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Information on EC 3.1.1.4 - phospholipase A2 and Organism(s) Homo sapiens and UniProt Accession O60733

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EC Tree
     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.1 Carboxylic-ester hydrolases
                3.1.1.4 phospholipase A2
IUBMB Comments
Also acts on phosphatidylethanolamine, choline plasmalogen and phosphatides, removing the fatty acid attached to the 2-position. Requires Ca2+.
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: O60733
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
phospholipase a2, cpla2, spla2, spla(2), prdx6, cytosolic phospholipase a2, crotoxin, pla2s, ipla2, spla2-iia, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
calcium-independent group VIA iPLA2
-
1-CysPrx
-
a dual-function enzyme with peroxidase and acidic Ca2+-independent phospholipase A2 activities, also known as peroxiredoxin VI, non-selenium glutathione peroxidase, LTW4, antioxidant protein 2 (AOP2), Clara cell protein 26 (CC26) and p67phox binding protein
1-cysteine peroxiredoxin
-
a dual-function enzyme with peroxidase and acidic Ca2+-independent phospholipase A2 activities
14 kDa phospholipase A2
-
-
-
-
acidic Ca2+-independent phospholipase A2
-
-
adiponutrin
-
-
Agkistrotoxin
-
-
-
-
aiPLA2
amdI1
-
-
-
-
Ammodytin I2
-
-
-
-
APLA
-
-
-
-
APP-D-49
-
-
-
-
ASPLA1
-
-
-
-
ASPLA10
-
-
-
-
ASPLA11
-
-
-
-
ASPLA12
-
-
-
-
ASPLA13
-
-
-
-
ASPLA14
-
-
-
-
ASPLA15
-
-
-
-
ASPLA16
-
-
-
-
ASPLA17
-
-
-
-
ASPLA2
-
-
-
-
ASPLA3
-
-
-
-
ASPLA4
-
-
-
-
ASPLA5
-
-
-
-
ASPLA6
-
-
-
-
ASPLA7
-
-
-
-
ASPLA8
-
-
-
-
ASPLA9
-
-
-
-
ATX
-
-
-
-
Basic protein I/II
-
-
-
-
BJ-PLA2
-
-
-
-
BJUPLA2
-
-
-
-
BPI/BPII
-
-
-
-
Ca2+ independent PLA2
-
group VIA PLA2
Ca2+-independent iPLA2
-
-
Ca2+-independent phospholipase A2
-
-
CaI-PLA2
-
-
-
-
Caudoxin
-
-
-
-
cPLA2
cPLA2-alpha
cPLA2-zeta2
-
cPLA2alpha
cPLA2beta
-
isoform
cPLA2delta
-
isoform
cPLA2epsilon
-
isoform
cPm09
-
-
-
-
cytosolic calcium-dependent PLA2
-
GIVA PLA2
cytosolic cPLA2
-
-
cytosolic gIVaPLA2
-
-
cytosolic group IVA cPLA2
-
cytosolic group IVa phospholipase A2
-
-
cytosolic phospholipase A2
-
-
cytosolic phospholipase A2-alpha
cytosolic phospholipase A2alpha
-
-
Enhancing factor
-
-
-
-
GIIA PLA2
-
-
GIIA sPLA2
-
GIIC sPLA2
-
-
-
-
GIID sPLA2
-
-
-
-
GIIE sPLA2
-
-
-
-
GIIF sPLA2
-
-
-
-
GIII sPLA2
-
-
-
-
GIVA cPLA2
-
-
GIVA phospholipase A2
-
GIVA PLA2
-
cytosolic calcium-dependent PLA2
GIVD cPLA2delta
-
Group IB phospholipase A2
-
-
-
-
Group IIA phospholipase A2
group IIA PLA2
-
-
group IIA secretory phospholipase A2
-
group IIA secretory PLA2
-
-
group IID secretory phospholipase A2
-
group IV cPLA2
-
group IVA cPLA2
-
-
group IVA cytosolic phospholipase A2
group IVA phospholipase A2
group IVA PLA2
-
cytosolic calcium-dependent PLA2
group IVB phospholipase A2
-
-
Group V phospholipase A2
-
-
-
-
group V secreted phospholipase A2
-
-
Group VI phospholipase A2
-
-
-
-
Group VIA Ankyrin-1
-
syn: iPLA2-1, splice variant of iPLA2
Group VIA Ankyrin-2
-
syn: iPLA2-2, splice variant of iPLA2
group VIA calcium-independent phospholipase A
-
-
group VIA cPLA2
-
Group VIA PLA2
-
-
Group VIA-3
-
syn: iPLA2-2, splice variant of iPLA2
GVI PLA2
-
-
-
-
GVIA iPLA2
-
-
GVIA PLA2
-
-
GVIIA PLA2
-
PAF acetyl hydrolase/oxidized lipid LpPLA2
GX sPLA2
-
-
-
-
GXII sPLA2
-
-
-
-
GXIII sPLA2
-
-
-
-
hGX sPLA2
-
-
hIIAPLA2
human group IB PLA2
-
human group IIA phospholipase A2
-
-
iPLA2
lecithinase A
-
-
-
-
lipoprotein-associated phospholipase A2
lipoprotein-associated PLA2
-
-
LLPL
-
-
Lp-PLA2
Lpla2
lysophospholipase
-
-
lysosomal phospholipase A2
-
lysosomal PLA2
-
-
MP-III 4R
-
-
-
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Muscarinic inhibitor
-
-
-
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Myotoxin
-
-
-
-
NAJPLA-2A
-
-
-
-
NAJPLA-2B
-
-
-
-
NAJPLA-2C
-
-
-
-
neuropathy target esterase
-
-
Nigexine
-
-
-
-
Non-pancreatic secretory phospholipase A2
Notechis 11'2
-
-
-
-
Notexin
-
-
-
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NPLA
-
-
-
-
NPS-PLA2
-
-
-
-
OHV A-PLA2
-
-
-
-
OHV-APLA2
-
-
-
-
PAF acetyl hydrolase/oxidized lipid LpPLA2
-
-
PAF-AH
-
Lp-PLA2
peroxiredoxin 6
pgPLA 1a/pgPLA 2a
-
-
-
-
phosphatidase
-
-
-
-
phosphatide 2-acylhydrolase
-
-
-
-
phosphatidolipase
-
-
-
-
Phosphatidylcholine 2-acylhydrolase
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GIIC
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GIID
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GIIE
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GIIF
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GIII
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GX
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GXII
-
-
-
-
Phosphatidylcholine 2-acylhydrolase GXIII
-
-
-
-
phospholipase A
-
-
-
-
phospholipase A2
-
-
phospholipase A2 gamma
-
-
Phospholipase A2 inhibitor
-
-
-
-
phospholipase A2alpha
phospholipase A2s
-
-
pkP5
-
-
-
-
PLA2-10
-
-
-
-
PLA2-V
-
-
PLA2-VI
-
-
-
-
PLA2-VII
-
-
-
-
PLA2alpha
-
-
PLA2G4C
-
-
PLA2IID
-
-
-
-
PLA2s
-
-
platelet activating factor acetyl hydrolase
-
-
-
-
platelet activating factor acetyl hydrolase/oxidized lipid LpPLA2
-
GVIIA PLA2
platlet-activating factor acetylhydrolase
-
Lp-PLA2
Prdx6
Pt-PLA1
-
-
-
-
Pt-PLA2
-
-
-
-
secreted group IID phospholipase A2
-
-
secreted human phospholipase A2
-
-
secreted phospholipase A2
secreted phospholipases A2
secreted PLA2
-
sPLA2
secreted sPLA2
-
-
secretory Ca2+-dependent PLA2
-
-
secretory phospholipase
-
-
secretory phospholipase A2
secretory phospholipase A2 group IIA
-
-
Secretory-type PLA, stroma-associated homolog
-
-
-
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sPLA(2)
-
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sPLA(2)-IID
-
-
-
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sPLA(2)-IIE
-
-
-
-
sPLA(2)-IIF
-
-
-
-
sPLA2
sPLA2 GIIA
-
-
sPLA2(IIA)
-
-
sPLA2-IIA
sPLA2-IID
-
-
sPLA2-V
-
-
sPLA2-X
-
-
sPLA2IB2
-
-
TMV-K49
-
-
-
-
Toxin VI
-
-
-
-
Toxin VI:5
-
-
-
-
TTS-2.2
-
-
type VIIA PLA2
-
Lp-PLA2
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
phosphatidylcholine + H2O = 1-acylglycerophosphocholine + a carboxylate
show the reaction diagram
mechanism
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of carboxylic ester
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
phosphatidylcholine 2-acylhydrolase
Also acts on phosphatidylethanolamine, choline plasmalogen and phosphatides, removing the fatty acid attached to the 2-position. Requires Ca2+.
CAS REGISTRY NUMBER
COMMENTARY hide
9001-84-7
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
1-palmitoyl-2-arachidonoylphosphatidylethanolamine
1-palmitoyl-glycerophosphorylethanolamine + arachidonic acid
show the reaction diagram
-
-
?
phospholipids + H2O
?
show the reaction diagram
release of arachidonic acid: biosynthesis of leucotrienes, thromboxans and prostaglandins
-
-
?
(+/-)-3-O-(4-cyanomethylphenyl)-1,2-O-di-n-heptylglycerol + H2O
?
show the reaction diagram
-
-
-
-
?
(+/-)-3-O-(4-hydroxymethylphenyl)-1,2-O-di-n-heptylglycerol + H2O
?
show the reaction diagram
-
-
-
-
?
(2'R,2S)-2,3-dihydroxypropyl 2'-octadecanoyloxy-5'-hexadecyloxy-5'-oxopentan-1'-yl phosphate + H2O
?
show the reaction diagram
-
-
-
?
(2S,2'S,3R)-2,3-dihydroxypropyl 2',3'-octadecanoyloxy-nonadecyl phosphate + H2O
?
show the reaction diagram
-
-
-
?
(2S,2'S,3S)-2,3-dihydroxypropyl 2',3'-octadecanoyloxy-nonadecyl phosphate + H2O
?
show the reaction diagram
-
-
-
?
(R)-1,2-dipalmitoyl-glycero-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
?
(R)-1,2-dipalmitoyl-glycero-3-phosphoglycerol + H2O
?
show the reaction diagram
-
-
-
?
(R)-1,2-dipalmitoyl-sn-glycero-3-phosphocholine + H2O
?
show the reaction diagram
-
enzyme adsorbs to monolayers of L-alpha-1,2-dipalmitoyl-sn-glycero-3-phosphocholine, leading to hydrolysis of the monlayer
-
-
?
(R)-1-O-hexadecyl-2-palmitoyl-sn-glycero-3-phoshocholine + H2O
?
show the reaction diagram
-
-
-
?
1,2-bis(heptanoylthio)-glycerophosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
1,2-bis-(10-pyrenedecanoyl)-sn-glycero-3-phosphocholine + H2O
1-(10-pyrenedecanoyl)-glycero-3-phosphocholine + 10-pyrenedecanoate
show the reaction diagram
1,2-bis-(4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene-3-undecanoyl)-sn-glycero-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
1,2-di-O-hexadecyl-sn-glycerol-3-phosphocholine + H2O
1-O-hexadecyl-sn-glycero-3-phosphocholine + hexadecanoate
show the reaction diagram
-
-
-
-
?
1,2-didecanoyl-sn-glycero-3-phosphocholine + H2O
1-decanoyl-sn-glycero-3-phosphocholine + decanoate
show the reaction diagram
-
-
-
?
1,2-didodecanoyl-sn-glycero-3-phosphocholine + H2O
1-decanoyl-sn-glycero-3-phosphocholine + decanoate
show the reaction diagram
-
-
-
?
1,2-diheptanoyl phosphatidylcholine + H2O
1-heptanoyl-sn-glycerophosphocholine + heptanoic acid
show the reaction diagram
-
-
-
-
?
1,2-diheptanoyl-sn-glycero-3-phophorylcholine + H2O
1-heptanoyl-sn-glycero-3-phophorylcholine + heptanoate
show the reaction diagram
-
-
-
-
?
1,2-diheptanoyl-sn-glycero-3-sulfate + H2O
1-heptanoyl-sn-glycero-3-sulfate + heptanoate
show the reaction diagram
-
-
-
?
1,2-dihexanoyl-sn-glycero-3-phosphocholine + H2O
1-hexanoyl-sn-glycero-3-phosphocholine + hexanoate
show the reaction diagram
-
-
-
?
1,2-dilauroyl-sn-glycero-3-phosphocholine + H2O
1-lauroyl-sn-glycero-3-phosphocholine + laureate
show the reaction diagram
-
-
-
?
1,2-dimyristoyl-sn-glycero-3-phosphocholine + H2O
1-myristoyl-sn-glycero-3-phosphocholine + myristic acid
show the reaction diagram
-
-
-
-
?
1,2-dimyristoyl-sn-phosphatidylcholine + H2O
1-myristoyl-phosphorylcholine + myristic acid
show the reaction diagram
1,2-dinonanoyl-sn-glycero-3-phosphocholine + H2O
1-nonanoyl-sn-glycero-3-phosphocholine + nonanoate
show the reaction diagram
-
-
-
?
1,2-dioctanoyl-sn-glycero-3-phosphocholine + H2O
1-octanoyl-sn-glycero-3-phosphocholine + octanoate
show the reaction diagram
1,2-dioctanoyl-sn-glycero-3-phosphoglycol + H2O
1-octanoyl-sn-glycero-3-phosphoglycol + octanoate
show the reaction diagram
-
-
-
?
1,2-dioleoyl-L-alpha-phosphatidylcholine + H2O
?
show the reaction diagram
-
-
-
-
?
1,2-dioleoyl-sn-glycero-3-phosphocholine + H2O
1-oleoylglycerophosphocholine + oleic acid
show the reaction diagram
-
-
-
-
?
1,2-dioleoyl-sn-glycerol + H2O
1-oleoyl-sn-glycerol + oleic acid
show the reaction diagram
-
-
-
-
?
1,2-dioleoyl-sn-glycerol + H2O
?
show the reaction diagram
-
-
-
-
?
1,2-dioleoyl-sn-phosphatidylcholine + H2O
1-oleoyl-sn-phosphatidylcholine + oleate
show the reaction diagram
-
-
-
?
1,2-dioleoyl-sn-phosphatidylethanolamine + H2O
1-oleoyl-sn-phosphatidylethanolamine + oleic acid
show the reaction diagram
-
-
-
?
1,2-dipalmitoyl-phosphatidylcholine + H2O
1-palmitoyl-glycerophosphorylcholine + palmitic acid
show the reaction diagram
1,2-dipalmitoyl-phosphatidylethanolamine + H2O
1-palmitoyl-phosphatidylethanolamine + palmitic acid
show the reaction diagram
-
-
-
?
1,2-dipalmitoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycero-3-phosphocholine + palmitic acid
show the reaction diagram
-
-
-
?
1,2-dipalmitoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycero-3-phosphorylcholine + palmitate
show the reaction diagram
1,2-dipalmitoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoylglycerophosphocholine + palmitic acid
show the reaction diagram
-
-
-
-
?
1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-(lissamine rhodamine B sulfonyl) + H2O
1-palmitoyl-sn-glycero-3-phosphoethanolamine-N-(lissamine rhodamine B sulfonyl) + palmitic acid
show the reaction diagram
-
-
-
-
?
1,2-dipalmitoyl-sn-glycero-3-phosphoglycerol + H2O
1-palmitoyl-glycero-3-phosphoglycerol + palmitate
show the reaction diagram
1,2-dipalmitoyl-sn-glycero-3-phosphorylcholine + H2O
1-palmitoyl-sn-glycero-3-phosphorylcholine + palmitic acid
show the reaction diagram
-
in mixed micelles with Triton X-100
-
?
1,2-dipalmitoyl-sn-glycero-3-phosphorylcholine + H2O
?
show the reaction diagram
-
-
-
-
?
1,2-dipalmitoyl-sn-phosphatidylcholine + H2O
1-palmitoyl-sn-phosphatidylcholine + palmitate
show the reaction diagram
the catalytic site for aiPLA2 activity is an S32-H26-D140 triad
-
-
?
1,2-dithio-heptanoylphosphatidylcholine + H2O
?
show the reaction diagram
-
detection of reaction product with 5,5'-dithio-bis-(2-nitrobenzoic acid)
-
-
?
1-acyl-2-arachidonoyl-glycerophosphocholine + H2O
1-acyl-glycerophosphocholine + arachidonic acid
show the reaction diagram
-
-
-
?
1-acyl-2-arachidonoyl-sn-glycero-3-phosphoethanolamine + H2O
1-acyl-sn-glycero-3-phosphoethanolamine + arachidonic acid
show the reaction diagram
-
-
-
?
1-acyl-2-arachidonoyl-sn-glycerol phosphoethanolamine + H2O
1-acyl-sn-glycerol phosphoethanolamine + arachidonate
show the reaction diagram
radiolabeled substrate
-
-
?
1-acyl-2-arachidonoyl-sn-glycerophosphoethanolamine + H2O
1-acyl-sn-glycerophosphoethanolamine + arachidonic acid
show the reaction diagram
-
-
-
?
1-acyl-2-linoleoyl-3-phosphoethanolamine + H2O
1-acyl-3-phosphoethanolamine + linolic acid
show the reaction diagram
1-acyl-2-linoleoyl-glycerophosphocholine + H2O
1-acyl-glycerophosphocholine + linolic acid
show the reaction diagram
-
-
-
?
1-decanoyl-2-(4-nitrophenylglutaryl)glycerol 3-phosphate + H2O
?
show the reaction diagram
-
HSD-PLA2
-
-
?
1-hexadecanoyl-2-(1-pyrenedecanoyl)-glycero-3-phosphatidic acid + H2O
?
show the reaction diagram
-
group V sPLA2
-
-
?
1-hexadecanoyl-2-(1-pyrenedecanoyl)-glycero-3-phosphocholine + H2O
1-hexadecanoyl-glycero-3-phosphocholine + 1-pyrenedecanoate
show the reaction diagram
1-hexadecanoyl-2-(1-pyrenedecanoyl)-glycero-3-phosphoethanolamine + H2O
1-hexadecanoyl-glycero-3-phosphoethanolamine + 1-pyrenedecanoate
show the reaction diagram
1-hexadecanoyl-2-(1-pyrenedecanoyl)-glycero-3-phosphoglycerol + H2O
1-hexadecanoyl-glycero-3-phosphoglycerol + 1-pyrenedecanoate
show the reaction diagram
1-hexadecanoyl-2-(1-pyrenedecanoyl)-glycero-3-phosphoserine + H2O
1-hexadecanoyl-glycero-3-phosphoserine + 1-pyrenedecanoate
show the reaction diagram
-
group V sPLA2
-
?
1-hexadecanoyl-2-(10-(1-pyrene)decanoyl)-sn-glycero-3-phosphoglycerol + H2O
1-hexadecanoyl-sn-glycero-3-phosphoglycerol + 10-(1-pyrene)decanoic acid
show the reaction diagram
-
-
-
-
?
1-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine + H2O
1-hexadecanoyl-glycero-3-phosphoglycerol + acetate
show the reaction diagram
-
i.e. PAF or platelet activating factor
-
-
?
1-hexadecyl-2-acetyl-sn-glycerol-3-phosphocholine + H2O
1-hexadecyl-sn-glycerol-3-phosphocholine + acetate
show the reaction diagram
i.e. platelet-activating factor
-
-
?
1-oleoyl-2-palmitoyl-phosphatidylcholine + H2O
1-oleoyl-phosphatidylcholine + palmitic acid
show the reaction diagram
-
-
-
?
1-oleoyl-sn-glycero-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-(10-pyrenyldecanoyl)-sn-glycero-3-phosphate + H2O
10-pyrenyldecanoic acid + 1-palmitoyl-sn-glycero-3-phosphate
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-glycero-3-phosphocholine + arachidonate
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphorylcholine + H2O
1-palmitoyl-sn-glycero-3-phosphorylcholine + arachidonic acid
show the reaction diagram
-
in mixed micelles with Triton X-100
-
?
1-palmitoyl-2-arachidonoylglycerophosphocholine + H2O
1-palmitoyl-glycerophosphorylcholine + arachidonic acid
show the reaction diagram
-
GIVA cPLA2 substrate and GIVA iPLA2
-
-
?
1-palmitoyl-2-arachidonoylphosphatidylcholine + H2O
1-palmitoyl-glycerophosphorylcholine + arachidonic acid
show the reaction diagram
1-palmitoyl-2-arachidonyl-phosphatidylcholine + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycero-3-phosphocholine + arachidonic acid
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-arachidonyl-sn-glycerol-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-linoleoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycero-3-phosphocholine + linolic acid
show the reaction diagram
-
-
-
?
1-palmitoyl-2-linoleoylphosphatidylcholine + H2O
1-palmitoyl-glycerophosphorylcholine + linolic acid
show the reaction diagram
-
group V sPLA2
-
?
1-palmitoyl-2-linoleoylphosphatidylethanolamine + H2O
1-palmitoyl-glycerophosphorylethanolamine + linolic acid
show the reaction diagram
1-palmitoyl-2-oleoyl-phosphatidylcholine + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-oleoyl-phosphatidylethanolamine + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-oleoyl-phosphatidylglycerol + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-oleoyl-phosphatidylinositol + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-oleoyl-sn-glycero-3-phosphate + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycero-3-phosphocholine + oleate
show the reaction diagram
1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoethanolamine + H2O
1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol + H2O
show the reaction diagram
-
-
-
?
1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol + H2O
1-palmitoyl-sn-glycero-3-phosphorylglycerol + oleate
show the reaction diagram
1-palmitoyl-2-oleoylphosphatidylcholine + H2O
1-palmitoyl-glycerophosphocholine + oleic acid
show the reaction diagram
1-palmitoyl-2-stearoyl-dibromo-sn-glycero-3-phosphocholine + H2O
?
show the reaction diagram
1-palmitoyl-sn-glycero-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-sn-glycerol-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine + H2O
1-stearoyl-sn-glycero-3-phosphocholine + arachidonate
show the reaction diagram
1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine + H2O
1-stearoyl-sn-glycero-3-phosphocholine + arachidonic acid
show the reaction diagram
1-stearoyl-2-arachidonoylphosphatidylcholine + H2O
1-stearoyl-glycerophosphorylcholine + arachidonic acid
show the reaction diagram
-
cPLA2 cleaves selectively arachidonoyl containing phospholipids
-
?
1-stearoyl-2-arachidonyl-phosphatidylinositol 4,5-bisphosphate + H2O
1-stearoyl-sn-glycero-3-phosphoinositol 4,5-bisphosphate + arachidonic acid
show the reaction diagram
-
-
-
-
?
4-nitro-3-octanoyloxy-benzoic acid + H2O
?
show the reaction diagram
-
-
-
-
?
arachidonyl thio-PC + H2O
arachidonic acid + (7R)-4-hydroxy-N,N,N-trimethyl-7-sulfanyl-3,5,9-trioxa-4-phosphapentacosan-1-aminium 4-oxide
show the reaction diagram
-
-
-
-
?
choline plasmalogen + H2O
lysoplasmalogen + fatty acid
show the reaction diagram
-
-
-
?
DBPA + H2O
?
show the reaction diagram
-
fluorogenic Dabcyl- and BODIPY-containing phospholipd-analogue
-
-
?
DBPC + H2O
?
show the reaction diagram
-
fluorogenic Dabcyl- and BODIPY-containing phospholipd-analogue
-
-
?
DBPE + H2O
?
show the reaction diagram
-
fluorogenic Dabcyl- and BODIPY-containing phospholipd-analogue
-
-
?
DBPG + H2O
?
show the reaction diagram
-
fluorogenic Dabcyl- and BODIPY-containing phospholipd-analogue
-
-
?
diarachidonylphosphatidylcholine + H2O
arachidonylphosphatidylcholine + arachidonic acid
show the reaction diagram
-
-
-
?
diheptanoyl phosphatidylcholine + H2O
1-heptanoyl-sn-glycerophosphocholine + heptanoic acid
show the reaction diagram
-
-
-
-
?
dioleoyl phosphatidylglycerol + H2O
?
show the reaction diagram
-
-
-
-
?
dipalmitoyl-phosphatidylcholine + H2O
1-palmitoyl-glycerophosphocholine + palmitic acid
show the reaction diagram
-
GIVA iPLA2 and GV sPLA2
-
-
?
L-alpha-dipalmitoyl phosphatidylcholine + H2O
1-palmitoyl-sn-glycerophosphocholine + palmitate
show the reaction diagram
-
-
-
-
?
oxidized high density lipoprotein + H2O
?
show the reaction diagram
-
-
-
-
?
oxidized low density lipoprotein + H2O
?
show the reaction diagram
-
-
-
-
?
oxidized palmitoyl arachidonyl phosphatidylcholine + H2O
?
show the reaction diagram
-
-
-
-
?
oxidized phosphatidylcholines + H2O
1-acylglycerophosphocholine + oxidized fatty acids
show the reaction diagram
phosphatidylcholine + arachidonic acid
1-acyl-2-arachidonoyl-sn-glycero-3-phosphocholine + carboxylic acid
show the reaction diagram
-
-
-
r
phosphatidylcholine + H2O
1-acylglycerophosphocholine + a carboxylate
show the reaction diagram
phosphatidylcholine + H2O
1-acylglycerophosphocholine + fatty acid
show the reaction diagram
phosphatidylcholine + linoleic acid
lineoyl phosphatidylcholine
show the reaction diagram
-
-
-
?
phosphatidylethanolamine + arachidonic acid
arachidonoyl phosphatidylethanolamine
show the reaction diagram
-
-
-
r
phosphatidylethanolamine + H2O
1-acylglycerophosphorylethanolamine + fatty acid
show the reaction diagram
phosphatidylethanolamine + linoleic acid
lineoyl phosphatidylethanolamine + fatty acid
show the reaction diagram
-
-
-
?
phosphatidylglycerol + H2O
1-acylglycerol + fatty acid
show the reaction diagram
-
-
-
?
phosphatidylinositol + arachidonic acid
arachidonoyl phosphatidylinositol + fatty acid
show the reaction diagram
-
-
-
?
phosphatidylinositol + linoleic acid
lineoyl phosphatidylinositol + fatty acid
show the reaction diagram
-
-
-
?
phosphatidylserine + arachidonic acid
arachidonoyl phosphatidylserine + fatty acid
show the reaction diagram
-
-
-
?
phosphatidylserine + linoleic acid
lineoyl phosphatidylserine + fatty acid
show the reaction diagram
-
-
-
?
phospholipids + H2O
?
show the reaction diagram
pigment epithelium-derived 6 + H2O
?
show the reaction diagram
-
i.e. PED6, a synthetic substrate
-
-
?
platelet activating factor + H2O
?
show the reaction diagram
platelet activating factor + H2O
lyso-platelet activating factor
show the reaction diagram
-
-
-
-
?
rac-1,2-dihexanoyldithiopropyl-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
phospholipids + H2O
?
show the reaction diagram
release of arachidonic acid: biosynthesis of leucotrienes, thromboxans and prostaglandins
-
-
?
1,2-dioleoyl-sn-glycero-3-phosphocholine + H2O
1-oleoylglycerophosphocholine + oleic acid
show the reaction diagram
-
-
-
-
?
1,2-dipalmitoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoylglycerophosphocholine + palmitic acid
show the reaction diagram
-
-
-
-
?
1-hexadecyl-2-acetyl-sn-glycerol-3-phosphocholine + H2O
1-hexadecyl-sn-glycerol-3-phosphocholine + acetate
show the reaction diagram
i.e. platelet-activating factor
-
-
?
1-oleoyl-sn-glycero-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
1-palmitoyl-sn-glycero-3-phosphocholine + H2O
?
show the reaction diagram
-
-
-
-
?
diheptanoyl phosphatidylcholine + H2O
1-heptanoyl-sn-glycerophosphocholine + heptanoic acid
show the reaction diagram
-
-
-
-
?
phosphatidylcholine + H2O
1-acylglycerophosphocholine + a carboxylate
show the reaction diagram
phospholipids + H2O
?
show the reaction diagram
platelet activating factor + H2O
?
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
ankyrin-iPLA2s
iPLA2-splice variant, contributes to formation of the iPLA2-tetrameric complex but possesses no active site
-
(+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
-
-
(2E,4E,6S)-6-[(2-oxohexadecanoyl)amino]deca-2,4-dienoic acid
-
reduces the cellular release of arachidonic acid by 6%
(2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoic acid
-
reduces the cellular release of arachidonic acid by 74%
(3-aminooxalyl-1-benzyl-2-ethyl-6-methyl-1H-indol-4-yl)oxyacetic acid methyl ester
-
LY374388, potent sPLA2 inhibitor
(3S)-4-[(4-benzylphenyl)sulfanyl]-3-[(7-phenylheptanoyl)amino]butane-1-sulfonic acid
bioisosteric replacements, binding energy of -22.05 kJ/mol
(3S)-4-[(4-benzylphenyl)sulfanyl]-3-[(7-phenylheptanoyl)amino]butyl phosphonic acid
bioisosteric replacements, binding energy of -19.76 kJ/mol
(3S)-4-[(4-benzylphenyl)sulfanyl]-3-[[7-(4-hydroxyphenyl)heptanoyl]amino]butane-1-sulfonic acid
bioisosteric replacements, molecular structure is characterized by a chiral centre of absolute (R)-configuration, four carbons in the R1 chain, a hydroxyl group as a substituent in the para-position of the phenyl ring in R1 chain and a sulphonate group instead of the carboxylate group, indicates the highest binding energy (-29.1 kJ/mol) than all the other analogues and the prototype
(4R)-5-[(4-benzylphenyl)sulfanyl]-4-[(7-phenylheptanoyl)amino]pentanoic acid
(R)-configuration of FPL67047XX, binding energy of -19.5 kJ/mol
(4R)-6-methyl-4-[(2-oxohexadecanoyl)amino]heptanoic acid
-
reduces the cellular release of arachidonic acid by 62%
(4S)-4-[(2-oxododecanoyl)amino]octanoic acid
-
reduces the cellular release of arachidonic acid by 56%
(4S)-4-[(2-oxohexadecanoyl)amino]nonanoic acid
-
-
(4S)-4-[(2-oxohexadecanoyl)amino]octanoic acid
-
reduces the cellular release of arachidonic acid by 79%
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[(5-phenylpentanoyl)amino]pentanoic acid
decreased carbon chain length between the amide group and the aromatic ring of the R1 chain, binding energy of -22.02 kJ/mol
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[[7-(4-hydroxyphenyl)heptanoyl]amino]pentanoic acid
substituents in the para-position of the aromatic ring R1, higher binding energy (-27.61 kJ/mol) than the prototype and all the other analogues except structure 9
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[[7-(4-methoxyphenyl)heptanoyl]amino]pentanoic acid
substituents in the para-position of the aromatic ring R1, binding energy of -22.23 kJ/mol
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[[7-(4-nitrophenyl)heptanoyl]amino]pentanoic acid
substituents in the para-position of the aromatic ring R1, binding energy of -20.25 kJ/mol
(5S)-5-[(2-oxohexadecanoyl)amino]decanoic acid
-
-
(5S)-5-[(2-oxohexadecanoyl)amino]nonanoic acid
-
reduces the cellular release of arachidonic acid by 59%
(6Z,9Z,12Z,15Z)-1,1,1-trifluorohenicosa-6,9,12,15-tetraen-2-one
(R)-4-(7-phenylheptanamido)octanoic acid
-
-
(R)-gamma-norleucine
-
a highly selective inhibitor of isozyme GV sPLA2
(R)-methyl 6-methyl-4-(2-oxohexadecanamido)heptanoate
-
-
(S)-2-(2-(2-oxohexadecanamido)hexanamido)acetic acid
-
contains a free carboxyl group, inhibits GIVA cPLA2 without affecting the activity of the other intracellular enzyme GVIA iPLA2
(S)-2-(2-(2-oxohexadecanamido)hexyloxy)acetic acid
-
selectively inhibits GIVA cPLA2, due to its free carboxyl group. Most potent inhibitor of GIVA cPLA2. Reduces the cellular release of arachidonic acid by 68%
(S)-2-(3-methyl-2-(2-oxohexadecanamido)butanamido)acetic acid
-
contains a free carboxyl group, inhibits GIVA cPLA2 without affecting the activity of the other intracellular enzyme GVIA iPLA2
(S)-ethyl 2-(2-(2-oxohexadecanamido)hexanamido)acetate
-
ethyl ester based on Nle-Gly dipeptide, potent inhibition of GVIA iPLA2, inhibits GIVA cPLA2 (73%) and GV sPLA2 (63%)
(S)-ethyl 2-(2-(2-oxohexadecanamido)hexyloxy)acetate
-
preferentially inhibits GVIA iPLA2, is a potent inhibitor of GVIA iPLA2, inhibits GIVA cPLA2 by 52% and GV sPLA2 by 81%
(S)-ethyl 6-(2-oxohexadecanamido)decanoate
-
-
(S)-methyl 2-(2-(2-oxohexadecanamido)hexanamido)acetate
-
methyl ester based on dipeptide Nle-Gly, inhibits both GIVA cPLA2 and GVIA iPLA2, showing a small preference for GIVA cPLA2, inhibits GV sPLA2 by 65%
(S)-methyl 2-(3-methyl-2-(2-oxohexadecanamido)butanamido)acetate
-
methyl ester based on dipeptide Val-Gly, inhibits activity of GIVA cPLA2 by 25%
(S)-methyl 4-(2-oxohexadecanamido)octanoate
-
-
(S)-methyl 4-(7-phenylheptanamido)octanoate
-
-
(S)-tert-butyl 2-(2-(2-oxohexadecanamido)hexanamido)acetate
-
tert-butyl ester based on Nle-Gly dipeptide, potent inhibition of GVIA iPLA2, inhibits GIVA cPLA2 (72%) and GV sPLA2 (59%)
(S)-tert-butyl 2-(2-(2-oxohexadecanamido)hexyloxy)acetate
-
preferentially inhibits GVIA iPLA2 (81% inhibition), inhibits GIVA cPLA2 by 44% and GV sPLA2 by 57%
(S)-tert-butyl 2-(3-methyl-2-(2-oxohexadecanamido)butanamido)acetate
-
tert-butyl ester based on dipeptide Val-Gly, inhibits both GIVA cPLA2 and GVIA iPLA2, showing a small preference for GIVA cPLA2, reduces GV sPLA2 activity by 78%. Reduces the cellular release of arachidonic acid by 30%
(S)-tert-butyl 4-(2-oxohexadecanamido)pentanoate
-
-
(S,2E,4E)-6-(2-oxohexadecanamido)deca-2,4-dienoic acid
-
-
(S,2E,4E)-ethyl 6-(2-oxohexadecanamido)deca-2,4-dienoate
-
-
([1-[amino(oxo)acetyl]-3-(biphenyl-2-ylmethyl)-2-(2-methylpropyl)indolizin-8-yl]oxy)acetic acid
-
-
([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-benzo[g]indol-4-yl]oxy)acetic acid
-
-
1,1,1,2,2-pentafluoro-5-(4-hexyloxy-phenyl)-pentan-3-one
-
-
1,1,1,2,2-pentafluoro-7-phenyl-heptan-3-one
-
a selective inhibitor of GVIA iPLA2
1,1,1,2,2-pentafluoro-8-phenyl-octan-3-one
-
-
1,1,1,2,2-pentafluoro-9-phenyl-nonan-3-one
-
-
1,1,1,2,2-pentafluoro-octadecan-3-one
-
-
1,1,1,3,3-pentafluoro-6-phenyl-hexane-2,2-diol
-
-
1,1,1,3-tetrafluoro-heptadecan-2-one
-
-
1,1,1-trifluoro-4-(4-hexyloxy-phenyl)-butan-2-one
-
-
1,1,1-trifluoro-6-(4-hexyloxy-phenyl)-hexan-2-one
-
-
1,1,1-trifluoro-6-phenylhexan-2-one
-
-
1,1,1-trifluoro-7-phenylheptan-2-one
-
-
1,1,1-trifluoro-8-phenyloctan-2-one
-
-
1,1,1-trifluoroheptadecan-2-one
-
-
1-(1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
-
-
1-(2-dimethylaminoethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(4-carboxybenzyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(4-octylphenoxy)-3-[5-(1H-tetrazol-5-yl)indol-1-yl]propan-2-one
-
inhibits isozyme cPLA2alpha
1-(5-nitro-1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
-
-
1-(carboxymethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(carboxypentyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(carboxypropyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-benzyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
-
-
1-H-indole-3-glyoxamide
-
varespladib methyl, potent sPLA2 inhibitor
1-hexyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-methyl 5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
-
-
1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
-
competitive inhibition of platelet activating factor hydrolysis
1-palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
-
competitive inhibitor toward sPLA2, dose-dependent inhibition
1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazole-5-carboxylic acid
-
-
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-5-carboxylic acid
-
43% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-6-carboxylic acid
-
44% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 2 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
1-[3-(4-octylphenoxy)-2-oxopropyl]-2,3-dihydro-1H-indole-5-carboxylic acid
-
-
1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-5-carboxylic acid
-
49% metabolic stability in an assay with rat liver microsomes, possesses the best thermodynamic solubility (22 microg/ml at pH 7.4)
1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-6-carboxylic acid
-
40% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 7 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid
-
reveals the highest cPLA2a inhibitory potency, is 7fold more active than the lead 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid, is the metabolically most stable compound in an assay with rat liver microsomes (64% stability). Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-6-carboxylic acid
-
36% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 5 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid
-
is 7fold less active than 1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid, is the metabolically most stable compound in an assay with rat liver microsomes (65% stability). Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
-
inhibits isozyme cPLA2alpha
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-6-carboxylic acid
-
39% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-[4-(decyloxy)phenoxy]-2-oxopropyl]-3-(methoxycarbonyl)-1H-indole-5-carboxylic acid
-
-
1-[5-(morpholine-4-carbonyl)indol-1-yl]-3-(4-octylphenoxy)propan-2-one
-
inhibits isozyme cPLA2alpha
2,2'-biphenyl-3,4'-diylbis(4H-chromen-4-one)
2,2'-biphenyl-4,4'-diylbis(4H-chromen-4-one)
2,2'-diphenyl-4H,4'H-6,6'-bichromene-4,4'-dione
2-(1-benzyl-2-ethyl-4-methoxy-1H-benzo[g]indol-3-yl)-2-oxoacetamide
-
-
2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-6,7-benzoindol-4-yloxy)acetic acid
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-benzo[g]indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(methylsulfonyl)propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(2-chlorophenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(2-methylphenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(3-chlorophenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(4-chlorophenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(4-methylphenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(trifluoromethyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[[2-(trifluoromethyl)phenyl]sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-benzo[g]indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
-
-
2-hydroxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
-
2-mercaptoethanol
-
-
2-methoxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
-
2-oxo-N-(4-oxooctyl)hexadecanamide
-
-
2-tetradecanoylaminohexanol-1-phosphocholine
-
competitive inhibition, R-enantiomer is a more potent inhibitor
2-tetradecanoylaminohexanol-1-phosphoethanolamine
-
competitive inhibition, R-enantiomer is a more potent inhibitor
2-tetradecanoylaminohexanol-1-phosphoglycol
-
competitive inhibition, R-enantiomer is a more potent inhibitor
2-[1-benzyl-2-(2-methylpropyl)-4-(2-oxopropoxy)-1H-indol-3-yl]-2-oxoacetamide
-
-
2-[1-benzyl-4-(2-oxopropoxy)-2-propyl-1H-indol-3-yl]-2-oxoacetamide
-
-
2-[3-(biphenyl-2-ylmethyl)-2-ethyl-8-(2-oxopropoxy)indolizin-1-yl]-2-oxoacetamide
-
-
2-[3-(biphenyl-2-ylmethyl)-2-ethyl-8-methoxyindolizin-1-yl]-2-oxoacetamide
-
-
25-O-acetyl-petrosaspongiolide M
an anti-inflammatory marine natural product
3,3'-[[2-(pentyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
-
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
-
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
-
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
-
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
-
3,4-dichloroisocoumarin
-
-
3-(1-benzyl-2,5-dimethylpyrrol-3-yl)-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
18% inhibition at 0.033 mM
3-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-yl)-4,5-dihydro-1,2,4-oxadiazol-5-one
-
inhibits isozyme cPLA2alpha
3-(2,5-dimethyl-1-phenylpyrrol-3-yl)-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
40% inhibition at 0.033 mM
3-(2,5-dimethylpyrrol-3-yl)-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
35% inhibition at 0.033 mM
3-(2-methylpropanoyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
-
3-(2-methylpropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
-
-
3-(3-acetamido-2-benzyl-2-ethylindolyl-5-oxy)propane phosphonic acid
-
LY311727, IC50 value of 36 nM, group IIa and V sPLA2
3-(3-carboxypropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
-
-
3-(4-fluorophenyl)-3-(1,2,5-trimethylpyrrol-3-yl)-3H-isobenzofuran-1-one
-
36% inhibition at 0.033 mM
3-(4-fluorophenyl)-3-[1-(3-hydroxyphenyl)-2,5-dimethylpyrrol-3-yl]-3H-isobenzofuran-1-one
-
30% inhibition at 0.033 mM
3-(4-fluorophenyl)-3-[1-(4-hydroxyphenyl)-2,5-dimethylpyrrol-3-yl]-3H-isobenzofuran-1-one
-
60% inhibition at 0.033 mM
3-(4-hydroxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(4-methoxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(5-carboxypentanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(6-hydroxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(6-methoxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-butanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-hexanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-pyrrol-3-yl-3H-isobenzofuran-1-one
-
synthesis and inhibitory potency of derivatives, overview
3-[1-(3,4-dihydroxyphenyl)-2,5-dimethylpyrrol-3-yl]-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
20% inhibition at 0.033 mM
3-[1-(4-aminophenyl)-2,5-dimethylpyrrol-3-yl]-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
55% inhibition at 0.033 mM
3-[1-benzyl-3-(carbamoylmethyl)-2-ethylindol-5-yl]oxypropylphosphonic acid
-
LY311727, potent sPLA2 inhibitor
3-[2,5-dimethyl-1-(4-methylaminophenyl)pyrrol-3-yl]-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
36% inhibition at 0.033 mM
3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[3-(pentyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
-
4-(2,4-dioxothiazolidin-5-ylidenemethyl)-N-(4-[1-(4-fluorophenyl)-3-one-1H-isobenzofuran-1-yl]-2,5-dimethyl-1-phenylpyrrol-3-ylmethyl)benzamide
-
-
4-(3-[1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-1-yl]-2,5-dimethylpyrrol-1-yl)benzamide
-
42% inhibition at 0.033 mM
4-(3-[1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-1-yl]-2,5-dimethylpyrrol-1-yl)benzoic acid
-
51% inhibition at 0.033 mM
4-(4-benzyloxy-phenyl)-1,1,1-trifluoro-butan-2-one
-
-
4-(4-decyloxy-phenyl)-1,1,1-trifluoro-butan-2-one
-
-
4-[(2-oxohexadecanoyl)amino]butanoic acid
4-[2-[5-chloro-2-(2-[[(3,4-dichlorobenzyl)sulfonyl]amino]ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy]benzoic acid
-
-
4-[3-[5-chloro-2-(2-[[(3,4-dichlorobenzyl)sulfonyl]amino]ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl]benzoic acid
-
-
4-[4-[2-([2-[bis(4-chlorophenyl)methoxy]ethyl]sulfonyl)ethoxy]phenyl]-1,1,1-trifluorobutan-2-one
-
-
5-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-ylmethylidene)thiazolidine-2,4-dione
-
inhibits isozyme cPLA2alpha
5-(4-[3-(1-[4-fluorophenyl]-3-oxo-1,3-dihydroisobenzofuran-1-yl)-2,5-dimethyl-pyrrol-1-yl]benzylidene)thiazolidine-2,4-dione
-
76% inhibition at 0.033 mM
5-[3-(4-octylphenoxy)-2-oxopropoxy]-1-propylindole-2-carboxylic acid
-
-
5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
6-(4-decyloxy-phenyl)-1,1,1-trifluoro-hexan-2-one
-
-
6-[3-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
6-[4-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
AACOCF3
-
significantly inhibits IL-1beta-stimulated prostaglandin E2 synthesis
allyl 4-(2-oxohexadecanamido)butanoate
-
-
amentoflavone
annexin A2
-
phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction, as annexin A2 complex annexin A2-p11 heterotetramer
-
annexin A2-p11 heterotetramer
-
annexin A2-p11 heterotetramer inhibits cPLA2alpha by interacting with Ser727, phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction as annexin A2 complex annexin A2-p11 heterotetramer. annexin A2-p11 heterotetramer inhibition of cPLA2alpha is independent of Ser505 phosphorylation
-
arachidonyl trifluoromethyl ketone
-
AACOCF3, inhibits release of [3H]arachidonic acid by a 0.01 mM concentration
arachidonyl trifluoromethylketone
-
causes inhibition to baseline level of gIVaPLA2 activity caused by IL-8/CXCL8
arachidonyltrifluoromethyl ketone
-
-
AX006
-
inhibits GIVA cPLA2
AX048
-
inhibits GIVA cPLA2 and GVIA iPLA2
AZ-1
cPLA2-alpha inhibitor, causes almost complete suppression of arachidonic acid release induced by various stimuli. Reduces by 70% the generation of platelet activating factor from macrophages
benzyl 4-(2-oxohexadecanamido)butanoate
-
-
bromoenol lactone
bromoenollactone
-
is not specific for GVIA PLA2 and actually functions through activation of the inhibitor by GVIA PLA2 followed by nonspecific covalent modification of cysteine residues in all proximally located enzymes
Ca2+
-
-
Calmodulin
-
GVIA PLA2 is regulated by calmodulin which negatively regulates GVIA PLA2 through direct binding on the residues 694-705 of GVIA-1 PLA2
catechin
-
reaches 50% inhibition at concentrations of 2.5 mM
cyanidin
-
mixed competitive and noncompetitive inhibition, partial hyperbolic type of inhibition
dantrolene
-
-
darapladib
-
inhibits Lp-PLA2 activity by 59%
delphinidin
-
mixed competitive and noncompetitive inhibition, complete inhibition
diethyl 4-nitrophenyl phosphate
-
Diethyl p-nitrophenyl phosphate
-
-
diisopropyl fluorophosphate
-
-
dithiothreitol
-
-
DTNB
-
plasmalogen-specific PLA2
ethyl (2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoate
-
reduces the cellular release of arachidonic acid by 16%
ethyl 2-(2-oxohexadecanamido)acetate
-
-
ethyl 3-(2-oxohexadecanamido)propanoate
-
-
ethyl 4-(2-oxohexadecanamido)benzoate
-
-
ethyl 4-[(2-oxohexadecanoyl)amino]butanoate
-
-
ethyl 5-(2-oxohexadecanamido)pentanoate
-
-
FPL67047XX
used as a prototype structure with a binding energy of -18.96 kJ/mol
genistein
-
inhibits sPLA(2) enzymes of inflammatory exudates in a concentration dependent manner. Increasing the Ca2+ concentration from 2.5 to 15 mM and substrate concentration up to 0.000120 mM does not alter the level of inhibition
giripladib
hexadecyl-3-trifluorethylglycero-sn-2-phospho-methanol
-
i.e. MJ33
indole-5-carboxamide
-
inhibits isozyme cPLA2alpha
indole-5-carboxylic acid
-
inhibits isozyme cPLA2alpha
indoxam
koninginin E
-
KonE, isolated from Trichoderma koningii, inhibits edema-inducing, myotoxic and enzymatic activities of PLA2
koninginin F
-
KonF, isolated from Trichoderma koningii, inhibits edema-inducing, myotoxic and enzymatic activities of PLA2
LY 329722
-
i.e. 3-(3-aminooxalyl-1-benzyl-2-ethyl-6-methyl-1H-indol-4-yl)propionic acid
LY311727
-
-
LY315920
-
-
malvidin
-
partial competitive inhibition
Me-Indoxam
methyl 2-(2-oxo-8-phenyloctanamido)acetate
-
-
methyl 2-(2-oxohexadecanamido)acetate
-
-
methyl 2-(7-phenylheptanamido)acetate
-
-
methyl 3-(2-oxohexadecanamido)propanoate
-
-
methyl 5-(2-oxohexadecanamido)pentanoate
-
-
methyl arachidonyl fluorophosphonate
methyl N-(2-oxohexadecanoyl)glycinate
-
reduces the cellular release of arachidonic acid by 30%
methyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
-
-
methyl-arachidonyl fluorophosphonate
an irreversible inhibitor
methylarachidonyl fluorophosphonate
-
inhibits release of [3H]arachidonic acid by a 0.01 mM concentration
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
-
inhibits isozyme cPLA2alpha
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
-
inhibits isozyme cPLA2alpha
N-(2-oxododecanoyl)-L-norleucine
-
reduces the cellular release of arachidonic acid by 21%
N-(4-ethoxybutyl)-2-oxohexadecanamide
-
-
N-(4-[3-(1-(4-fluorophenyl)3-oxo-1,3-dihydroisobenzofuran-1-yl)-2,5-dimethylpyrrol-1-yl]phenyl)acetamide
-
35% inhibition at 0.033 mM
N-(cyclopent-1-en-1-yl)pyrrolidine
ccPLA2-alpha inhibitor, causes almost complete suppression of arachidonic acid release induced by various stimuli. Reduces by 70% the generation of platelet activating factor from macrophages
N-cyclohexyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
-
-
N-ethyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
-
-
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
-
inhibits isozyme cPLA2alpha
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
-
inhibits isozyme cPLA2alpha
N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
-
N-[[(2S,4R)-1-([2-[(2,4-difluorophenyl)carbonyl]phenyl]carbonyl)-4-(tritylsulfanyl)pyrrolidin-2-yl]methyl]-4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]benzamide
-
-
nifedipine
-
-
ochnaflavone
ONO-RS-082
-
reversible PLA2 antagonist, treatment for 45 min causes the intact Golgi ribbon to break up into fragments of disconnected mini-stacks
p-bromophenacyl bromide
-
-
pelargonidin
-
mixed competitive and noncompetitive inhibition, complete inhibition
peonidin
-
mixed competitive and noncompetitive inhibition, partial hyperbolic type of inhibition
petrosaspongiolide M
an anti-inflammatory marine natural product, mechanism of sPLA2-IIA inactivation, overview
petunidin
-
mixed competitive and noncompetitive inhibition, partial hyperbolic type of inhibition
phenyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
-
-
protein p11
-
phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction as annexin A2 complex annexin A2-p11 heterotetramer
-
protocatechuic acid
-
reaches 50% inhibition at concentrations of 3.3 mM
pyrrolidine-1
pyrrolidine-2
pyrrophenone
-
potent gIVaPLA2 inhibitor, attenuates gIVaPLA2 activity in concentration-dependent manner
SB-203580
-
-
SB222657
-
-
SB435495
SB480848
-
darapladib, completely inhibits lp-PLA2 enzyme activity in the whole culture media of THP-1 cells with 0.0001 mM
sodium 2-(1-benzyl-2-ethyl)-3-oxamoylindol-4-yl oxyacetate
-
varespladib sodium or LY315920, most potent sPLA2 inhibitor
sodium deoxycholate
-
-
sphingomyelin
-
suppresses the activating effect of oxidized palmitoyl arachidonyl phosphatidylcholine in a dose-dependent manner, abolishing it almost completely at a concentration 8times as high as that of oxidized palmitoyl arachidonyl phosphatidylcholine. Oxidized palmitoyl arachidonyl phosphatidylcholine completely abolishes the inhibitory effect of low density lipoprotein-incorporated sphingomyelin on the enzyme activity at the oxidized palmitoyl arachidonyl phosphatidylcholine/sphingomyelin concentration ratio 1:2
suramin
the C-terminal region of the enzyme is crucial to the stabilization of the complex with suramin and consequently is a major structural determinant of the inhibitory action of suramin
surfactant protein A
-
-
-
tert-butyl ([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)acetate
-
-
tert-butyl 2-(2-oxohexadecanamido)acetate
-
-
tert-butyl 3-(2-oxo-8-phenyloctanamido)propanoate
-
-
tert-butyl 3-(2-oxohexadecanamido)propanoate
-
-
tert-butyl 3-(7-phenylheptanamido)propanoate
-
-
tert-butyl 5-(2-oxohexadecanamido)pentanoate
-
-
tert-butyl 5-[(2-oxohexadecanoyl)amino]pentanoate
-
reduces the cellular release of arachidonic acid by 11%
thioetheramide phosphatidylcholine
-
exhibits complete competitive inhibition
Tris/maleate buffer
-
-
Triton X-100
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
12-O-tetradecanoylphorbol-13-acetate
-
a protein kinase C agonist, has no effect on Prdx6 expression but leads to about 75% increase in aiPLA2 activity
ATP
-
plasmalogen-specific PLA2, activating
bile acid
-
bile acids cause sPLA2 activity enhancement, revertible by exogenous surfactant administration, overview. Bile acids are likely to contribute to lung injury, causing surfactant inactivation through the increased sPLA2 activity
cardiolipin
-
cytosolic isoform PLA2beta action on phosphatidylcholine vesicles is activated by anionic phosphoinositides and cardiolipin
deoxycholate
-
-
IL-1beta
-
stimulates transient phosphorylation of cPLA2 in a time-dependent manner
-
oxidized palmitoyl arachidonyl phosphatidylcholine
-
either added to the assay medium as separated liposomes or incorporated in varied amounts into low density lipoprotein progressively enhances the activity of purified sPLA2(IIA)
-
phosphate
-
phosphorylation needed for activity
serine
-
human serine dependent PLA2
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
3.6
1,2-diheptanoyl-sn-glycero-3-phosphocholine
-
-
2.4 - 4.3
1,2-dihexanoyl-sn-glycero-3-phosphocholine
0.9
1,2-dinonanoyl-sn-glycero-3-phosphocholine
-
-
0.2
1,2-dioctanoyl-sn-glycero-3-phosphocholine
-
-
0.1
1,2-dioctanoyl-sn-glycero-3-phosphoglycol
-
-
0.01
1-decanoyl-2-(4-nitrophenylglutaryl) phosphate
-
-
0.0137 - 0.0142
1-hexadecyl-2-acetyl-sn-glycerol-3-phosphocholine
0.004
choline plasmalogen
-
-
0.05 - 0.051
phosphatidylcholine
0.02 - 0.024
phosphatidylethanolamine
0.042
platelet activating factor
-
-
additional information
additional information
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0021
cyanidin
-
in an aqueous buffer solution, pH 7.5, containing 94 mM KCl, 9 mM CaCl2, 24 mM Tris and 0.28 mM Triton-X 100
0.018
delphinidin
-
in an aqueous buffer solution, pH 7.5, containing 94 mM KCl, 9 mM CaCl2, 24 mM Tris and 0.28 mM Triton-X 100
0.0064
malvidin
-
in an aqueous buffer solution, pH 7.5, containing 94 mM KCl, 9 mM CaCl2, 24 mM Tris and 0.28 mM Triton-X 100
0.325
pelargonidin
-
in an aqueous buffer solution, pH 7.5, containing 94 mM KCl, 9 mM CaCl2, 24 mM Tris and 0.28 mM Triton-X 100
0.01
peonidin
-
in an aqueous buffer solution, pH 7.5, containing 94 mM KCl, 9 mM CaCl2, 24 mM Tris and 0.28 mM Triton-X 100
0.014
petunidin
-
in an aqueous buffer solution, pH 7.5, containing 94 mM KCl, 9 mM CaCl2, 24 mM Tris and 0.28 mM Triton-X 100
0.0159
SB435495
isozyme Lp-PLA2
0.00059
thioetheramide phosphatidylcholine
-
in an aqueous buffer solution, pH 7.5, containing 94 mM KCl, 9 mM CaCl2, 24 mM Tris and 0.28 mM Triton-X 100
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0007 - 0.0058
(+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
0.025
(2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoic acid
Homo sapiens
-
at 37°C, pH not specified in the publication
0.025
(4R)-6-methyl-4-[(2-oxohexadecanoyl)amino]heptanoic acid
Homo sapiens
-
at 37°C, pH not specified in the publication
0.01
(4S)-4-[(2-oxododecanoyl)amino]octanoic acid
Homo sapiens
-
at 37°C, pH not specified in the publication
0.025
(4S)-4-[(2-oxohexadecanoyl)amino]octanoic acid
Homo sapiens
-
at 37°C, pH not specified in the publication
0.007
(5S)-5-[(2-oxohexadecanoyl)amino]nonanoic acid
Homo sapiens
-
at 37°C, pH not specified in the publication
0.0023
(6Z,9Z,12Z,15Z)-1,1,1-trifluorohenicosa-6,9,12,15-tetraen-2-one
Homo sapiens
-
pH 7.4
0.002
(S)-2-(2-(2-oxohexadecanamido)hexyloxy)acetic acid
Homo sapiens
-
at 37°C, pH not specified in the publication
0.00097
([1-[amino(oxo)acetyl]-3-(biphenyl-2-ylmethyl)-2-(2-methylpropyl)indolizin-8-yl]oxy)acetic acid
Homo sapiens
-
isozyme sPLA2 group IIF
0.00001
([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-benzo[g]indol-4-yl]oxy)acetic acid
Homo sapiens
-
isozyme sPLA2 group IIX
0.0063
1-(1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.01
1-(2-dimethylaminoethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
Homo sapiens
-
above, pH 7.4
0.0015
1-(4-carboxybenzyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.0011
1-(4-octylphenoxy)-3-[5-(1H-tetrazol-5-yl)indol-1-yl]propan-2-one
Homo sapiens
-
-
0.0016
1-(5-nitro-1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.3
1-(carboxymethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.6
1-(carboxypentyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.4
1-(carboxypropyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.01
1-benzyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.01
1-hexyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
Homo sapiens
-
above, pH 7.4
0.0012
1-methyl 5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.000005
1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazole-5-carboxylic acid
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.000026
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-5-carboxylic acid
Homo sapiens
-
-
0.000016
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-6-carboxylic acid
Homo sapiens
-
-
0.00035
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000035
1-[3-(4-octylphenoxy)-2-oxopropyl]-2,3-dihydro-1H-indole-5-carboxylic acid
Homo sapiens
-
pH 7.4
0.00015
1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-5-carboxylic acid
Homo sapiens
-
-
0.000085
1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-6-carboxylic acid
Homo sapiens
-
-
0.000005
1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid
Homo sapiens
-
-
0.000026
1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-6-carboxylic acid
Homo sapiens
-
-
0.000035
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid
Homo sapiens
-
-
0.00039
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
Homo sapiens
-
-
0.0011
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-6-carboxylic acid
Homo sapiens
-
-
0.0005
1-[5-(morpholine-4-carbonyl)indol-1-yl]-3-(4-octylphenoxy)propan-2-one
Homo sapiens
-
-
0.013 - 0.1
2,2'-biphenyl-3,4'-diylbis(4H-chromen-4-one)
0.011 - 0.1
2,2'-biphenyl-4,4'-diylbis(4H-chromen-4-one)
0.024 - 0.1
2,2'-diphenyl-4H,4'H-6,6'-bichromene-4,4'-dione
0.000014
2-(1-benzyl-2-ethyl-4-methoxy-1H-benzo[g]indol-3-yl)-2-oxoacetamide
Homo sapiens
-
isozyme sPLA2 group IIA
0.000007
2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-6,7-benzoindol-4-yloxy)acetic acid
Homo sapiens
-
isozymes sPLA2 group IIE and IID
0.00003
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-benzo[g]indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.000007
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(methylsulfonyl)propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.000021
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.00008
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.000014
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(2-chlorophenyl)sulfonyl]propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.000011
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(2-methylphenyl)sulfonyl]propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.00014
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(3-chlorophenyl)sulfonyl]propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.00054
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(4-chlorophenyl)sulfonyl]propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.00032
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(4-methylphenyl)sulfonyl]propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.00003
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(trifluoromethyl)sulfonyl]propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.00007
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[[2-(trifluoromethyl)phenyl]sulfonyl]propanamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.000016
2-([3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-benzo[g]indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
Homo sapiens
-
isozyme sPLA2 group IIE
0.000007
2-([3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
Homo sapiens
-
isozyme sPLA2 group IIE
0.00066
2-hydroxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.00059
2-methoxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.00005
2-[1-benzyl-2-(2-methylpropyl)-4-(2-oxopropoxy)-1H-indol-3-yl]-2-oxoacetamide
Homo sapiens
-
isozyme sPLA2 group IIX
0.000009
2-[1-benzyl-4-(2-oxopropoxy)-2-propyl-1H-indol-3-yl]-2-oxoacetamide
Homo sapiens
-
isozyme sPLA2 group IIE
0.009
2-[3-(biphenyl-2-ylmethyl)-2-ethyl-8-(2-oxopropoxy)indolizin-1-yl]-2-oxoacetamide
Homo sapiens
-
isozyme sPLA2 group IIE
0.000035
2-[3-(biphenyl-2-ylmethyl)-2-ethyl-8-methoxyindolizin-1-yl]-2-oxoacetamide
Homo sapiens
-
isozyme sPLA2 group IIA
0.0305
3,3'-[[2-(pentyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
Homo sapiens
-
above, pH 7.5, isozyme hGIIA sPLA2
0.0021
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
Homo sapiens
-
pH 7.5, isozyme hGIIA sPLA2
0.0477
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
Homo sapiens
-
above, pH 7.5, isozyme hGIIA sPLA2
0.0031
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
Homo sapiens
-
pH 7.5, isozyme hGIIA sPLA2
0.021
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
Homo sapiens
-
pH 7.5, isozyme hGIIA sPLA2
0.0035
3-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-yl)-4,5-dihydro-1,2,4-oxadiazol-5-one
Homo sapiens
-
-
0.000012
3-(2-methylpropanoyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.00001
3-(2-methylpropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.0187
3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.000036
3-(3-acetamido-2-benzyl-2-ethylindolyl-5-oxy)propane phosphonic acid
Homo sapiens
-
LY311727, IC50 value of 36 nM, group IIa and V sPLA2
0.00021
3-(3-carboxypropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.0053
3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.000023
3-(4-hydroxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000015
3-(4-methoxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000022
3-(5-carboxypentanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000031
3-(6-hydroxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000049
3-(6-methoxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.00001
3-butanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000071
3-hexanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.0035
3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.00271
3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.0035 - 0.1
3-[4-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
0.0045
3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.004
3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.004
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.0008
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.0011
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.0022
3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.00508
3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.009
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.1
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
-
0.00029 - 0.022
3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.014 - 0.1
3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.00028 - 0.01
3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.00028 - 0.018
3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0083
3-[4-[3-(pentyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
pH 7.5, isozyme hGIIA sPLA2
0.0298
3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
Homo sapiens
-
pH 7.5, isozyme hGIIA sPLA2
0.025
4-[(2-oxohexadecanoyl)amino]butanoic acid
Homo sapiens
-
at 37°C, pH not specified in the publication
0.01
5-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-ylmethylidene)thiazolidine-2,4-dione
Homo sapiens
-
above
0.0021
5-[3-(4-octylphenoxy)-2-oxopropoxy]-1-propylindole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.0033
5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
Homo sapiens
-
pH 7.4
0.0065 - 0.1
6-[3-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
0.048 - 0.1
6-[4-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
0.016 - 0.1
amentoflavone
0.0001
annexin A2-p11 heterotetramer
Homo sapiens
-
pH 7.4, 37°C, recombinant enzyme
-
0.00003
bromoenol lactone
Homo sapiens
-
plasmalogen-specific PLA2, suicide inhibitor, IC50 30nM
0.000013
FPL67047XX
Homo sapiens
-
0.00012
indole-5-carboxamide
Homo sapiens
-
-
0.000035
indole-5-carboxylic acid
Homo sapiens
-
-
0.00001
indoxam
Homo sapiens
-
isozyme sPLA2 group IIE
0.00047
LY311727
Homo sapiens
-
-
0.00005
LY315920
Homo sapiens
-
isozyme sPLA2 group IIE
0.0021
methyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.00084
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
Homo sapiens
-
-
0.0005
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
Homo sapiens
-
-
0.00029
N-cyclohexyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.0019
N-ethyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.00037
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
Homo sapiens
-
-
0.00031
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
Homo sapiens
-
-
0.00013
N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
0.003 - 0.1
ochnaflavone
0.00055
phenyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
Homo sapiens
-
37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
additional information
additional information
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.000006
-
isoform cPLA2delta, using 1-palmitoyl-2-arachidonyl-sn-glycerol-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, 0.02 mM Ca2+, at 37°C
0.00001
-
cytosolic colon mucosa PLA2, substrate: 1-palmitoyl-2-oleolylphosphatidylcholine
0.000015
0.000019
-
cytosolic colon mucosa PLA2, substrate: 1-palmitoyl-2-arachidonylphosphatidylcholine
0.00002
-
microsomal colon mucosa PLA2, substrate: 1-palmitoyl-2-arachidonylphosphatidylcholine
0.000021
-
isoform cPLA2epsilon, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, in the absence of Ca2+, at 37°C
0.00004
-
isoform cPLA2epsilon, using 1-palmitoyl-2-arachidonyl-sn-glycerol-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, 0.02 mM Ca2+, at 37°C
0.00006
-
isoform cPLA2delta, using 1-palmitoyl-2-arachidonyl-sn-glycerol-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, in the absence of Ca2+, at 37°C
0.000145
-
isoform cPLA2epsilon, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, 0.02 mM Ca2+, at 37°C
0.00021
-
isoform cPLA2delta, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, 0.02 mM Ca2+, at 37°C
0.0003
0.0011
-
isoform cPLA2alpha, using 1-palmitoyl-2-arachidonyl-sn-glycerol-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, in the absence of Ca2+, at 37°C
0.0014
-
oleate labelled Escherichia coli membrane
0.0016
-
arachidonate labelled Escherichia coli membrane
0.0021
-
arachidonate labelled Escherichia coli membrane
0.0023
-
oleate labelled Escherichia coli membrane
0.0062
-
sigmoid colon mucosa, substrate: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol
0.0071
-
cecal mucosa, substrate: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol
0.0072
-
ascending colon mucosa, substrate: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol
0.0078
-
transverse colon mucosa, substrate: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol
0.0092
-
descending colon mucosa, substrate: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol
0.0225
-
isoform cPLA2delta, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, in the absence of Ca2+, at 37°C
0.05
-
isoform cPLA2gamma, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, 0.02 mM Ca2+, at 37°C
0.0509
-
ileal mucosa, substrate: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol
0.058
-
isoform cPLA2gamma, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, in the absence of Ca2+, at 37°C
0.0609
-
substrate: 1-palmitoyl-2-arachidonylphosphatidylcholine
0.126
-
isoform cPLA2alpha, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, 0.02 mM Ca2+, at 37°C
0.14
-
substrate 1-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine
0.145
-
isoform cPLA2alpha, using 1-palmitoyl-sn-glycero-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, in the absence of Ca2+, at 37°C
0.23
-
isoform cPLA2alpha, using 1-palmitoyl-2-arachidonyl-sn-glycerol-3-phosphocholine as substrate, in 10 mM MOPS, pH 7.2, 0.5 mM EGTA, 100 mM KCl, 0.5 mg/ml bovine serum albumin, 0.02 mM Ca2+, at 37°C
0.259
-
substrate: 1-acyl-2-arachidonoyl-glycerophosphocholine
0.5
-
substrate: 1-palmitoyl-2-arachidonylphosphatidylcholine
0.51
-
substrate: standardized commercial phospholipid emulsion
1.8
-
substrate: 1-palmitoyl-2-linoleoylphosphatidylcholine
110
-
recombinant enzyme, substrate: 1-palmitoyl-2-linoleoylphosphatidylethanolamine
1140
-
substrate: egg yolk emulsion
118
-
substrate: 1,2-didecanoyl-sn-glycero-3-phosphocholine
124
-
substrate: 1,2-dilaureoyl-sn-glycero-3-phosphocholine
155
-
substrate: dioleolyl-sn-phosphatidylethanolamine
1693
-
pH6, micellar 1,2-dioctanoyl-sn-glycero-3-phosphocholine, 0.42 mM Ca2+
171
-
substrate: 1,2-dinonanoyl-sn-glycero-3-phosphocholine
172
-
substrate: 1,2-dioctanoyl-sn-glycero-3-phosphocholine
208
-
substrate: dioleolyl phosphatidylglycerol
221
-
natural enzyme, substrate: 1-palmitoyl-2-linoleoylphosphatidylethanolamine
25
-
substrate: dioleolyl-sn-phosphatidylcholine
3.22
-
substrate: 1,2-dipalmitoyl-phosphatidylcholine
30
-
substrate: 1,2-dipalmitoyl-phosphatidylcholine
306
-
purified PLA2 from ileal mucosa, substrate: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoglycerol
35
-
HSD-PLA2, 21fold purification, platelet activating factor for substrate
57
-
substrate: dimyristoyl-sn-phosphatidylcholine
573
-
pH 8, micellar 1,2-dioctanoyl-sn-glycero-3-phosphocholine, 0.013 mM Ca2+
628.1
purified recombinant His-tagged Lp-PLA2
63
-
in 20 mM HEPES buffer, 20 mM NaCl, 1 mM CaCl2, pH and temperature not specified in the publication
637.9
purified native Lp-PLA2
8.56
-
substrate 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine
9300
-
substrate: 1,2-dioctanoyl-sn-glycero-3-phosphoglycol
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 10
-
optimum at pH 9
7.5 - 8.5
-
substrate: egg yolk emulsion
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
Uniprot
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
peripheral blood
Manually annotated by BRENDA team
-
group IIF sPLA2
Manually annotated by BRENDA team
cPLA2-zeta2
Manually annotated by BRENDA team
-
Lp-PLA2, cells involved in atherogenesis
Manually annotated by BRENDA team
-
high levels of expression of 1-CysPrx/aiPLA2
Manually annotated by BRENDA team
-
sPLA2 present in the limits of the infarcted myocardium
Manually annotated by BRENDA team
-
SH-5YSY cell
Manually annotated by BRENDA team
-
GVIIA PLA2
Manually annotated by BRENDA team
-
group IID and X sPLA2
Manually annotated by BRENDA team
-
high levels of expression of 1-CysPrx/aiPLA2
Manually annotated by BRENDA team
-
group IIC and IIF sPLA2
Manually annotated by BRENDA team
-
group X sPLA2
Manually annotated by BRENDA team
-
group IIE sPLA2
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
isozymes GIVA cPLA2 and GVIA iPLA2
Manually annotated by BRENDA team
-
time-related phosphorylation and translocation of cytosolic gIVaPLA2 to the nucleus for polymorphonuclear leukocytes stimulated with IL-8/CXCL8 in concentration sufficient to cause upstream phosphorylation of MAPKs (ERK-1/2 and p38) and Akt/PKB
Manually annotated by BRENDA team
-
cPLA2-alpha is phosphorylated and translocated to the nucleus
Manually annotated by BRENDA team
-
during phagocytosis, cPLA2alpha translocates to the phagosome. JNK regulates the translocation of cPLA2alpha to phagosomal membranes. Phosphorylation of cPLA2alpha is necessary for translocation
-
Manually annotated by BRENDA team
additional information
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
the enzyme catalyzes the hydrolysis of phospholipid substrates that compose the membrane bilayers
malfunction
metabolism
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
PLPL9_HUMAN
806
0
89903
Swiss-Prot
Mitochondrion (Reliability: 4)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
88000
SDS-PAGE
100000
-
SDS-PAGE
105000
-
endogenous enzyme
135000
-
transfected protein
13700
-
natural PLA2, SDS-PAGE
13900
-
amino acid composition analysis
14000
-
heparin-sepharose affinity chromatography, SDS-PAGE after digestion with thrombin, SDS-PAGE
14100
-
recombinant enzyme, SDS-PAGE
16000
-
SDS-PAGE
25000
-
x * 25000
26000
-
-
40000
44160
-
SDS-PAGE and liquid chromatography
61000
-
SDS-PAGE
75000
-
SDS-PAGE
78000
-
native PAGE
85000
85000 - 88000
-
aggregated form
90000
-
SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
tetramer
4 * 88000 Da, homologous subunits, iPLA2
monomer
oligomer
-
-
additional information
-
the GVIA PLA2 contains multiple ankyrin repeats which may be important in mediating protein-protein interactions
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
phosphoprotein
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
2.4 A x-ray crystal structure
-
group IVA PLA2 isozyme, crystal structure determination and analysis
-
in complex with 6-phenyl-4(R)-(7-phenyl-heptanoylamino)-hexanoic acid
vapor diffusion at 4°C, X-ray structures of human cPLA2delta, capturing an apo state, and in complex with a substrate-like inhibitor
wild-type and H48Q mutant
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A206K
-
site-directed mutagenesis
C47S
-
the mutation results in the loss of peroxidase activity but acidic Ca2+-independent phospholipase A2 activity remains intact
D43N
-
site-directed mutagenesis
D47E
-
site-directed mutagenesis, inactive mutant
D47K
-
site-directed mutagenesis, inactive mutant
DELTAK57/R58
suramin affinity is significantly increased
E89K
-
surface charge replacements, mutant shows increased activitiy at neutral pH, 2.3 times that of the wild-type enzyme at pH 7
F5W
-
site-directed mutagenesis, mutation of the substrate binding pocket leads to reduced enzyme activity, the inhibitory effect of the F5W mutation results from the high affinity of Trp for the membrane-water interface
G30S
mutant shows 50% reduced hydrolytic activity against dioleoylphosphatidylcholine:dioleoylphosphatidylcholine liposome membranes and reduced killing of Gram-negative bacteria
H46N
-
site-directed mutagenesis, inactive mutant
H48A
mutation has a serious effect on the structural integrity of the enzyme
H48N
0.2% catalytic activity
K116A
suramin affinity is increased, inhibitory effect of suramin in relation to wild-type protein is enhanced
K123A
suramin affinity is significantly reduced, inhibitory effect of suramin in relation to wild-type protein is reduced
K15A
suramin affinity is significantly reduced, inhibitory effect of suramin in relation to wild-type protein is reduced
K488N/K543N/K544N
-
site-directed mutagenesis, the mutant shows 2fold increased activity compared to the wild-type enzyme
K554A/D555A/K556A
to crystallize apo-cPLA2d, three surface mutations (K554A, D555A, and K556A) are introduced to decrease surface entropy
M20L
-
according the gapped-duplex method, using amber selection
M8L
-
according the gapped-duplex method, using amber selection
N273
mutation in potential N-glycosylation site, reduction in catalytic activity, mutant is recovered in the soluble fraction
N289
mutation in potential N-glycosylation site, reduction in catalytic activity, mutant is recovered in the soluble fraction
N398
mutation in potential N-glycosylation site, reduction in catalytic activity, mutant is recovered in the soluble fraction
N99
mutation in potential N-glycosylation site, marked reduction in catalytic activity, mutant is mostly retained in the membrane fraction
N99/N273/N289/N398
mutation in all potential glycosylation sites, loss of catalyic activity
R100E
-
surface charge replacements, mutant shows increased activitiy at neutral pH, 2.8, and times that of the wild-type enzyme at pH 7
R42E
-
surface charge replacements, mutant shows increased activitiy at neutral pH, 2.3times that of the wild-type enzyme at pH 7
R54A
suramin affinity is significantly reduced, inhibitory effect of suramin in relation to wild-type protein is reduced
R58A
inhibitory effect of suramin in relation to wild-type protein is reduced
R7A
inhibitory effect of suramin in relation to wild-type protein is reduced
S32A
-
the mutation abolishes acidic Ca2+-independent phospholipase A2 activity while the peroxidase activity remained unaffected
S505A
S505A/S727A
-
site-directed mutagenesis
S505A/S727A/S515A
-
site-directed mutagenesis
S505E
S505E/S727A
-
site-directed mutagenesis
S515A
-
site-directed mutagenesis
S727A
S727E
-
mutation of the phosphorylation site Ser727 leading to a phosphorylation-mimicking mutant, the mutant shows unaltered enzyme activity compared to the wild-type enzyme
S727T
-
mutation of the phosphorylation site Ser727, S727T is as potently inhibited by annexin A2-p11 heterotetramer as the wild type cPLA2alpha, the mutant shows unaltered enzyme activity compared to the wild-type enzyme
T177A
-
the mutation of Thr177 abolishes protein phosphorylation and the increase in MAP kinase-mediated activity of the mutant
T177E
-
the mutation of Thr177 abolishes protein phosphorylation and the increase in MAP kinase-mediated activity of the mutant
Y50F
-
site-directed mutagenesis, inactive mutant
additional information
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
2
-
exposure to acidic conditions, i.e. pH 2 for 60 min at 4°C, causes irreversible loss of activity, stable in basic medium
133895
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
20
-
after 7 days more than 95% of the activity remains, in presence or absence of Ca2+, pH ranging from 4.5 to 9.0
50
-
highly susceptible to temperatures above 50°C under acidic and neutral conditions
57
-
significantly reduced activity at 57°C
70
-
group V sPLA2 shows a half-life for inactivation of 10 min., group IIa sPLA2 retains 75% of activity after 1 h
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20°C, in 5 mM Tris-HCl buffer, pH 7.5
-
-20°C, lyophilized enzyme, no loss of activity over 3 months
-
-4°C, for months without losing enzymatic activity
-
-4°C, more than 2 weeks without precipitation
-
-70°C, with bovine serum albumin, loss of enzyme activity only partially avoided
-
-80°C
-
room temperature, in presence or absence of Ca2+, pH ranging from 4.5 to 9.0, after 7 days more than 95% of the activity remains
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
by single-step cation-exchange chromatography
-
cation exchange column, reversed phase HPLC
-
column chromatography steps, 11700fold
-
column chromatography, 4500fold
-
column chromatography, gel electrophoresis, 1206fold
-
cPLA2s and sPLA2s
gel filtration
-
gel filtration chromatography
-
gel filtration chromatography, more than 100fold
-
GVIA PLA2
-
ion exchange chromatography
-
ion-exchange chromatography, gel-filtration
-
Ni-NTA affinity chromatography
-
Ni-NTA resin column chromatography
-
recombinant C-terminally His6-tagged Lp-PLA2 from Pichia pastoris by nickel affinity chromatography
recombinant full-length wild-type and mutant cPLA2alphas containing the affinity peptide YHHHHHH
-
recombinant His-tagged enzyme by nickel affinity chromatography and gel filtration
-
recombinant human group IIA PLA2isozyme and isozyme hIBPLA2 from Escherichia coli strain BL21(DE3)
recombinant solubilized wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by heparin affinity chromatography and gel filtration to homogeneity
-
recombinant tagged cPLA2 from Spodoptera frugiperda okadaic acid-treated Sf9 cells
-
semipurification, heparin-Sepharose affinity chromatography
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
into pcDNA3.1 for later transfections
CHO-K1 cells or HEK cells stably expressing N-terminal enhanced green fluorescent protein-cPLA2alpha fusion protein
-
cPLA2-alpha and sPLA2s
cPLA2gamma, expressed in Sf9 cells, lung fibroblasts and KEK293 cells
-
DNA and amino acid sequence determination and analysis, expression of wild-type and mutant isozymes sPLA2-X in Spodoptery frugiperda Sf9 cells using the baculovirus transfection system, expression of wild-type and D47K mutant isozymes sPLA2-X in HEK-293 cells
-
DNA-coding sequence subcloned into the vector pET3a, and expressed as inclusion bodies in Escherichia coli strain BL21(DE3)[pLysS]
-
expressed in insect cells (Sf9)
expressed in Sf9 insect cells
-
expression in COS-7 cell
expression in Escherichia coli
-
expression in HEK293 cells
expression of full-length wild-type and mutant cPLA2alphas containing the affinity peptide YHHHHHH fused to the C-terminal Ala749, involving a recombinant adenovirus
-
expression of His-tagged wild-type and mutant enzymes
-
expression of isozyme hIBPLA2 and wild-type and mutant isozymes hIIAPLA2 in Escherichia coli strain BL21(DE3)
expression of isozyme sPLA2IB2 in HEK293 cells
expression of isozymes in HEK293 cells
expression of wild-type and mutant enzymes in Escherichia coli strain BL21(DE3) in inclusion bodies
-
for construction of the cPLA2-luc plasmid, cPLA2 promoter, a region spanning -2,375 to -75 bp, cloned into pGL3-basic vector
-
full length human cPLA2, residues 1-749, expressed in E5-CHO-cells
-
GIVA PLA2 and GVIIA PLA2
-
GVIA-2 iPLA2 is membrane-associated when overexpressed in COS-7 cells as well as rat vascular smooth muscle cells. The human group VIA PLA2 gene yields multiple splice variants, including GVIA-1, GVIA-2, GVIA-3 PLA2, GVIA ankyrin-1 and GVIA ankyrin-2
-
into baculovirus, transfection of SF9 insect cells
-
into M13-vector mp8 for site directed mutagenesis, into pUEX 1 vector for tranformation of Escherichia coli
-
into pAcYM1, transfer into baculovirus, transfection of Sf9 S.frugiperda cells
-
into pET21a vector, transformation of Escherichia coli strain BL21(DE3)
-
into pET28a(+) vector, transformation of Escherichia coli strain BL21
-
Lp-PLA2 gene, cloning from differentiated THP-1 cells, DNA and amino acid sequence determination and anaylsis, expression of C-terminally His6-tagged enzyme in Pichia pastoris strain GS115 and Escherichia coli
macrophages transfected with the construct EGFP-cPLA2alpha, ECFP-S505A or ECFP-S505E
-
overexpression of type IIa human PLA2 in mice correlating with elevated atherosclerotic lesions, membranes with elevated cholesterol content can be generated by PLA2 activation, mechanism, overview
-
wild type and mutant cPLA2s overexpression in HEK293 EcR or HEK293-BLT1 cells, expression of fluorescence of FLAG-tagged cPLA2 in Spodoptera frugiperda Sf9 cells using the baculovirus transfection method
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
fetal bovine serum and serum starved conditions stimulate cPLA2alpha
-
IL-1beta induces cPLA2 protein expression in a time-dependent manner with a maximal response within 16-24 h. IL-1beta also enhances cPLA2 mRNA accumulation in a time-dependent manner with a maximal response within 5 h. IL-1beta-induced cPLA2 expression requires ongoing transcription and translation. Association of p300 and histone H4 leads to cPLA2 gene transcription. In human tracheal smooth muscle cells, activation of MAPKs (p42/p44 MAPK and p38 MAPK), NF-kappaB, JNK1/2 an the co-activator p300 are essential for IL-1beta-induced cPLA2 expression and prostaglandin E2 secretion
-
IL-1beta-mediated induction of cPLA2 expression is abolished by either actinomycin D or cycloheximide in a concentration-dependent manner. SB202190 or SP600125 inhibit cPLA2 protein and mRNA expression induced by IL-1beta. Transfection with JNK2 siRNA or p300 siRNA blocks cPLA2 expression induced by IL-1beta. AACOCF3, U0126, SB202190, SP600125, or helenalin significantly inhibit IL-1beta-stimulated prostaglandin E2 synthesis linked to cPLA2 activity
-
iPLA2 mRNA expression is increased in neutrophils from people with diabetes and mediates superoxide generation
-
lipopolysaccharide has no effect on iPLA2 mRNA and does not induce expression of cPLA2-zeta. Lipopolysaccharide does not induce or enhance the release of any sPLA2s. Lipopolysaccharide neither enhances the sPLA2s GIID, GIIE, GIIF, GX and GXIIA constitutively expressed by macrophages nor induces the expression of GIB and GIII, which are undetectable in resting cells
Lp-PLA2 is highly expressed in the necrotic core of atherosclerotic lesions
-
macrophages express the alpha isoform of group IV and group VIA cPLA2. Stimulation of macrophages with lipopolysaccharide for 24 hours induces on average a 7fold increase of cPLA2-alpha expression. GIIA is also upregulated by lipopolysaccharide. Both Mycobacterium tuberculosis purified protein derivative and lipopolysaccharide induce arachidonic acid mobilization via cPLA2-alpha in macrophages
oxidized low density lipoprotein, and more specifically its unhydrolyzed oxidized phospholipids, upregulate lp-PLA2 expression in monocytes through the phosphatidylinositol 3-kinase and p38 mitogen-activating protein kinase pathway. Oxidized low density lipoprotein-treated cells produce lp-PLA2 mRNA in a concentration- and time-dependent manner. Oxidized high density lipoprotein can also induce lp-PLA2 expression
-
siRNA1 reduces the expression of cPLA2alpha
-
transfection with iPLA2 siRNA results in ca. 50% reduction in mRNA levels of iPLA2
-
unstimulated and low density lipoprotein-treated THP-1 cells fail to produce detectable levels of lp-PLA2. Inhibition of either phosphatidylinositol 3-kinase (by LY294002 and wortmannin) or p38 mitogen-activating protein kinase (by SB203580 and SB202190) completely blocks oxidized low density lipoprotein-induced lp-PLA2 expression. Neither platelet activating factor and lyso-platelet activating factor nor 1-palmitoyl-sn-glycerol-3-phosphocholine and high density lipoprotein can induce lp-PLA2 expression
-
RENATURED/Commentary
ORGANISM
UNIPROT
LITERATURE
recombinant wild-type and mutant enzymes from Escherichia coli inclusion bodies
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
-
simple and inexpensive protein expression, refolding and purification system may be useful for site-directed mutagenesis experiments of sPLA2-IID which will advance the understanding of the structure–function relationship and biological effects of the protein
drug development
medicine
pharmacology
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Dessen, A.; Tang, J.; Schmidt, H.; Stahl, M.; Clark, J.D.; Seehra, J.; Somers, W.S.
Crystal structure of human cytosolic Phospholipase A2 reveals a novel topology and catalytic mechanism
Cell
97
349-360
1999
Homo sapiens
Manually annotated by BRENDA team
Larsson Forsell, P.K.A.; Kennedy, B.P.; Claesson, H.E.
The human calcium-independent phospholipase A2 gene
Eur. J. Biochem.
262
575-585
1999
Rattus norvegicus, Homo sapiens (O60733), Homo sapiens
Manually annotated by BRENDA team
Rice, S.Q.J.; Southan, C.; Boyd, H.F.; Terrett, J.A.; MacPhee, C.H.; Moores, K.; Gloger, I.S.; Tew, D.G.
Expression, purification and characterization of a human serine-dependent phospholipase A2 with high specificity for oxidized phospholipids and platelet activating factor
Biochem. J.
330
1309-1315
1998
Homo sapiens
-
Manually annotated by BRENDA team
Han, S.K.; Yoon, E.T.; Cho, W.
Bacterial expression and characterization of human secretory class V phospholipase A2
Biochem. J.
331
353-357
1998
Homo sapiens
-
Manually annotated by BRENDA team
Chen, D.; Dennis, E.A.
Expression and characterization of human group V phospholipase A2
Biochim. Biophys. Acta
1394
57-64
1998
Homo sapiens, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Akiba, S.; Dodia, C.; Chen, X.; Fisher, A.B.
Characterization of acidic Ca2+-independent phospholipase A2 of bovine lung
Comp. Biochem. Physiol. B
120
393-404
1998
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Lamura, E.; Hillier, K.; Kinkaid, A.; Wilton, D.
Compartmentalisation and characteristics of a Ca2+-dependent phospholipase A2 in human colon mucosa
Biochem. Pharmacol.
53
1323-1332
1997
Homo sapiens
Manually annotated by BRENDA team
Han, S.K.; Lee, B.I.; Cho, W.
Bacterial expression and characterisation of human pancreatic phospholipase A2
Biochim. Biophys. Acta
1346
185-192
1997
Homo sapiens
Manually annotated by BRENDA team
Yang, H.C.; Farooqui, A.A.; Horrocks, L.A.
Characterization of plasmalogen-selective phospholipase A2 from bovine brain
Adv. Exp. Med. Biol.
416
309-313
1996
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Kawauchi, Y.; Takasaki, J.; Matsuura, Y.; Masuho, Y.
Preparation and characterization of human rheumatoid arthritic synovial fluid phospholipase A2 produced by recombinant baculovirus-infected cells
J. Biochem.
116
82-87
1994
Homo sapiens
-
Manually annotated by BRENDA team
Minami, T.; Tojo, H.; Shinomura, Y.; Matsuzawa, Y.; Okamoto, M.
Purification and characterization of a phospholipase A2 from human ileal mucosa
Biochim. Biophys. Acta
1170
125-130
1993
Homo sapiens
Manually annotated by BRENDA team
Rehfeldt, W.; Resch, K.; Goppelt-Struebe, M.
Cytosolic phospholipase A2 from human monocytic cells: characterization of substrate specificity and Ca2+-dependent membrane association
Biochem. J.
293
255-261
1993
Homo sapiens
Manually annotated by BRENDA team
Hoffmann, G.E.; Schneider, E.; Brand, K.; Kozumplik, V.; Fateh-Moghadam, S.
Characterization of a phospholipase A2 in human serum
Eur. J. Clin. Chem. Clin. Biochem.
30
111-117
1992
Homo sapiens
Manually annotated by BRENDA team
Franken, P.A.; van den Berg, L.; Huang, J.; Gunyuzlu, P.; Lugtigheid, R.B.; Verheij, H.M.; de Haas, G.H.
Purification and characterization of a mutant human platelet phospholipase A2 expressed in Escherichia coli
Eur. J. Biochem.
203
89-98
1992
Homo sapiens, Naja melanoleuca, Sus scrofa
Manually annotated by BRENDA team
Takayama, K.; Kudo, I.; Kim, D.K.; Nagata, K.; Nozawa, Y.; Inoue, K.
Purification and characterization of human platelet phospholipase A2 which preferentially hydrolyzes an arachidonoyl residue
FEBS Lett.
282
326-330
1991
Homo sapiens
Manually annotated by BRENDA team
Donne-Op den Kelder, G.M.; de Haas, G.H.; Egmond, M.R.
Localization of the second calcium ion binding site in porcine and equine phospholipase A2
Biochemistry
22
2470-2478
1983
Bos taurus, Equus caballus, Homo sapiens, Sus scrofa
Manually annotated by BRENDA team
Sahu, S.; Lynn, W.S.
Characterization of phospholipase A from pulmonary secretions of patients with alveolar proteinosis
Biochim. Biophys. Acta
489
307-317
1977
Homo sapiens
Manually annotated by BRENDA team
Perisic, O.; Fong, S.; Lynch, D.E.; Bycroft, M.; Williams, R.L.
Crystal structure of a calcium-phospholipid binding domain from cytosolic phospholipase A2
J. Biol. Chem.
273
1596-1604
1998
Homo sapiens
Manually annotated by BRENDA team
Edwards, S.H.; Thompson, D.; Baker, S.F.; Wood, S.P.; Wilton, D.C.
The crystal structure of the H48Q active site mutant of human group IIA secreted phospholipase A2 at 1.5 A resolution provides an insight into the catalytic mechanism
Biochemistry
41
15468-15476
2002
Homo sapiens (P14555), Homo sapiens
Manually annotated by BRENDA team
Winstead, M.V.; Balsinde, J.; Dennis, E.A.
Calcium-independent phospholipase A2: structure and function
Biochim. Biophys. Acta
1488
28-39
2000
Homo sapiens, Mammalia, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Shin, H.S.; Chin, M.R.; Kim, J.S.; Chung, J.H.; Ryu, C.K.; Jung, S.Y.; Kim, D.K.
Purification and characterization of a cytosolic, 42-kDa and Ca2+-dependent phospholipase A2 from bovine red blood cells: its involvement in Ca2+-dependent release of arachidonic acid from mammalian red blood cells
J. Biol. Chem.
277
21086-21094
2002
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Stewart, A.; Ghosh, M.; Spencer, D.M.; Leslie, C.C.
Enzymatic properties of human cytosolic phospholipase A2g
J. Biol. Chem.
277
29526-29536
2002
Homo sapiens
Manually annotated by BRENDA team
Farooqui, A.A.; Ong, W.Y.; Horrocks, L.A.; Farooqui, T.
Brain cytosolic phospholipase A2: localization, role, and involvement in neurological diseases
Neuroscientist
6
169-180
2000
Bos taurus, Homo sapiens, Mammalia, Rattus norvegicus
-
Manually annotated by BRENDA team
Rose, T.M.; Prestwich, G.D.
Fluorogenic phospholipids as head group-selective reporters of phospholipase A activity
ACS Chem. Biol.
1
83-92
2006
Streptomyces violaceoruber, Apis mellifera, Bos taurus, Homo sapiens, Naja mossambica
Manually annotated by BRENDA team
Qin, S.; Pande, A.H.; Nemec, K.N.; Tatulian, S.A.
The N-terminal alpha-helix of pancreatic phospholipase A2 determines productive-mode orientation of the enzyme at the membrane surface
J. Mol. Biol.
344
71-89
2004
Homo sapiens
Manually annotated by BRENDA team
Pande, A.H.; Qin, S.; Nemec, K.N.; He, X.; Tatulian, S.A.
Isoform-specific membrane insertion of secretory phospholipase A2 and functional implications
Biochemistry
45
12436-12447
2006
Apis mellifera (P00630), Apis mellifera, Homo sapiens (P14555), Homo sapiens
Manually annotated by BRENDA team
Nemec, K.N.; Pande, A.H.; Qin, S.; Bieber Urbauer, R.J.; Tan, S.; Moe, D.; Tatulian, S.A.
Structural and functional effects of tryptophans inserted into the membrane-binding and substrate-binding sites of human group IIA phospholipase A2
Biochemistry
45
12448-12460
2006
Homo sapiens
Manually annotated by BRENDA team
Gora, S.; Lambeau, G.; Bollinger, J.G.; Gelb, M.; Ninio, E.; Karabina, S.
The proinflammatory mediator Platelet Activating Factor is an effective substrate for human group X secreted phospholipase A2
Biochim. Biophys. Acta
1761
1093-1099
2006
Homo sapiens
Manually annotated by BRENDA team
Hess, M.; Schulze Elfringhoff, A.; Lehr, M.
1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: bioisosteric replacement of the carboxylic acid and carboxamide moiety
Bioorg. Med. Chem.
15
2883-2891
2007
Homo sapiens
Manually annotated by BRENDA team
Moon, T.C.; Quan, Z.; Kim, J.; Kim, H.P.; Kudo, I.; Murakami, M.; Park, H.; Chang, H.W.
Inhibitory effect of synthetic C-C biflavones on various phospholipase A2s activity
Bioorg. Med. Chem.
15
7138-7143
2007
Homo sapiens, Homo sapiens (P47712)
Manually annotated by BRENDA team
Davis, B.; Koster, G.; Douet, L.J.; Scigelova, M.; Woffendin, G.; Ward, J.M.; Smith, A.; Humphres, J.; Burnand, K.G.; Macphee, C.H.; Postle, A.D.
Electrospray ionization mass spectrometry identifies substrates and products of lipoprotein-associated phospholipase A2 in oxidized human low density lipoprotein
J. Biol. Chem.
283
6428-6437
2007
Homo sapiens
Manually annotated by BRENDA team
Touaibia, M.; Djimde, A.; Cao, F.; Boilard, E.; Bezzine, S.; Lambeau, G.; Redeuilh, C.; Lamouri, A.; Massicot, F.; Chau, F.; Dong, C.Z.; Heymans, F.
Inhibition of secreted phospholipase A2. 4-glycerol derivatives of 4,5-dihydro-3-(4-tetradecyloxybenzyl)-1,2,4-4H-oxadiazol-5-one with broad activities
J. Med. Chem.
50
1618-1626
2007
Homo sapiens, Sus scrofa
Manually annotated by BRENDA team
Kim, J.O.; Chakrabarti, B.K.; Guha-Niyogi, A.; Louder, M.K.; Mascola, J.R.; Ganesh, L.; Nabel, G.J.
Lysis of human immunodeficiency virus type 1 by a specific secreted human phospholipase A2
J. Virol.
81
1444-1450
2007
Homo sapiens
Manually annotated by BRENDA team
Zhang, F.; Wang, Y.
Cloning, expression, and purification of lipoprotein-associated phospholipase A2 in Pichia pastoris
Mol. Biotechnol.
33
29-36
2006
Homo sapiens (Q13093)
Manually annotated by BRENDA team
Ho, T.C.; Chen, S.L.; Yang, Y.C.; Lo, T.H.; Hsieh, J.W.; Cheng, H.C.; Tsao, Y.P.
Cytosolic phospholipase A2-alpha is an early apoptotic activator in PEDF-induced endothelial cell apoptosis
Am. J. Physiol. Cell Physiol.
296
C273-C284
2009
Homo sapiens
Manually annotated by BRENDA team
Wu, Y.; Feinstein, S.I.; Manevich, Y.; Chowdhury, I.; Pak, J.H.; Kazi, A.; Dodia, C.; Speicher, D.W.; Fisher, A.B.
Mitrogen-activated protein kinase-mediated phosphorylation of peroxiredoxin 6 regulates its phospholipase A2 activity
Biochem. J.
419
669-679
2009
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Antonopoulou, G.; Barbayianni, E.; Magrioti, V.; Cotton, N.; Stephens, D.; Constantinou-Kokotou, V.; Dennis, E.A.; Kokotos, G.
Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A2 enzymes
Bioorg. Med. Chem.
16
10257-10269
2008
Homo sapiens
Manually annotated by BRENDA team
Fritsche, A.; Elfringhoff, A.S.; Fabian, J.; Lehr, M.
1-(2-Carboxyindol-5-yloxy)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis, biological activity, metabolic stability, and solubility
Bioorg. Med. Chem.
16
3489-3500
2008
Homo sapiens
Manually annotated by BRENDA team
Simonsen, A.C.
Activation of phospholipase A2 by ternary model membranes
Biophys. J.
94
3966-3975
2008
Homo sapiens
Manually annotated by BRENDA team
Kim, C.; Kim, J.Y.; Kim, J.H.
Cytosolic phospholipase A2, lipoxygenase metabolites, and reactive oxygen species
BMB Rep.
41
555-559
2008
Homo sapiens
Manually annotated by BRENDA team
Burke, J.E.; Dennis, E.A.
Phospholipase A2 biochemistry
Cardiovasc. Drugs Ther.
23
49-59
2009
Apis mellifera, Bitis gabonica, Bos taurus, Crotalus sp., Homo sapiens, Mus musculus, Naja naja, Oryza sativa, Rattus norvegicus, Sus scrofa, Protoparvovirus
Manually annotated by BRENDA team
Monti, M.C.; Casapullo, A.; Cavasotto, C.N.; Tosco, A.; Dal Piaz, F.; Ziemys, A.; Margarucci, L.; Riccio, R.
The binding mode of petrosaspongiolide M to the human group IIA phospholipase A2: exploring the role of covalent and noncovalent interactions in the inhibition process
Chemistry
15
1155-1163
2009
Homo sapiens (P14555), Homo sapiens
Manually annotated by BRENDA team
De Luca, D.; Minucci, A.; Zecca, E.; Piastra, M.; Pietrini, D.; Carnielli, V.P.; Zuppi, C.; Tridente, A.; Conti, G.; Capoluongo, E.D.
Bile acids cause secretory phospholipase A2 activity enhancement, revertible by exogenous surfactant administration
Intensive Care Med.
35
321-326
2009
Homo sapiens
Manually annotated by BRENDA team
Burke, J.E.; Hsu, Y.H.; Deems, R.A.; Li, S.; Woods, V.L.; Dennis, E.A.
A phospholipid substrate molecule residing in the membrane surface mediates opening of the lid region in group IVA cytosolic phospholipase A2
J. Biol. Chem.
283
31227-31236
2008
Homo sapiens (P47712)
Manually annotated by BRENDA team
Tian, W.; Wijewickrama, G.T.; Kim, J.H.; Das, S.; Tun, M.P.; Gokhale, N.; Jung, J.W.; Kim, K.P.; Cho, W.
Mechanism of regulation of group IVA phospholipase A2 activity by Ser727 phosphorylation
J. Biol. Chem.
283
3960-3971
2008
Homo sapiens
Manually annotated by BRENDA team
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
Homo sapiens
Manually annotated by BRENDA team
Hess, M.; Schulze Elfringhoff, A.; Lehr, M.
Design and synthesis of 3-pyrrol-3-yl-3H-isobenzofuran-1-ones as inhibitors of human cytosolic phospholipase A2alpha
J. Enzyme Inhib. Med. Chem.
23
946-957
2008
Homo sapiens
Manually annotated by BRENDA team
Oslund, R.C.; Cermak, N.; Gelb, M.H.
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2
J. Med. Chem.
51
4708-4714
2008
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Baskakis, C.; Magrioti, V.; Cotton, N.; Stephens, D.; Constantinou-Kokotou, V.; Dennis, E.A.; Kokotos, G.
Synthesis of polyfluoro ketones for selective inhibition of human phospholipase A2 enzymes
J. Med. Chem.
51
8027-8037
2008
Homo sapiens
Manually annotated by BRENDA team
Souza, A.D.; Rodrigues-Filho, E.; Souza, A.Q.; Pereira, J.O.; Calgarotto, A.K.; Maso, V.; Marangoni, S.; Da Silva, S.L.
Koninginins, phospholipase A2 inhibitors from endophytic fungus Trichoderma koningii
Toxicon
51
240-250
2008
Homo sapiens, Bothrops jararacussu
Manually annotated by BRENDA team
Methot, M.; Demers, E.; Bussieres, S.; Desbat, B.; Breton, R.; Salesse, C.
Phospholipid monolayer hydrolysis by cytosolic phospholipase A2 gamma and lecithin retinol acyl transferase
Colloids Surf. A Physicochem. Eng. Asp.
321
147-150
2008
Homo sapiens
-
Manually annotated by BRENDA team
Judson, B.L.; Brown, W.J.
Assembly of an intact Golgi complex requires phospholipase A2 (PLA2) activity, membrane tubules, and dynein-mediated microtubule transport
Biochem. Biophys. Res. Commun.
389
473-477
2009
Homo sapiens
Manually annotated by BRENDA team
Giannattasio, G.; Lai, Y.; Granata, F.; Mounier, C.M.; Nallan, L.; Oslund, R.; Leslie, C.C.; Marone, G.; Lambeau, G.; Gelb, M.H.; Triggiani, M.
Expression of phospholipases A2 in primary human lung macrophages: role of cytosolic phospholipase A2-alpha in arachidonic acid release and platelet activating factor synthesis
Biochim. Biophys. Acta
1791
92-102
2009
Homo sapiens (O15496), Homo sapiens
Manually annotated by BRENDA team
Bovens, S.; Kaptur, M.; Elfringhoff, A.S.; Lehr, M.
1-(5-Carboxyindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis and properties of bioisosteric benzimidazole, benzotriazole and indazole analogues
Bioorg. Med. Chem. Lett.
19
2107-2111
2009
Homo sapiens
Manually annotated by BRENDA team
Boukli, L.; Touaibia, M.; Meddad-Belhabich, N.; Djimde, A.; Park, C.; Kim, J.; Yoon, J.; Lamouri, A.; Heymans, F.
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: Synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines
Bioorg. Med. Chem.
16
1242-1253
2008
Homo sapiens, Sus scrofa
Manually annotated by BRENDA team
Barbayianni, E.; Stephens, D.; Grkovich, A.; Magrioti, V.; Hsu, Y.H.; Dolatzas, P.; Kalogiannidis, D.; Dennis, E.A.; Kokotos, G.
2-Oxoamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudodipeptides
Bioorg. Med. Chem.
17
4833-4843
2009
Homo sapiens
Manually annotated by BRENDA team
Wang, W.Y.; Li, J.; Yang, D.; Xu, W.; Zha, R.P.; Wang, Y.P.
OxLDL stimulates lipoprotein-associated phospholipase A2 expression in THP-1 monocytes via PI3K and p38 MAPK pathways
Cardiovasc. Res.
85
845-852
2010
Homo sapiens
Manually annotated by BRENDA team
Chalbot, S.; Zetterberg, H.; Blennow, K.; Fladby, T.; Grundke-Iqbal, I.; Iqbal, K.
Cerebrospinal fluid secretory Ca2+-dependent phospholipase A2 activity is increased in Alzheimer disease
Clin. Chem.
55
2171-2179
2009
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Garcia-Garcia, H.M.; Serruys, P.W.
Phospholipase A2 inhibitors
Curr. Opin. Lipidol.
20
327-332
2009
Homo sapiens, Sus scrofa
Manually annotated by BRENDA team
Dharmappa, K.K.; Mohamed, R.; Shivaprasad, H.V.; Vishwanath, B.S.
Genistein, a potent inhibitor of secretory phospholipase A2: a new insight in down regulation of inflammation
Inflammopharmacology
18
25-31
2010
Homo sapiens
Manually annotated by BRENDA team
Gubern, A.; Casas, J.; Barcelo-Torns, M.; Barneda, D.; de la Rosa, X.; Masgrau, R.; Picatoste, F.; Balsinde, J.; Balboa, M.A.; Claro, E.
Group IVA phospholipase A2 is necessary for the biogenesis of lipid droplets
J. Biol. Chem.
283
27369-27382
2008
Homo sapiens
Manually annotated by BRENDA team
Lee, C.W.; Lee, I.T.; Lin, C.C.; Lee, H.C.; Lin, W.N.; Yang, C.M.
Activation and induction of cytosolic phospholipase A2 by IL-1beta in human tracheal smooth muscle cells: role of MAPKs/p300 and NF-kappaB
J. Cell. Biochem.
109
1045-1056
2010
Homo sapiens
Manually annotated by BRENDA team
Mouchlis, V.D.; Mavromoustakos, T.M.; Kokotos, G.
Design of new secreted phospholipase A2 inhibitors based on docking calculations by modifying the pharmacophore segments of the FPL67047XX inhibitor
J. Comput. Aided Mol. Des.
24
107-115
2010
Homo sapiens (P14555)
Manually annotated by BRENDA team
Casas, J.; Meana, C.; Esquinas, E.; Valdearcos, M.; Pindado, J.; Balsinde, J.; Balboa, M.A.
Requirement of JNK-mediated phosphorylation for translocation of group IVA phospholipase A2 to phagosomes in human macrophages
J. Immunol.
183
2767-2774
2009
Homo sapiens
Manually annotated by BRENDA team
Ayilavarapu, S.; Kantarci, A.; Fredman, G.; Turkoglu, O.; Omori, K.; Liu, H.; Iwata, T.; Yagi, M.; Hasturk, H.; Van Dyke, T.E.
Diabetes-induced oxidative stress is mediated by Ca2+-independent phospholipase A2 in neutrophils
J. Immunol.
184
1507-1515
2010
Homo sapiens
Manually annotated by BRENDA team
Meliton, A.Y.; Munoz, N.M.; Meliton, L.N.; Binder, D.C.; Osan, C.M.; Zhu, X.; Dudek, S.M.; Leff, A.R.
Cytosolic group IVa phospholipase A2 mediates IL-8/CXCL8-induced transmigration of human polymorphonuclear leukocytes in vitro
J. Inflamm.
7
14
2010
Homo sapiens
Manually annotated by BRENDA team
Burke, J.; Dennis, E.
Phospholipase A2 structure/function, mechanism, and signaling
J. Lipid Res.
50 Suppl
S237-S242
2009
Apis mellifera, Homo sapiens, Mus musculus, Naja naja
Manually annotated by BRENDA team
Dreiseitel, A.; Korte, G.; Schreier, P.; Oehme, A.; Locher, S.; Hajak, G.; Sand, P.G.
sPhospholipase A(2) is inhibited by anthocyanidins
J. Neural Transm.
116
1071-1077
2009
Homo sapiens
Manually annotated by BRENDA team
Korotaeva, A.A.; Samoilova, E.V.; Piksina, G.F.; Prokazova, N.V.
Oxidized phosphatidylcholine stimulates activity of secretory phospholipase A2 group IIA and abolishes sphingomyelin-induced inhibition of the enzyme
Prostaglandins Other Lipid Mediat.
91
38-41
2010
Homo sapiens
Manually annotated by BRENDA team
Fonseca, R.G.; Ferreira, T.L.; Ward, R.J.
Refolding and purification of the human secreted group IID phospholipase A2 expressed as inclusion bodies in Escherichia coli
Protein Expr. Purif.
67
82-87
2009
Homo sapiens
Manually annotated by BRENDA team
Nevalainen, T.J.
1-Cysteine peroxiredoxin: A dual-function enzyme with peroxidase and acidic Ca2+-independent phospholipase A2 activities
Biochimie
92
638-644
2010
Homo sapiens
Manually annotated by BRENDA team
Ghomashchi, F.; Naika, G.S.; Bollinger, J.G.; Aloulou, A.; Lehr, M.; Leslie, C.C.; Gelb, M.H.
Interfacial kinetic and binding properties of mammalian group IVB phospholipase A2 (cPLA2beta) and comparison with the other cPLA2 isoforms
J. Biol. Chem.
285
36100-36111
2010
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Madsen, J.J.; Linderoth, L.; Subramanian, A.K.; Andresen, T.L.; Peters, G.H.
Secretory phospholipase A2 activity toward diverse substrates
J. Phys. Chem. B
115
6853-6861
2011
Agkistrodon piscivorus piscivorus, Apis mellifera (P00630), Homo sapiens (P14555)
Manually annotated by BRENDA team
Schmidt, J.A.; Kalkofen, D.N.; Donovan, K.W.; Brown, W.J.
A role for phospholipase A2 activity in membrane tubule formation and TGN trafficking
Traffic
11
1530-1536
2010
Homo sapiens
Manually annotated by BRENDA team
Qiu, S.; Lai, L.
Tailoring the pH dependence of human non-pancreatic secretory phospholipase A2 by engineering surface charges
Appl. Biochem. Biotechnol.
171
1454-1464
2013
Homo sapiens
Manually annotated by BRENDA team
Aragao, E.A.; Vieira, D.S.; Chioato, L.; Ferreira, T.L.; Lourenzoni, M.R.; Silva, S.R.; Ward, R.J.
Characterization of suramin binding sites on the human group IIA secreted phospholipase A2 by site-directed mutagenesis and molecular dynamics simulation
Arch. Biochem. Biophys.
519
17-22
2012
Homo sapiens (P14555)
Manually annotated by BRENDA team
Fonseca-Maldonado, R.; Ferreira, T.L.; Ward, R.J.
The bactericidal effect of human secreted group IID phospholipase A2 results from both hydrolytic and non-hydrolytic activities
Biochimie
94
1437-1440
2012
Homo sapiens (Q9UNK4), Homo sapiens
Manually annotated by BRENDA team
Hiraoka, M.; Okamoto, K.; Ohguro, H.; Abe, A.
Role of N-glycosylation of human lysosomal phospholipase A2 for the formation of catalytically active enzyme
J. Lipid Res.
54
3098-3105
2013
Homo sapiens (Q8NCC3), Homo sapiens
Manually annotated by BRENDA team
Xu, S.; Pei, R.; Guo, M.; Han, Q.; Lai, J.; Wang, Y.; Wu, C.; Zhou, Y.; Lu, M.; Chen, X.
Cytosolic phospholipase A2 gamma is involved in hepatitis C virus replication and assembly
J. Virol.
86
13025-13037
2012
Homo sapiens
Manually annotated by BRENDA team
Duvernay, M.T.; Matafonov, A.; Lindsley, C.W.; Hamm, H.E.
Platelet lipidomic profiling novel insight into cytosolic phospholipase A2alpha activity and its role in human platelet activation
Biochemistry
54
5578-5588
2015
Homo sapiens (P47712), Homo sapiens (W0FXB0)
Manually annotated by BRENDA team
Batchu, K.C.; Haenninen, S.; Jha, S.K.; Jeltsch, M.; Somerharju, P.
Factors regulating the substrate specificity of cytosolic phospholipase A2-alpha in vitro
Biochim. Biophys. Acta
1861
1597-1604
2016
Homo sapiens (P47712), Homo sapiens
Manually annotated by BRENDA team
Arnsmann, M.; Hanekamp, W.; Elfringhoff, A.S.; Lehr, M.
Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A2. Effect of substituents at the indole 3-position on activity, solubility, and metabolic stability
Eur. J. Med. Chem.
125
1107-1114
2017
Homo sapiens (P47712)
Manually annotated by BRENDA team
Fisher, A.B.
The phospholipase A2 activity of peroxiredoxin 6
J. Lipid Res.
59
1132-1147
2018
Trematomus bernacchii, Xenopus tropicalis (B1WAZ6), Mus musculus (O08709), Rattus norvegicus (O35244), Bos taurus (O77834), Homo sapiens (P30041), Gallus gallus (Q5ZJF4), Arabidopsis thaliana (Q8S8N6)
Manually annotated by BRENDA team
Wang, H.; Klein, M.G.; Snell, G.; Lane, W.; Zou, H.; Levin, I.; Li, K.; Sang, B.C.
Structure of human GIVD cytosolic phospholipase A2 reveals insights into substrate recognition
J. Mol. Biol.
428
2769-2779
2016
Homo sapiens (Q86XP0), Homo sapiens
Manually annotated by BRENDA team
Movahedi Naini, S.; Sheridan, A.M.; Force, T.; Shah, J.V.; Bonventre, J.V.
Group IVA cytosolic phospholipase A2 regulates the G2-to-M transition by modulating the activity of tumor suppressor SIRT2
Mol. Cell. Biol.
35
3768-3784
2015
Homo sapiens (P47712)
Manually annotated by BRENDA team
Mouchlis, V.D.; Bucher, D.; McCammon, J.A.; Dennis, E.A.
Membranes serve as allosteric activators of phospholipase A2, enabling it to extract, bind, and hydrolyze phospholipid substrates
Proc. Natl. Acad. Sci. USA
112
E516-E525
2015
Homo sapiens (O60733), Homo sapiens (P47712), Homo sapiens
Manually annotated by BRENDA team
Althaus, J.; Hake, T.; Hanekamp, W.; Lehr, M.
1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2? and fatty acid amide hydrolase bioisosteric replacement of the carboxylic acid moiety
J. Enzyme Inhib. Med. Chem.
31
131-140
2016
Homo sapiens
Manually annotated by BRENDA team