Inhibitors | Comment | Organism | Structure |
---|---|---|---|
SB435495 | SB435495-treated oxidized low density lipoprotein has nearly undetectable lp-PLA2 activity. Completely inhibits lp-PLA2 enzyme activity in the whole culture media of THP-1 cells with 0.0001 mM | Homo sapiens | |
SB480848 | darapladib, completely inhibits lp-PLA2 enzyme activity in the whole culture media of THP-1 cells with 0.0001 mM | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
THP-1 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
1-palmitoyl-sn-glycerol-3-phosphocholine + H2O | - |
Homo sapiens | ? | - |
? | |
oxidized high density lipoprotein + H2O | - |
Homo sapiens | ? | - |
? | |
oxidized low density lipoprotein + H2O | - |
Homo sapiens | ? | - |
? | |
platelet activating factor + H2O | - |
Homo sapiens | lyso-platelet activating factor | - |
? |
Synonyms | Comment | Organism |
---|---|---|
lipoprotein-associated phospholipase A2 | - |
Homo sapiens |
Lp-PLA2 | - |
Homo sapiens |
Organism | Comment | Expression |
---|---|---|
Homo sapiens | unstimulated and low density lipoprotein-treated THP-1 cells fail to produce detectable levels of lp-PLA2. Inhibition of either phosphatidylinositol 3-kinase (by LY294002 and wortmannin) or p38 mitogen-activating protein kinase (by SB203580 and SB202190) completely blocks oxidized low density lipoprotein-induced lp-PLA2 expression. Neither platelet activating factor and lyso-platelet activating factor nor 1-palmitoyl-sn-glycerol-3-phosphocholine and high density lipoprotein can induce lp-PLA2 expression | down |
Homo sapiens | oxidized low density lipoprotein, and more specifically its unhydrolyzed oxidized phospholipids, upregulate lp-PLA2 expression in monocytes through the phosphatidylinositol 3-kinase and p38 mitogen-activating protein kinase pathway. Oxidized low density lipoprotein-treated cells produce lp-PLA2 mRNA in a concentration- and time-dependent manner. Oxidized high density lipoprotein can also induce lp-PLA2 expression | up |
General Information | Comment | Organism |
---|---|---|
malfunction | inhibition of lp-PLA2 activity in conditioned medium by SB435495 or SB480848 significantly decreases lipid accumulation in macrophages | Homo sapiens |
physiological function | lp-PLA2 promotes lipoprotein uptake in macrophages | Homo sapiens |