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Gene and Protein Information  |
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| 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 |
| 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 |
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| Alphafold | P14555 (Hs), P31482 (Mm), P14423 (Rn) |
| BRENDA | 3.1.1.4 |
| CATH/Gene3D | 1.20.90.10 |
| ChEMBL Target | CHEMBL3474 (Hs), CHEMBL5761 (Mm), CHEMBL3686 (Rn) |
| DrugBank Target | P14555 (Hs) |
| Ensembl Gene | ENSG00000188257 (Hs), ENSMUSG00000058908 (Mm), ENSRNOG00000016945 (Rn) |
| Entrez Gene | 5320 (Hs), 18780 (Mm), 29692 (Rn) |
| Human Protein Atlas | ENSG00000188257 (Hs) |
| KEGG Enzyme | 3.1.1.4 |
| KEGG Gene | hsa:5320 (Hs), mmu:18780 (Mm), rno:29692 (Rn) |
| OMIM | 172411 (Hs) |
| Pharos | P14555 (Hs) |
| RefSeq Nucleotide | NM_000300 (Hs), NM_001082531 (Mm), NM_031598 (Rn) |
| RefSeq Protein | NP_000291 (Hs), NP_113786 (Mm), NP_001076000 (Mm) |
| UniProtKB | P14555 (Hs), P31482 (Mm), P14423 (Rn) |
| Wikipedia | PLA2G2A (Hs) |
| Enzyme Reaction |
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Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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]. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Clinically-Relevant Mutations and Pathophysiology
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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]
