General Information of the Protein
Protein ID
PT01265
Protein Name
Cytosolic phospholipase A2
Secondarily
Protein Name
Phospholipase A2 group IVA
Phosphatidylcholine 2-acylhydrolase
Gene Name
PLA2G4A
Secondarily
Gene Name
CPLA2
PLA2G4
Sequence
MSFIDPYQHIIVEHQYSHKFTVVVLRATKVTKGAFGDMLDTPDPYVELFISTTPDSRKRTRHFNNDINPVWNETFEFILDPNQENVLEITLMDANYVMDETLGTATFTVSSMKVGEKKEVPFIFNQVTEMVLEMSLEVCSCPDLRFSMALCDQEKTFRQQRKEHIRESMKKLLGPKNSEGLHSARDVPVVAILGSGGGFRAMVGFSGVMKALYESGILDCATYVAGLSGSTWYMSTLYSHPDFPEKGPEEINEELMKNVSHNPLLLLTPQKVKRYVESLWKKKSSGQPVTFTDIFGMLIGETLIHNRMNTTLSSLKEKVNTAQCPLPLFTCLHVKPDVSELMFADWVEFSPYEIGMAKYGTFMAPDLFGSKFFMGTVVKKYEENPLHFLMGVWGSAFSILFNRVLGVSGSQSRGSTMEEELENITTKHIVSNDSSDSDDESHEPKGTENEDAGSDYQSDNQASWIHRMIMALVSDSALFNTREGRAGKVHNFMLGLNLNTSYPLSPLSDFATQDSFDDDELDAAVADPDEFERIYEPLDVKSKKIHVVDSGLTFNLPYPLILRPQRGVDLIISFDFSARPSDSSPPFKELLLAEKWAKMNKLPFPKIDPYVFDREGLKECYVFKPKNPDMEKDCPTIIHFVLANINFRKYRAPGVPRETEEEKEIADFDIFDDPESPFSTFNFQYPNQAFKRLHDLMHFNTLNNIDVIKEAMVESIEYRRQNPSRCSVSLSNVEARRFFNKEFLSKPKA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Has primarily calcium-dependent phospholipase and lysophospholipase activities, with a major role in membrane lipid remodeling and biosynthesis of lipid mediators of the inflammatory response (PubMed:7794891, PubMed:8619991, PubMed:8702602, PubMed:9425121, PubMed:10358058, PubMed:14709560, PubMed:16617059, PubMed:17472963, PubMed:27642067, PubMed:18451993). Plays an important role in embryo implantation and parturition through its ability to trigger prostanoid production (By similarity). Preferentially hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids (phospholipase A2 activity) (PubMed:7794891, PubMed:8619991, PubMed:9425121, PubMed:10358058, PubMed:17472963, PubMed:18451993). Selectively hydrolyzes sn-2 arachidonoyl group from membrane phospholipids, providing the precursor for eicosanoid biosynthesis via the cyclooxygenase pathway (PubMed:18451993, PubMed:7794891, PubMed:9425121, PubMed:10358058, PubMed:17472963). In an alternative pathway of eicosanoid biosynthesis, hydrolyzes sn-2 fatty acyl chain of eicosanoid lysophopholipids to release free bioactive eicosanoids (PubMed:27642067). Hydrolyzes the ester bond of the fatty acyl group attached at sn-1 position of phospholipids (phospholipase A1 activity) only if an ether linkage rather than an ester linkage is present at the sn-2 position. This hydrolysis is not stereospecific (PubMed:7794891). Has calcium-independent phospholipase A2 and lysophospholipase activities in the presence of phosphoinositides (PubMed:12672805). Has O-acyltransferase activity. Catalyzes the transfer of fatty acyl chains from phospholipids to a primary hydroxyl group of glycerol (sn-1 or sn-3), potentially contributing to monoacylglycerol synthesis (PubMed:7794891).
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Uniprot ID
Primary ID:
P47712

Secondarily ID:
B1AKG4
Q29R80
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Ensembl ID
ENSG00000116711
HGNC ID
HGNC:9035
Subcellular Location
Cytoplasm
Golgi apparatus membrane
Nucleus envelope
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0464803
2-{4-[4-(4-oxo-4H-chromen-2-yl)phenyl]phenyl}-4H-chromen-4-one
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C30H18O4
 1
1
IC50 = 6000 nM
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CP0381515
3-(4-(4-oxo-4H-chromen-2-yl)phenyl)-2-phenyl-4H-chromen-4-one
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C30H18O4
 1
1
IC50 = 8420 nM
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CP0394409
6-[4-(4-Oxo-4H-chromen-2-yl)-phenyl]-2-phenyl-chromen-4-one
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C30H18O4
 1
1
IC50 = 11900 nM
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CP0453270
6-[3-(4-Oxo-4H-chromen-2-yl)-phenyl]-2-phenyl-chromen-4-one
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C30H18O4
 1
1
IC50 = 16800 nM
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CP0440729
2-{4-[3-(4-oxo-4H-chromen-2-yl)phenyl]phenyl}-4H-chromen-4-one
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C30H18O4
 1
1
IC50 = 38700 nM
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CP0390962
2,2'-Diphenyl-[6,6']bichromenyl-4,4'-dione
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C30H18O4
 1
1
IC50 = 48100 nM
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CP0012462
acs.jmedchem.1c00409_ST.480
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C30H18O10
 1
1
IC50 > 100000 nM
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CP0847707
Ochnaflavone
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C30H18O10
 1
1
IC50 > 100000 nM
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Clinical Information about the Protein
Target 1 ( Cytosolic phospholipase A2 (GIVA cPLA2) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Asthma [ICD-11: CA23]
Discontinued Drug(s) 1 Discontinued Drug  1
1 EFIPLADIB Terminated
Asthma