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Literature summary for 3.1.1.4 extracted from
- Mechanism of regulation of group IVA phospholipase A2 activity by Ser727 phosphorylation (2008), J. Biol. Chem., 283, 3960-3971.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| additional information | phosphorylation of Ser727 disrupts this inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction, thereby activating cPLA2alpha | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| wild type and mutant cPLA2s overexpression in HEK293 EcR or HEK293-BLT1 cells, expression of fluorescence of FLAG-tagged cPLA2 in Spodoptera frugiperda Sf9 cells using the baculovirus transfection method | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| S505E | site-directed mutagenesis | Homo sapiens |
| S505E/S727A | site-directed mutagenesis | Homo sapiens |
| S727A | mutation of the phosphorylation site Ser727 leading to a dephosphorylation-mimicking mutant, the mutant shows unaltered enzyme activity compared to the wild-type enzyme | Homo sapiens |
| S727E | mutation of the phosphorylation site Ser727 leading to a phosphorylation-mimicking mutant, the mutant shows unaltered enzyme activity compared to the wild-type enzyme | Homo sapiens |
| S727T | mutation of the phosphorylation site Ser727, S727T is as potently inhibited by annexin A2-p11 heterotetramer as the wild type cPLA2alpha, the mutant shows unaltered enzyme activity compared to the wild-type enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| annexin A2 | phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction, as annexin A2 complex annexin A2-p11 heterotetramer | Homo sapiens | |
| annexin A2-p11 heterotetramer | annexin A2-p11 heterotetramer inhibits cPLA2alpha by interacting with Ser727, phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction as annexin A2 complex annexin A2-p11 heterotetramer. annexin A2-p11 heterotetramer inhibition of cPLA2alpha is independent of Ser505 phosphorylation | Homo sapiens | |
| additional information | p11 overexpression inhibits the Ca2+-induced perinuclear translocation of and amino acid release by cPLA2alpha wild type, S727E, and S727T but not by S727A | Homo sapiens | |
| protein p11 | phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction as annexin A2 complex annexin A2-p11 heterotetramer | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Homo sapiens | 5829 | - |
| membrane | - |
Homo sapiens | 16020 | - |
| additional information | p11 overexpression inhibits the Ca2+-induced perinuclear translocation of wild-type and mutant enzymes and the amino acid release by cPLA2alpha wild type, S727E, and S727T but not by S727A | Homo sapiens | - |
- |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | required | Homo sapiens |  |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | cPLA2alpha interacts with the cPLA2alpha-binding protein p11 via the hydroxyl group of Ser727, binding as annexin A2 complex, mechanism of regulation of group IVA phospholipase A2 activity by Ser727 phosphorylation, surface plasmon resonance analysis, overview | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| phosphoprotein | phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction, thereby activating cPLA2alpha, mechanism of regulation, overview | Homo sapiens |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant tagged cPLA2 from Spodoptera frugiperda okadaic acid-treated Sf9 cells | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 1,2-di-O-hexadecyl-sn-glycerol-3-phosphocholine + H2O | - |
Homo sapiens | 1-O-hexadecyl-sn-glycero-3-phosphocholine + hexadecanoate | - |
? | |
| 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine + H2O | 1-stearoyl-2-[14C]arachidonoyl-sn-glycero-3-phosphocholine | Homo sapiens | 1-stearoyl-sn-glycero-3-phosphocholine + arachidonate | - |
? | |
| additional information | cPLA2alpha interacts with the cPLA2alpha-binding protein p11 via the hydroxyl group of Ser727, binding as annexin A2 complex, mechanism of regulation of group IVA phospholipase A2 activity by Ser727 phosphorylation, surface plasmon resonance analysis, overview | Homo sapiens | ? | - |
? | |
| additional information | Ser727 is not directly involved in either membrane binding or catalytic steps | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| cPLA2 | - |
Homo sapiens |
| group IVA cytosolic phospholipase A2 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0001 | - |
pH 7.4, 37°C, recombinant enzyme | Homo sapiens | annexin A2-p11 heterotetramer |
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