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BioAssay: AID 730945

Transactivation of PPARdelta (unknown origin) expressed in HEK293 cells co-transfected with PDK4-PPRE by luciferase reporter gene assay

Type 2 diabetes is at epidemic proportions and thus development of novel pharmaceutical therapies for improving insulin sensitivity has become of paramount importance. The objectives of the current study were to develop novel dual PPARgamma/delta agonists without the deleterious side effects associated with full PPARgamma agonists. Docking simulations of 23 novel compounds within the ligand more ..
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Active(3)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(3)
 
 
AID: 730945
Data Source: ChEMBL (943513)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-08-27

Data Table ( Complete ):           View Active Data    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..
BioActive Compounds: 3
Description:
Title: Design, development and evaluation of novel dual PPARdelta/PPARgamma agonists.

Abstract: Type 2 diabetes is at epidemic proportions and thus development of novel pharmaceutical therapies for improving insulin sensitivity has become of paramount importance. The objectives of the current study were to develop novel dual PPARgamma/delta agonists without the deleterious side effects associated with full PPARgamma agonists. Docking simulations of 23 novel compounds within the ligand binding domain of PPARgamma/delta were performed using AutoDock Vina which consistently reproduced experimental binding poses from known PPAR agonists. Comparisons were made and described with other docking programs AutoDock and Surflex-Dock (from SYBYL-X). Biological evaluation of compounds was accomplished by transcriptional promoter activity assays, quantitative PCR gene analysis for known PPARgamma/delta targets as well as in vitro assays for lipid accumulation and mitochondrial biogenesis verses known PPAR agonists. We found one (compound 9) out of the 23 compounds evaluated, to be the most potent and selective dual PPARgamma/delta agonist which did not display the deleterious side effects associated with full PPARgamma agonists.
(PMID: 23273519)
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
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat

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