Application | Comment | Organism |
---|---|---|
drug development | capacity of the cPLA2-alpha inhibitors to block or reduce simultaneously the production of the two major classes of lipid mediators, eicosanoids and platelet activating factor, potentially endows these molecules with a very potent anti-inflammatory activity. The cPLA2-alpha inhibitors AZ-1 and pyrrolidine-1 are effective at submicromolar concentrations when macrophages are stimulated by physiological agonists (Mycobacterium tuberculosis purified protein derivative and lipopolysaccharide) provides a rationale for the use of these inhibitors in the treatment of inflammatory lung diseases | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
cPLA2-alpha and sPLA2s | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
AZ-1 | cPLA2-alpha inhibitor, causes almost complete suppression of arachidonic acid release induced by various stimuli. Reduces by 70% the generation of platelet activating factor from macrophages | Homo sapiens | |
Me-Indoxam | sPLA2 inhibitor, has no effect on arachidonic acid release and platelet activating factor synthesis | Homo sapiens | |
N-(cyclopent-1-en-1-yl)pyrrolidine | ccPLA2-alpha inhibitor, causes almost complete suppression of arachidonic acid release induced by various stimuli. Reduces by 70% the generation of platelet activating factor from macrophages | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O15496 | - |
- |
Purification (Comment) | Organism |
---|---|
cPLA2s and sPLA2s | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
colonic cancer cell | cPLA2-zeta2 | Homo sapiens | - |
HT-29 cell | cPLA2-zeta2 | Homo sapiens | - |
macrophage | primary lung macrophage, cPLA2-alpha and iPLA2. Contains the following sPLA2s: GXIIA, GIID, GIIE, GIIF, GX and GIIA. Only GX appears to be released to a limited extent. GIIE and GIIF are only present at the protein level and not on the mRNA level | Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
cPLA2-alpha | - |
Homo sapiens |
cPLA2-zeta2 | - |
Homo sapiens |
cytosolic phospholipase A2-alpha | - |
Homo sapiens |
GIIA | - |
Homo sapiens |
GIID | - |
Homo sapiens |
GIIE | - |
Homo sapiens |
GIIF | - |
Homo sapiens |
GIVA | - |
Homo sapiens |
GIVF | - |
Homo sapiens |
group IV cPLA2 | - |
Homo sapiens |
group VIA cPLA2 | - |
Homo sapiens |
GVIA | - |
Homo sapiens |
GX | - |
Homo sapiens |
GXIIA | - |
Homo sapiens |
iPLA2 | - |
Homo sapiens |
secreted phospholipases A2 | - |
Homo sapiens |
sPLA2 | - |
Homo sapiens |
Organism | Comment | Expression |
---|---|---|
Homo sapiens | lipopolysaccharide has no effect on iPLA2 mRNA and does not induce expression of cPLA2-zeta. Lipopolysaccharide does not induce or enhance the release of any sPLA2s. Lipopolysaccharide neither enhances the sPLA2s GIID, GIIE, GIIF, GX and GXIIA constitutively expressed by macrophages nor induces the expression of GIB and GIII, which are undetectable in resting cells | additional information |
Homo sapiens | macrophages express the alpha isoform of group IV and group VIA cPLA2. Stimulation of macrophages with lipopolysaccharide for 24 hours induces on average a 7fold increase of cPLA2-alpha expression. GIIA is also upregulated by lipopolysaccharide. Both Mycobacterium tuberculosis purified protein derivative and lipopolysaccharide induce arachidonic acid mobilization via cPLA2-alpha in macrophages | up |
General Information | Comment | Organism |
---|---|---|
physiological function | cPLA2-alpha is the major enzyme responsible for lipid mediator production in human macrophages. cPLA2-alpha is a critical enzyme for the release of arachidonic acid which is then available for conversion to eicosanoids | Homo sapiens |