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Drug-Target Interaction

Drug

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PubChem ID:1367
Structure:
Synonyms:
07035_FLUKA
1-Abtz
1-Aminobenzotriazole
1-Benzotriazolamine
1614-12-6
1H-1,2,3-Benzotriazol-1-amine
1H-1,2,3-Benzotriazol-1-ylamine
1H-Benzotriazol-1-amine
A 3940
A3940_SIGMA
ABT
AC1L1BBK
AC1Q4XI6
AIDS-141419
AIDS141419
AK-830/25033013
AKOS001013369
AR-1C3327
benzotriazol-1-amine
C033020
CCG-204151
CHEBI:266277
CHEMBL101168
EU-0100056
HMS2235A14
HMS3260K13
Lopac-A-3940
Lopac0_000056
LS-41531
M01240
MLS001056764
MolPort-001-768-990
NCGC00015056-01
NCGC00015056-02
NCGC00015056-03
NCGC00015056-04
NCGC00093570-01
NCGC00093570-02
NCI60_019729
NSC 114498
NSC114498
NSC656987
SBB004208
SMR000326746
ZINC00230381

Target

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Uniprot ID:PA2GA_CAVPO
Synonyms:
GIIC sPLA2
Group IIA phospholipase A2
Phosphatidylcholine 2-acylhydrolase
Phospholipase A2, membrane associated
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.