General Information of the Protein
Protein ID
PT00906
Protein Name
Phospholipase A2, membrane associated
Secondarily
Protein Name
GIIC sPLA2
Group IIA phospholipase A2
Non-pancreatic secretory phospholipase A2
Phosphatidylcholine 2-acylhydrolase 2A
Gene Name
PLA2G2A
Secondarily
Gene Name
PLA2B
PLA2L
RASF-A
Sequence
MKTLLLLAVIMIFGLLQAHGNLVNFHRMIKLTTGKEAALSYGFYGCHCGVGGRGSPKDATDRCCVTHDCCYKRLEKRGCGTKFLSYKFSNSGSRITCAKQDSCRSQLCECDKAAATCFARNKTTYNKKYQYYSNKHCRGSTPRC
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
Secretory calcium-dependent phospholipase A2 that primarily targets extracellular phospholipids with implications in host antimicrobial defense, inflammatory response and tissue regeneration (PubMed:10455175, PubMed:10681567, PubMed:2925633). Hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids (phospholipase A2 activity) with preference for phosphatidylethanolamines and phosphatidylglycerols over phosphatidylcholines (PubMed:10455175, PubMed:10681567). Contributes to lipid remodeling of cellular membranes and generation of lipid mediators involved in pathogen clearance. Displays bactericidal activity against Gram-positive bacteria by directly hydrolyzing phospholipids of the bacterial membrane (PubMed:11694541, PubMed:10358193). Upon sterile inflammation, targets membrane phospholipids of extracellular mitochondria released from activated platelets, generating free unsaturated fatty acids such as arachidonate that is used by neighboring leukocytes to synthesize inflammatory eicosanoids such as leukotrienes. Simultaneously, by compromising mitochondrial membrane integrity, promotes the release in circulation of potent damage-associated molecular pattern molecules that activate the innate immune response (PubMed:25082876). Plays a stem cell regulator role in the intestinal crypt. Within intracellular compartment mediates Paneth cell differentiation and its stem cell supporting functions by inhibiting Wnt signaling pathway in intestinal stem cell (ICS). Secreted in the intestinal lumen upon inflammation, acts in an autocrine way and promotes prostaglandin E2 synthesis that stimulates Wnt signaling pathway in ICS cells and tissue regeneration (By similarity). May play a role in the biosynthesis of N-acyl ethanolamines that regulate energy metabolism and inflammation. Hydrolyzes N-acyl phosphatidylethanolamines to N-acyl lysophosphatidylethanolamines, which are further cleaved by a lysophospholipase D to release N-acyl ethanolamines (PubMed:14998370). Independent of its catalytic activity, acts as a ligand for integrins (PubMed:18635536, PubMed:25398877). Binds to and activates integrins ITGAV:ITGB3, ITGA4:ITGB1 and ITGA5:ITGB1 (PubMed:18635536, PubMed:25398877). Binds to a site (site 2) which is distinct from the classical ligand-binding site (site 1) and induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:25398877). Induces cell proliferation in an integrin-dependent manner (PubMed:18635536).
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Uniprot ID
Primary ID:
P14555

Secondarily ID:
A8K5I7
Q6DN24
Q6IBD9
Q9UCD2
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Ensembl ID
ENSG00000188257
HGNC ID
HGNC:9031
Subcellular Location
Secreted
Cell membrane
Mitochondrion outer membrane
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 = 3000 nM
   TI
   LI
   LO
   TS
CP0847707
Ochnaflavone
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C30H18O10
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0440729
2-{4-[3-(4-oxo-4H-chromen-2-yl)phenyl]phenyl}-4H-chromen-4-one
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C30H18O4
 1
1
IC50 = 15500 nM
   TI
   LI
   LO
   TS
CP0453270
6-[3-(4-Oxo-4H-chromen-2-yl)-phenyl]-2-phenyl-chromen-4-one
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C30H18O4
 1
1
IC50 = 19900 nM
   TI
   LI
   LO
   TS
CP0381515
3-(4-(4-oxo-4H-chromen-2-yl)phenyl)-2-phenyl-4H-chromen-4-one
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C30H18O4
 1
1
IC50 = 23200 nM
   TI
   LI
   LO
   TS
CP0012462
acs.jmedchem.1c00409_ST.480
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C30H18O10
 1
1
IC50 = 23800 nM
   TI
   LI
   LO
   TS
CP0394409
6-[4-(4-Oxo-4H-chromen-2-yl)-phenyl]-2-phenyl-chromen-4-one
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C30H18O4
 1
1
IC50 = 63900 nM
   TI
   LI
   LO
   TS
CP0390962
2,2'-Diphenyl-[6,6']bichromenyl-4,4'-dione
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C30H18O4
 1
1
IC50 = 69300 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Group IIA phospholipase A2 (GIIA sPLA2) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Breast cancer [ICD-11: 2C60-2C65]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 KH064 Clinical trial
Breast cancer