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Literature summary for 3.1.1.4 extracted from

  • Giannattasio, G.; Lai, Y.; Granata, F.; Mounier, C.M.; Nallan, L.; Oslund, R.; Leslie, C.C.; Marone, G.; Lambeau, G.; Gelb, M.H.; Triggiani, M.
    Expression of phospholipases A2 in primary human lung macrophages: role of cytosolic phospholipase A2-alpha in arachidonic acid release and platelet activating factor synthesis (2009), Biochim. Biophys. Acta, 1791, 92-102.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.1.4

Application

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(Commentary)

Cloned (Comment) Organism
cPLA2-alpha and sPLA2s Homo sapiens

Inhibitors

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

Localization Comment Organism GeneOntology No. Textmining

Organism

Organism UniProt Comment Textmining
Homo sapiens O15496
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-

Purification (Commentary)

Purification (Comment) Organism
cPLA2s and sPLA2s Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
colonic cancer cell cPLA2-zeta2 Homo sapiens
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HT-29 cell cPLA2-zeta2 Homo sapiens
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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
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Synonyms

Synonyms Comment Organism
cPLA2-alpha
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 Homo sapiens
cPLA2-zeta2
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 Homo sapiens
cytosolic phospholipase A2-alpha
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 Homo sapiens
GIIA
-
 Homo sapiens
GIID
-
 Homo sapiens
GIIE
-
 Homo sapiens
GIIF
-
 Homo sapiens
GIVA
-
 Homo sapiens
GIVF
-
 Homo sapiens
group IV cPLA2
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 Homo sapiens
group VIA cPLA2
-
 Homo sapiens
GVIA
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 Homo sapiens
GX
-
 Homo sapiens
GXIIA
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 Homo sapiens
iPLA2
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 Homo sapiens
secreted phospholipases A2
-
 Homo sapiens
sPLA2
-
 Homo sapiens

Expression

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

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