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BioAssay: AID 436247

Inhibition of human group-6A iPLA2 at 0.091 mole fraction by mixed micellar assay

A series of 2-oxoamides based on dipeptides and pseudodipeptides were synthesized and their activities towards two human intracellular phospholipases A(2) (GIVA cPLA(2) and GVIA iPLA(2)) and one human secretory phospholipase A(2) (GV sPLA(2)) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA(2) inhibitors. A derivative based on the ethyl ester of an ether more ..
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Unspecified(12)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Unspecified(12)
 
 
 Related BioAssays
 Related BioAssays
AID: 436247
Data Source: ChEMBL (587425)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-07-08
Modify Date: 2014-08-23

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=85/88 kDa calcium-independent phospholipase A2; Short=CaI-PLA2; AltName: Full=Group VI phospholipase A2; Short=GVI PLA2; AltName: Full=Intracellular membrane-associated calcium-independent phospholipase A2 beta; Short=iPLA2-beta; AltName: Full=Patatin-like phospholipase domain-containing protein 9; Short=PNPLA9
Description ..   
Protein Family: Patatin-like phospholipase domain containing protein 9
Comment ..   

Gene:PLA2G6     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: 2-Oxoamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudodipeptides.

Abstract: A series of 2-oxoamides based on dipeptides and pseudodipeptides were synthesized and their activities towards two human intracellular phospholipases A(2) (GIVA cPLA(2) and GVIA iPLA(2)) and one human secretory phospholipase A(2) (GV sPLA(2)) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA(2) inhibitors. A derivative based on the ethyl ester of an ether pseudodipeptide is the first 2-oxoamide, which preferentially inhibits GVIA iPLA(2). The effect of 2-oxoamides on the generation of arachidonic acid from RAW 264.7 macrophages was also studied and it was found that selective GIVA cPLA(2) inhibitors preferentially inhibited cellular arachidonic acid release; one pseudodipeptide gave an IC(50) value of 2muM.
(PMID: 19443224)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

Data Table (Concise)
Data Table ( Complete ):     View All Data
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