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sPLA2-2A

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Target not currently curated in GtoImmuPdb

Target id: 1417

Nomenclature: sPLA2-2A

Family: Hydrolases, Phospholipase A2

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 144 1p36.13 PLA2G2A phospholipase A2 group IIA
Mouse - 146 4 70.57 cM Pla2g2a phospholipase A2, group IIA (platelets, synovial fluid)
Rat - 146 5q36 Pla2g2a phospholipase A2 group IIA
Previous and Unofficial Names Click here for help
GIIC sPLA2 | NPS-PLA2 | PLA2B | PLA2L | phospholipase A2, membrane associated | secreted enzyme type IIA phospholipase A2 | EF | Enhancing factor | phospholipase A2, group IIA (platelets, synovial fluid) | phospholipase A2
Database Links Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.1.1.4

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
varespladib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.1 – 8.1 pIC50 1,4
pIC50 8.1 (IC50 7x10-9 M) [1]
Description: IC50 from a radiometric deoxycholate/phosphatidylcholine assay.
pIC50 8.1 (IC50 9x10-9 M) [1,4]
Description: IC50 from a chromogenic in vitro assay.
KH064 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.5 pIC50 2
pIC50 7.5 (IC50 2.9x10-8 M) [2]
compound 12e [PMID: 18605714] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4x10-8 M) [3]
Inhibitor Comments
A more valid measurement of varespladib's inhibitory activity is represented by the mole fraction (Xi50, which is the IC50 divided by the lipid concentration used in the assay) calculated from the deoxycholate/phosphatidylcholine (DOC/PC) assay, which addresses the fact that the very high potency of varespladib approaches the stoichiometric limit of the assay (limited by the enzyme concentration used in the assay). The Xi50 for varespladib in the DOC/PC assay was 1.5-1.8 x 10-6 [1,4].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 3 GO processes
GO:0050729 positive regulation of inflammatory response TAS
GO:1902563 regulation of neutrophil activation IDA
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GO:0006954 inflammatory response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0042130 negative regulation of T cell proliferation IBA
GO:0050729 positive regulation of inflammatory response TAS
GO:1902563 regulation of neutrophil activation IDA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes
GO:0042130 negative regulation of T cell proliferation IBA
GO:1902563 regulation of neutrophil activation IDA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0042130 negative regulation of T cell proliferation IBA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0042130 negative regulation of T cell proliferation IBA
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Colorectal cancer
Disease Ontology: DOID:9256
OMIM: 114500

References

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1. Draheim SE, Bach NJ, Dillard RD, Berry DR, Carlson DG, Chirgadze NY, Clawson DK, Hartley LW, Johnson LM, Jones ND et al.. (1996) Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides. J Med Chem, 39 (26): 5159-75. [PMID:8978844]

2. Hansford KA, Reid RC, Clark CI, Tyndall JD, Whitehouse MW, Guthrie T, McGeary RP, Schafer K, Martin JL, Fairlie DP. (2003) D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem, 4 (2-3): 181-5. [PMID:12616631]

3. Oslund RC, Cermak N, Gelb MH. (2008) Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. J Med Chem, 51 (15): 4708-14. [PMID:18605714]

4. Snyder DW, Bach NJ, Dillard RD, Draheim SE, Carlson DG, Fox N, Roehm NW, Armstrong CT, Chang CH, Hartley LW et al.. (1999) Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. J Pharmacol Exp Ther, 288 (3): 1117-24. [PMID:10027849]

Contributors

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