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Drug-Target Interaction

Drug

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PubChem ID:444899
Structure:
Synonyms:
(14C)Arachidonic acid
(5Z,8Z,11Z,14Z)-5,8,11,14-icosatetraenoic acid
(5Z,8Z,11Z,14Z)-Eicosatetraenoic acid
(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoic acid
(5Z,8Z,11Z,14Z)-Icosatetraenoic acid
(5Z,8Z,11Z,14Z)icosa-5,8,11,14-tetraenoic acid
10931_FLUKA
10931_SIGMA
1adl
1gnj
1vyg
5,8,11,14-Eicosatetraenoic acid
5,8,11,14-Eicosatetraenoic acid, (all-Z)-
5,8,11,14-Eicosatetraenoic acid, labeled with carbon-14, (all-Z)-
5,8,11,14-Icosatetraenoic Acid
506-32-1
5Z,8Z,11Z,14Z-icosatetraenoic acid
93444-49-6
A0781
A3555_SIGMA
A3925_SIGMA
A9673_SIGMA
AA
AB1004494
AC-14348
AC1L9H30
ACD
AG-F-70356
AIDS-045704
AIDS045704
all-cis-5,8,11,14-eicosatetraenoic acid
ARA
Arachidonate
Arachidonic acid
ARACHIDONIC ACID (20:4 n-6)
Arachidonsaeure
BML3-B03
BRD-K03070961-001-02-8
BSPBio_001539
C00219
CHEBI:15843
CHEMBL15594
cis,cis,cis,cis-5,8,11,14-Eicosatetraenoic acid
cis,cis,cis,cis-5,8,11,14-Eicosatetraenoic acid;
cis-5,8,11,14-Eicosatetraenoic acid
cis-Delta(5,8,11,14)-eicosatetraenoic acid
D18DBC10-379C-4E78-9A50-8B791A2F4E68
Eicosa-5Z,8Z,11Z,14Z-tetraenoic acid
HMS1361M21
HMS1791M21
HMS1989M21
Icosa-5,8,11,14-tetraenoic acid
IDI1_034009
LMFA01030001
MLS001361328
MolPort-003-666-529
NCGC00094608-01
NCGC00094608-02
NCGC00094608-03
NCGC00094608-04
NCGC00094608-05
NCGC00094608-06
nchembio.129-comp13
nchembio.86-comp6
SMR000857374
Spectrum5_001910
ST069383
[1-14C]Arachidonic acid

Target

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Uniprot ID:PA21B_CAVPO
Synonyms:
Group IB phospholipase A2
Phosphatidylcholine 2-acylhydrolase
Phospholipase A2
EC-Numbers:3.1.1.4
Organism:Cavia porcellus
Guinea pig
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

10848980
Inhibition by unsaturated fatty acids of type II secretory phospholipase A2 synthesis in guinea-pig alveolar macrophages evidence for the eicosanoid-independent pathway.. M Alaoui El Azher; N Havet; M Singer; C Dumarey; L Touqui (2000) European journal of biochemistry / FEBS display abstract
The effect of arachidonic acid (C20:4) on the production of secretory type II phospholipase A2 (sPLA2-II) by guinea-pig alveolar macrophages was investigated. We show that incubation of these cells with 1-30 microM of arachidonic acid inhibits the synthesis of sPLA2-II in a concentration-dependent manner with an IC50 of approximately 7.5 microM. The inhibition by low concentrations (5 microM) of arachidonic acid was partially reduced by pretreatment of alveolar macrophages with cyclooxygenase or cytochrome P450 inhibitors (aspirin and 1-aminobenzotriazole, respectively), but not by lipoxygenase inhibitor, BW A4C. However, these inhibitors failed to interfere with the effect of high concentrations (30 microM) of arachidonic acid, suggesting that the latter may act on the expression of sPLA2-II, at least in part, independently of eicosanoid generation. Indeed, a similar inhibitory effect on sPLA2-II activity and mRNA expression was observed with other unsaturated fatty acids such as eicosapentaenoic (C20:5) and oleic (C18:1) acids, but not with the saturated fatty acid, palmitic acid (C16:0). In addition, arachidonic acid partially reduced the secretion of tumor necrosis factor alpha, an important intermediate in the induction of sPLA2-II synthesis by guinea-pig alveolar macrophages. However, addition of recombinant tumor necrosis factor alpha failed to reverse the inhibitory effect of arachidonic acid on sPLA2-II expression, suggesting that this process occurs downstream of tumor necrosis factor alpha secretion. We conclude that the expression of sPLA2-II in alveolar macrophages is down-regulated at the transcriptional level by arachidonic acid either directly or via its cyclooxygenase and cytochrome P450-derived metabolites.