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Information on EC 3.1.1.52 - phosphatidylinositol deacylase
for references in articles please use BRENDA:EC3.1.1.52
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EC Tree 3 Hydrolases
3.1 Acting on ester bonds
3.1.1 Carboxylic-ester hydrolases
3.1.1.52 phosphatidylinositol deacylase
The enzyme appears in viruses and cellular organisms
- 3.1.1.52
-
arachidonic
- prostaglandin
-
eicosanoids
-
leukotrienes
-
spla2s
-
platelet-activating
- pyrrophenone
- cpla2gamma
Reaction Schemes
showSynonyms
cpla2alpha, phosphatidylinositol phospholipase a2, group iva cytosolic phospholipase a2alpha, more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
phosphatidylinositol phospholipase A2
-
-
-
-
phospholipase A2, phosphatidylinositol
-
-
-
-
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
1-phosphatidyl-D-myo-inositol + H2O = 1-acylglycerophosphoinositol + a carboxylate
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of carboxylic ester
-
-
-
-
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PATHWAY SOURCE
PATHWAYS
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SYSTEMATIC NAME
IUBMB Comments
1-phosphatidyl-D-myo-inositol 2-acylhydrolase
-
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CAS REGISTRY NUMBER
COMMENTARY
81604-94-6
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
1-acyl-2-arachidonoyl-sn-glycerol-3-phosphoinositol + H2O
1-acylglycerophosphoinositol + arachidonic acid
1-acyl-2-arachidonoyl-sn-glycerol-3-phosphoinositol + H2O
?
-
Substrates: release of arachidonic acid for subsequent metabolic activity in macrophages
Products: -
Products: -
?
1-acyl-2-oleoyl-sn-glycerol 3-phosphate + H2O
1-acylglycerol 3-phosphate + oleic acid
-
Substrates: 32.6% of 1-acyl-2-oleoyl-sn-glycerol-3-phosphorylinositol
Products: -
Products: -
?
1-acyl-2-oleoyl-sn-glycerol-3-phosphocholine + H2O
1-acylglycerol-3-phosphorylcholine + oleic acid
-
Substrates: 62.5% of 1-acyl-2-oleoyl-sn-glycerol-3-phosphorylinositol
Products: -
Products: -
?
1-acyl-2-oleoyl-sn-glycerol-3-phosphoinositol + H2O
1-acylglycerophosphoinositol + oleic acid
-
Substrates: -
Products: -
Products: -
?
1-acyl-2-oleoyl-sn-glycerol-3-phosphorylethanolamine + H2O
1-acylglycerol-3-phosphorylethanolamine + oleic acid
-
Substrates: 25.1% of 1-acyl-2-oleoyl-sn-glycerol-3-phosphorylinositol
Products: -
Products: -
?
1-acyl-2-oleoyl-sn-glycerol-3-phosphorylserine + H2O
1-acylglycerol-3-phosphorylserine + oleic acid
-
Substrates: 21.51% of 1-acyl-2-oleoyl-sn-glycerol-3-phosphorylinositol
Products: -
Products: -
?
1-acyl-2-palmitoyl-sn-glycerol-3-phosphoinositol + H2O
1-acylglycerophosphoinositol + palmitic acid
-
Substrates: -
Products: -
Products: -
?
1-acyl-2-stearoyl-sn-glycerol-3-phosphoinositol + H2O
1-acylglycerophosphoinositol + stearic acid
-
Substrates: -
Products: -
Products: -
?
1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphocholine + H2O
arachidonic acid + 1-palmitoyl-sn-glycero-3-phosphocholine
-
Substrates: 2 min, 37Ā°C (pre-warmed), in presence of 0.5 mg/ml bovine serum albumin and various concentrations of calcium
Products: quantification of release of radio-labelled arachidonic acid
Products: quantification of release of radio-labelled arachidonic acid
?
1-acyl-2-arachidonoyl-sn-glycerol-3-phosphoinositol + H2O
1-acylglycerophosphoinositol + arachidonic acid
-
Substrates: -
Products: -
Products: -
?
1-acyl-2-arachidonoyl-sn-glycerol-3-phosphoinositol + H2O
1-acylglycerophosphoinositol + arachidonic acid
-
Substrates: -
Products: -
Products: -
?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
1-acyl-2-arachidonoyl-sn-glycerol-3-phosphoinositol + H2O
?
-
Substrates: release of arachidonic acid for subsequent metabolic activity in macrophages
Products: -
Products: -
?
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
Ca2+
-
50% of maximal activation at 0.7 +/-0.1 microM (independent of presence of 10 mol% phosphatidylinositol 4,5-biphosphate), 12% less activity in absence of calcium
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
phorbol myristate acetate
-
PMA, 100 nM to cells induces translocation (maximum after 15 min) of enzyme to the Golgi apparatus and release of 4-5% of cell-associated arachidonic acid within 80 min, effect impaired by PKC inhibition and block of protein synthesis
serum
-
10% mouse serum to cells induces immediate translocation (within 60 seconds) of enzyme to the Golgi apparatus and release of 20% of cell-associated arachidonic acid within 80 min, effect depends on ERK and p38/MAPK pathway activation and calcium binding, effect is impaired by block of protein synthesis
-
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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Arthritis, Experimental
Reduction of cPLA2alpha overexpression: an efficient anti-inflammatory therapy for collagen-induced arthritis.
Arthritis, Rheumatoid
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.
Asthma
Cytosolic phospholipase A2 group IVA influence on GM-CSF expression in human lung cells: a pilot study.
Atherosclerosis
Participation of ATP7A in macrophage mediated oxidation of low density lipoprotein.
Bacterial Infections
Critical role of cytosolic phospholipase a2{alpha} in bronchial mucus hyper-secretion in CFTR-deficient mice.
Bone Diseases
An essential role of cytosolic phospholipase A2alpha in prostaglandin E2-mediated bone resorption associated with inflammation.
Bone Resorption
An essential role of cytosolic phospholipase A2alpha in prostaglandin E2-mediated bone resorption associated with inflammation.
Brain Ischemia
Cytosolic phospholipase A2 alpha amplifies early cyclooxygenase-2 expression, oxidative stress and MAP kinase phosphorylation after cerebral ischemia in mice.
Carcinoma, Ehrlich Tumor
Hypotonic cell swelling induces translocation of the alpha isoform of cytosolic phospholipase A2 but not the gamma isoform in Ehrlich ascites tumor cells.
Carcinoma, Non-Small-Cell Lung
Nucleolin regulates c-Jun/Sp1-dependent transcriptional activation of cPLA2alpha in phorbol ester-treated non-small cell lung cancer A549 cells.
Cholangiocarcinoma
A novel positive feedback loop between peroxisome proliferator-activated receptor-delta and prostaglandin E2 signaling pathways for human cholangiocarcinoma cell growth.
Dehydration
Critical role of cytosolic phospholipase a2{alpha} in bronchial mucus hyper-secretion in CFTR-deficient mice.
Lung Neoplasms
Nucleolin regulates c-Jun/Sp1-dependent transcriptional activation of cPLA2alpha in phorbol ester-treated non-small cell lung cancer A549 cells.
Neoplasms
Hypotonic cell swelling induces translocation of the alpha isoform of cytosolic phospholipase A2 but not the gamma isoform in Ehrlich ascites tumor cells.
Neoplasms
Transforming growth factor-beta (TGF-beta) activates cytosolic phospholipase A2alpha (cPLA2alpha)-mediated prostaglandin E2 (PGE)2/EP1 and peroxisome proliferator-activated receptor-gamma (PPAR-gamma)/Smad signaling pathways in human liver cancer cells. A novel mechanism for subversion of TGF-beta-induced mitoinhibition.
Osteoarthritis
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.
Pheochromocytoma
Decrease in cytosolic phospholipase A2alpha mRNA levels by reactive oxygen species via MAP kinase pathways in PC12 cells: effects of dopaminergic neurotoxins.
phosphatidylinositol deacylase deficiency
Cytosolic phospholipase A2alpha is crucial [correction of A2alpha deficiency is crucial] for 'on-time' embryo implantation that directs subsequent development.
phosphatidylinositol deacylase deficiency
Group X secretory phospholipase A2 can induce arachidonic acid release and eicosanoid production without activation of cytosolic phospholipase A2 alpha.
Pneumonia
Critical role of cytosolic phospholipase a2{alpha} in bronchial mucus hyper-secretion in CFTR-deficient mice.
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.39
-
mutant K488N/K543N/K544N, from activated platelets, in presence of 10 mol% phosphatidylinositol 4,5-biphosphate
0.68
-
mutant K271N/K273N/K274N, from activated platelets, in presence of 10 mol% phosphatidylinositol 4,5-biphosphate
0.866
-
phoshorylated at residue S515, from activated platelets, in presence of 10 mol% phosphatidylinositol 4,5-biphosphate
1.03
-
wild-type, from activated platelets, in presence of 10 mol% phosphatidylinositol 4,5-biphosphate
1.45
-
phoshorylated at residue S505, from activated platelets, in presence of 10 mol% phosphatidylinositol 4,5-biphosphate
additional information
-
5fold increase in specific activity of activated platelet-derived wild-type and phosphorylated forms in presence of 10 mol% phosphatidylinositol 4,5-biphosphate
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
isolated from wild-type or knockout mice, subsequently SV40 transformed
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
transient serum-induced translocation of EGFP-tagged enzyme (7%) in parallel to sharp increase in intracellular calcium (within initial 60 seconds), stable binding dependent on influx of extracellular calcium induced here by phorbol myristate acetate
brenda
Highest Expressing Human Cell Lines
Cell Line LinksPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phosphoprotein
-
phosphorylation at S505 increases activity 2fold, phosphorylation state not influenced by serum or phorbol myristate acetate, no impact on calcium-mediated membrane binding, constitutively phosphorylated at S505 in immortalized cells (SV40 transformed)
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
K271N/K273N/K274N
-
wild-type activity, half the wild-type increase in activity in presence of phosphatidylinositol 4,5-biphosphate
K43N
-
impaired release of arachidonic acid in response to serum and phorbol myristate acetate, no translocation to Golgi apparatus in response to serum, C2-domain mutant, calcium and membrane binding
K488N/K543N/K544N
-
2fold increased specific activity (independent of phosphatidylinositol 4,5-biphosphate), 78% reduced release of arachidonic acid and increased Golgi-binding in response to serum, PIP2-binding site triple mutant
K541N/K543N/K544N
-
2fold increased specific activity (independent of phosphatidylinositol 4,5-biphosphate)
S505A
-
38% reduced release of arachidonic acid and prolonged accumulation at Golgi apparatus in response to serum and 30% reduced release of arachidonic acid in response to phorbol myristate acetate, phosphorylation site mutant
S505A/S727A
-
30% reduced release of arachidonic acid in response to phorbol myristate acetate and 50% in response to serum which is further reduced by ERK inhibition, prolonged accumulation at Golgi apparatus in response to serum, phosphorylation site double mutant
S505A/S727A/S515A
-
similar response to serum as double mutant S505A/S727A, phosphorylation site triple mutant
S727A
-
similar release of arachidonic acid in response to serum like wild-type enzyme, phosphorylation site mutant
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TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
following expression with C-terminal hexa-His-tag, dephosphorylation with potato acid phosphatase
-
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
together with EGFP cDNA in AdEasy vector or together with monomeric EYFP or ECFP cDNA in pVQAd5CMVK-NpA shuttle plasmid for adenovirus-mediated infection of lung fibroblasts
-
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REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Gray, N.C.C.; Strickland, K.P.
The purification and characterization of a phospholipase A2 activity from the 106000 x g pellet (microsomal fraction) of bovine brain acting on phosphatidylinositol
Can. J. Biochem.
60
108-117
1981
Bos taurus
brenda
Gray, N.C.C.; Strickland, K.P.
On the specificity of a phospholipase A2 purified from the 106,000 X g pellet of bovine brain
Lipids
17
91-96
1982
Bos taurus
brenda
Shibata, Y.; Abiko, Y.; Takiguchi, H.
Phospholipase A2 in macrophage plasma membrane releases arachidonic acid from phosphatidylinositol
Biochim. Biophys. Acta
971
121-126
1988
Cavia porcellus
brenda
Hong, S.L.; Deykin, D.
The activation of phosphatidylinositol-hydrolyzing phospholipase A2 during prostaglandin synthesis in transformed mouse BALB/3T3 cells
J. Biol. Chem.
256
5215-5219
1981
Mus musculus
brenda
Tucker, D.E.; Ghosh, M.; Ghomashchi, F.; Loper, R.; Suram, S.; St John, B.; Girotti, M.; Bollinger, J.G.; Gelb, M.H.; Leslie, C.C.
Role of phosphorylation and basic residues in the catalytic domain of cytosolic phospholipase A2alpha in regulating interfacial kinetics and binding and cellular function
J. Biol. Chem.
284
9596-9611
2009
Mus musculus
brenda
EXTERNAL LINKS (specific for EC-Number 3.1.1.52)
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