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Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | - | 441 | 6p12.3 | PLA2G7 | phospholipase A2 group VII | |
| Mouse | - | 440 | 17 B3 | Pla2g7 | phospholipase A2, group VII (platelet-activating factor acetylhydrolase, plasma) | |
| Rat | - | 440 | 9q12 | Pla2g7 | phospholipase A2 group VII | |
| Previous and Unofficial Names |
| GVII | platelet-activating factor acetylhydrolase | PAF acetylhydrolase | LDL-associated phospholipase A2 | LDL-PLA2 | PAFAH | phospholipase A2, group VII (platelet-activating factor acetylhydrolase, plasma) | phospholipase A2 |
| Database Links |
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| Alphafold | Q13093 (Hs), Q60963 (Mm) |
| BRENDA | 3.1.1.4 |
| CATH/Gene3D | 3.40.50.1820 |
| ChEMBL Target | CHEMBL3514 (Hs), CHEMBL5383 (Mm) |
| Ensembl Gene | ENSG00000146070 (Hs), ENSMUSG00000023913 (Mm), ENSRNOG00000025691 (Rn) |
| Entrez Gene | 7941 (Hs), 27226 (Mm), 301265 (Rn) |
| Human Protein Atlas | ENSG00000146070 (Hs) |
| KEGG Enzyme | 3.1.1.4 |
| KEGG Gene | hsa:7941 (Hs), mmu:27226 (Mm), rno:301265 (Rn) |
| OMIM | 601690 (Hs) |
| Pharos | Q13093 (Hs) |
| RefSeq Nucleotide | NM_005084 (Hs), NM_013737 (Mm), NM_001009353 (Rn) |
| RefSeq Protein | NP_005075 (Hs), NP_038765 (Mm), NP_001009353 (Rn) |
| SynPHARM |
84828 (in complex with darapladib) 84827 (in complex with darapladib) 78680 (in complex with darapladib) 84830 (in complex with (S)-23 [PMID: 27933945]) 84829 (in complex with (S)-23 [PMID: 27933945]) |
| UniProtKB | Q13093 (Hs), Q60963 (Mm) |
| Wikipedia | PLA2G7 (Hs) |
| Selected 3D Structures |
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| 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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| Immunopharmacology Comments |
| PLA2-G7 (also referred to as Lp-PLA2) is a pro-inflammatory enzyme. It cleaves oxidatively damaged phospholipid substrates to generate pro-inflammatory mediators including lysophosphatidylcholine and oxidized nonesterified fatty acids [5] and this activity has been linked to atherogenesis and cardiovascular disease. PLA2-G7 has been investigated as a CVD drug target, with one clinical candidate (darapladib) failing in Phase 3 trials. In addition, polymorphisms in the PLA2G7 gene are associated with atopy and asthma [3]. The search for drug-like PLA2-G7 inhibitors with alternative chemotypes to darapladib is continuing [4,7]. |
| Immuno Process Associations | ||
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| Clinically-Relevant Mutations and Pathophysiology
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1. Blackie JA, Bloomer JC, Brown MJ, Cheng HY, Hammond B, Hickey DM, Ife RJ, Leach CA, Lewis VA, Macphee CH et al.. (2003) The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett, 13 (6): 1067-70. [PMID:12643913]
2. Cisar JS, Weber OD, Clapper JR, Blankman JL, Henry CL, Simon GM, Alexander JP, Jones TK, Ezekowitz RAB, O'Neill GP et al.. (2018) Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders. J Med Chem, 61 (20): 9062-9084. [PMID:30067909]
3. Kruse S, Mao XQ, Heinzmann A, Blattmann S, Roberts MH, Braun S, Gao PS, Forster J, Kuehr J, Hopkin JM et al.. (2000) The Ile198Thr and Ala379Val variants of plasmatic PAF-acetylhydrolase impair catalytical activities and are associated with atopy and asthma. Am J Hum Genet, 66 (5): 1522-30. [PMID:10733466]
4. Liu Q, Huang F, Yuan X, Wang K, Zou Y, Shen J, Xu Y. (2017) Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2. J Med Chem, 60 (24): 10231-10244. [PMID:29193967]
5. MacPhee CH, Moores KE, Boyd HF, Dhanak D, Ife RJ, Leach CA, Leake DS, Milliner KJ, Patterson RA, Suckling KE et al.. (1999) Lipoprotein-associated phospholipase A2, platelet-activating factor acetylhydrolase, generates two bioactive products during the oxidation of low-density lipoprotein: use of a novel inhibitor. Biochem J, 338 ( Pt 2): 479-87. [PMID:10024526]
6. Wilensky RL, Macphee CH. (2009) Lipoprotein-associated phospholipase A(2) and atherosclerosis. Curr Opin Lipidol, 20 (5): 415-20. [PMID:19667981]
7. Woolford AJ, Day PJ, Bénéton V, Berdini V, Coyle JE, Dudit Y, Grondin P, Huet P, Lee LY, Manas ES et al.. (2016) Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2). J Med Chem, 59 (23): 10738-10749. [PMID:27933945]
target has curated data in GtoImmuPdb
