
pH 7.4, 37°C
0.00758
3-chloro-1-(3-chloro-4-methoxyphenyl)-4-(2-methoxyphenoxy)-1H-pyrrole-2,5-dione
Homo sapiens
pH 7.4, 37°C
0.02
3-chloro-1-(4,5-dichloro-2-methoxyphenyl)-4-(2-hydroxyanilino)-1H-pyrrole-2,5-dione
Homo sapiens
pH 7.4, 37°C
0.00116
3-chloro-4-(morpholin-4-yl)-1-(4-phenoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
pH 7.4, 37°C
0.00033
butyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
Homo sapiens
pH 7.4, 37°C
0.06
honokiol
Homo sapiens
-
IC50: 0.06 mM, reversible inhibition
0.07
magnolol
Homo sapiens
-
IC50: 0.07 mM, reversible inhibition
0.0116
methyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
Homo sapiens
pH 7.4, 37°C
0.02
methyl 4-[3-chloro-2,5-dioxo-4-(4-sulfamoylanilino)-2,5-dihydro-1H-pyrrol-1-yl]benzoate
Homo sapiens
pH 7.4, 37°C
0.06
nordihydroguaiaretic acid
Homo sapiens
-
IC50: 0.06 mM
0.00127
propan-2-yl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
Homo sapiens
pH 7.4, 37°C
0.00047
propan-2-yl 4-(3-chloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
Homo sapiens
pH 7.4, 37°C
0.0133
propan-2-yl 4-[3-chloro-4-(2-hydroxyanilino)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
Homo sapiens
pH 7.4, 37°C
0.02
propan-2-yl 4-[3-chloro-4-(morpholin-4-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
Homo sapiens
pH 7.4, 37°C
0.0003
propyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
Homo sapiens
pH 7.4, 37°C
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Lee, T.C.; Vallari, D.S.; Snyder, F.
1-Alkyl-2-lyso-sn-glycero-3-phosphocholine acetyltransferase
Methods Enzymol.
209
396-401
1992
Homo sapiens
brenda
Ninio, E.; Joly, F.; Bessou, G.
Biosynthesis of paf-acether. XI. Regulation of acetyltransferase by enzyme-substrate imbalance
Biochim. Biophys. Acta
963
288-294
1988
Homo sapiens
brenda
Yamazaki, R.; Sugatani, J.; Fujii, I.; Kuroyanagi, M.; Umehara, K.; Ueno, A.; Suzuki, Y.; Miwa, M.
Development of a novel method for determination of acetyl-CoA:1-alkyl-sn-glycero-3-phosphocholine acetyltransferase activity and its application to screening for acetyltransferase inhibitors. Inhibition by magnolol and honokiol from Magnoliae cortex
Biochem. Pharmacol.
47
995-1006
1994
Homo sapiens, Rattus norvegicus
brenda
Garcia, C.; Montero, M.; Alvarez, J.; Sanchez Crespo, M.
Biosynthesis of platelet-activating factor (PAF) induced by chemotactic peptide is modulated at the lyso-PAF:acetyl-CoA acetyltransferase level by calcium transient and phosphatidic acid
J. Biol. Chem.
268
4001-4008
1993
Homo sapiens
brenda
Nomikos, T.N.; Iatrou, C.; Demopoulos, C.A.
Acetyl-CoA:1-O-alkyl-sn-glycero-3-phosphocholine acetyltransferase (lyso-PAF AT) activity in cortical and medullary human renal tissue
Eur. J. Biochem.
270
2992-3000
2003
Homo sapiens
brenda
Owen, J.S.; Baker, P.R.; OFlaherty, J.T.; Thomas, M.J.; Samuel, M.P.; Wooten, R.E.; Wykle, R.L.
Stress-induced platelet-activating factor synthesis in human neutrophils
Biochim. Biophys. Acta
1733
120-129
2005
Homo sapiens
brenda
Tosaki, T.; Sakamoto, H.; Kitahara, J.; Imai, H.; Nakagawa, Y.
Enhancement of acetyl-CoA: 1-O-alkyl-2-lyso-sn-glycero-3-phosphocholine acetyltransferase activity by hydrogen peroxide
Biol. Pharm. Bull.
30
272-278
2007
Homo sapiens, Homo sapiens (Q7L5N7)
brenda
Shindou, H.; Hishikawa, D.; Nakanishi, H.; Harayama, T.; Ishii, S.; Taguchi, R.; Shimizu, T.
A single enzyme catalyzes both platelet-activating factor production and membrane biogenesis of inflammatory cells: cloning and characterization of acetyl-CoA:lyso-PAF acetyltransferase
J. Biol. Chem.
282
6532-6539
2007
Homo sapiens (Q7L5N7), Mus musculus (Q8BYI6)
brenda
Fragopoulou, E.; Iatrou, C.; Demopoulos, C.A.
Characterization of acetyl-CoA:lyso-PAF acetyltransferase of human mesangial cells
Mediators Inflamm.
2005
263-272
2005
Homo sapiens
brenda
Tsoupras, A.B.; Chini, M.; Tsogas, N.; Fragopoulou, E.; Nomikos, T.; Lioni, A.; Mangafas, N.; Demopoulos, C.A.; Antonopoulou, S.; Lazanas, M.C.
Anti-platelet-activating factor effects of highly active antiretroviral therapy (HAART): a new insight in the drug therapy of HIV infection?
AIDS Res. Hum. Retroviruses
24
1079-1086
2008
Homo sapiens
brenda
Egea, L.; Gimenez, R.; Lucia, D.; Modolell, I.; Badia, J.; Baldoma, L.; Aguilar, J.
Increased production of the ether-lipid platelet-activating factor in intestinal epithelial cells infected by Salmonella enteritidis
Biochim. Biophys. Acta
1781
270-276
2008
Homo sapiens
brenda
Detopoulou, P.; Nomikos, T.; Fragopoulou, E.; Antonopoulou, S.; Kotroyiannis, I.; Vassiliadou, C.; Panagiotakos, D.B.; Chrysohoou, C.; Pitsavos, C.; Stefanadis, C.
Platelet activating factor (PAF) and activity of its biosynthetic and catabolic enzymes in blood and leukocytes of male patients with newly diagnosed heart failure
Clin. Biochem.
42
44-49
2009
Homo sapiens
brenda
Ntzouvani, A.; Nomikos, T.; Petrogianni, M.; Dede, V.; Stamatakis, G.; Manios, Y.
Effect of fortified milk on lyso-platelet-activating factor acetyltranferase and lipoprotein-associated phospholipase A2 in hypercholesterolemic adults
Eur. J. Lipid Sci. Technol.
115
142-152
2013
Homo sapiens (Q7L5N7)
-
brenda
Detopoulou, P.; Fragopoulou, E.; Nomikos, T.; Yannakoulia, M.; Stamatakis, G.; Panagiotakos, D.B.; Antonopoulou, S.
The relation of diet with PAF and its metabolic enzymes in healthy volunteers
Eur. J. Nutr.
54
25-34
2015
Homo sapiens
brenda
Tarui, M.; Shindou, H.; Kumagai, K.; Morimoto, R.; Harayama, T.; Hashidate, T.; Kojima, H.; Okabe, T.; Nagano, T.; Nagase, T.; Shimizu, T.
Selective inhibitors of a PAF biosynthetic enzyme lysophosphatidylcholine acyltransferase 2
J. Lipid Res.
55
1386-1396
2014
Homo sapiens (Q7L5N7), Mus musculus (Q8BYI6), Mus musculus
brenda
Vlachogianni, I.C.; Fragopoulou, E.; Stamatakis, G.M.; Kostakis, I.K.; Antonopoulou, S.
Platelet activating factor (PAF) biosynthesis is inhibited by phenolic compounds in U-937 cells under inflammatory conditions
Prostaglandins Other Lipid Mediat.
121
176-183
2015
Homo sapiens
brenda
Gavriil, L.; Detopoulou, M.; Petsini, F.; Antonopoulou, S.; Fragopoulou, E.
Consumption of plant extract supplement reduces platelet activating factor-induced platelet aggregation and increases platelet activating factor catabolism a randomised, double-blind and placebo-controlled trial
Br. J. Nutr.
121
982-991
2019
Homo sapiens
brenda
Argyrou, C.; Vlachogianni, I.; Stamatakis, G.; Demopoulos, C.A.; Antonopoulou, S.; Fragopoulou, E.
Postprandial effects of wine consumption on platelet activating factor metabolic enzymes
Prostaglandins Other Lipid Mediat.
130
23-29
2017
Homo sapiens
brenda