Bookmark and Share
BioAssay: AID 736345

Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as beta-galactosidase activity at 25 uM measured after 48 hrs relative to vehicle control

Twenty three dual PPARalpha and gamma molecules of natural product origin, previously reported by our group, were further investigated for pan PPAR transactivation against PPARdelta. The in vitro cell toxicity profile, as well as, in silico study of the most active molecules within this new class of pan PPAR agonists are also described. 3',5' Dimethoxy-7 hydroxyisoflavone 6, Psi-baptigenin 7, 4' more ..
_
   
 Tested Compounds
 Tested Compounds
All(24)
 
 
Unspecified(24)
 
 
 Tested Substances
 Tested Substances
All(24)
 
 
Unspecified(24)
 
 
 Related BioAssays
 Related BioAssays
AID: 736345
Data Source: ChEMBL (948913)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-08-27

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Peroxisome proliferator-activated receptor delta; Short=PPAR-delta; AltName: Full=NUCI; AltName: Full=Nuclear hormone receptor 1; Short=NUC1; AltName: Full=Nuclear receptor subfamily 1 group C member 2; AltName: Full=Peroxisome proliferator-activated receptor beta; Short=PPAR-beta
Description ..   
Protein Family: The ligand binding domain of peroxisome proliferator-activated receptors
Comment ..   

Gene:PPARD     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.

Abstract: Twenty three dual PPARalpha and gamma molecules of natural product origin, previously reported by our group, were further investigated for pan PPAR transactivation against PPARdelta. The in vitro cell toxicity profile, as well as, in silico study of the most active molecules within this new class of pan PPAR agonists are also described. 3',5' Dimethoxy-7 hydroxyisoflavone 6, Psi-baptigenin 7, 4' fluoro-7 hydroxyisoflavone 8, and 3' methoxy-7 hydroxyisoflavone 9 were identified as the most potent molecules studied within the set compared to the commercially available pan PPAR agonist, bezafibrate 1. These novel active molecules may thus be useful as future leads in PPAR-related disorders, including type II diabetes mellitus and metabolic syndrome.
(PMID: 23265844)
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
BAO: Assay Format: cell-based format
Assay Cell Type: HEK293
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1FC activity commentFC activity commentString
2FC standard flagFC standard flagInteger
3FC qualifierFC qualifierString
4FC published valueFC published valueFloat
5FC standard valueFC standard valueFloat

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