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BioAssay: AID 600524

Agonist activity at yeast GAL4 fused human RXRbeta ligand binding domain expressed in HeLa cells assessed as receptor transactivation by luciferase reporter gene assay

A series of retinoids designed to interfere with the repositioning of H12 have been synthesized to identify novel RARgamma antagonists based on the structure of known RARgamma agonists. The transcriptional activities of the novel ligands were revealed by cell-based reporting assays, using engineered cells containg RAR subtype-selective fusions of the RAR ligand-binding domains with the yeast GAL4 more ..
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 Tested Compounds
 Tested Compounds
All(6)
 
 
Active(3)
 
 
Inactive(3)
 
 
 Tested Substances
 Tested Substances
All(6)
 
 
Active(3)
 
 
Inactive(3)
 
 
AID: 600524
Data Source: ChEMBL (750675)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Retinoic acid receptor RXR-beta; AltName: Full=Nuclear receptor subfamily 2 group B member 2; AltName: Full=Retinoid X receptor beta
Description ..   
Protein Family: The ligand binding domain of the retinoid X receptor and Ultraspiracle, members of nuclear receptor superfamily
Comment ..   

Gene:RXRB     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 3
Description:
Title: Retinoid receptor subtype-selective modulators through synthetic modifications of RARgamma agonists.

Abstract: A series of retinoids designed to interfere with the repositioning of H12 have been synthesized to identify novel RARgamma antagonists based on the structure of known RARgamma agonists. The transcriptional activities of the novel ligands were revealed by cell-based reporting assays, using engineered cells containg RAR subtype-selective fusions of the RAR ligand-binding domains with the yeast GAL4 activator DNA-binding domain and the cognate luciferase reporter gene. Whereas none of the ligands exhibited features of a selective RARgamma antagonist, some of them are endowed with interesting activities. In particular 24a acts as a pan-RAR agonist that induces at high concentration a higher transactivation potential on RARalpha than TTNPB and synergizes at low concentration with TTNPB-bound RARalpha but not RARbeta or RARgamma. Similarly, 24c synergizes with TTNPB-bound RARgamma and exhibits RARalpha,beta antagonist activity. Compounds 24b and 25b are strong RARalpha,beta-selective antagonists without agonist or antagonist activities for RARgamma. Compounds 24b and 24c display weak RXR antagonist activity. In addition several pan-antagonists and partial agonist/antagonists have been defined.
(PMID: 19482478)
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: HeLa
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
Classification
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