ERRbeta Human Estrogen-Related NHR Functional Agonist & Antagonist Coactivator LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
The estrogen-related receptors ERRα, ERRβ, and ERRγ form a subfamily of orphan nuclear receptors that share significant homology with the estrogen receptors ERα and ERβ to possess the potential to positively and negatively regulate estrogen responsiveness. The ER agonist diethylstilbestrol (DES) and the selective ER modulator (SERM) 4-hydroxytamoxifen (4-OHT) have been identified as ERR antagonists. The rational development of synthetic ligands on ERR targets may be useful in improving the treatment of menopause, metabolic disorders, osteoporosis, serum lipids, breast and other cancers.
No. of Assays on Panel:
2
Assays on Panel:
Family
NHR
Name
ERRbeta Human Estrogen-Related NHR Functional Agonist Coactivator LeadHunter Assay - TW
Item
311530-0
Protein
ERRbeta
Organism
Human
Assay Sub Type
Protein-Protein Interaction
Family
NHR
Name
ERRbeta Human Estrogen-Related NHR Functional Antagonist Coactivator LeadHunter Assay - TW
Item
311530-1
Protein
ERRbeta
Organism
Human
Assay Sub Type
Protein-Protein Interaction
Family:
NHR
Sub Family:
Estrogen-Related
Class:
Non-Steroid
Protein Name:
ERRbeta
Uniprot Number:
O95718
Gene Name:
ESRRB
Gene ID:
2103
Gene Aliases:
ERR2|ERRbeta|NR3B2|ERRb
Accession Number:
XM_011536547
Organism:
Human
Construct Details:
LBD, Recombinant
Assay Information
Assay Type:
Functional
Assay Sub Type:
Protein-Protein Interaction
Functional Mode:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
"Test compound and/or vehicle is incubated with the 2.5 nM‡ estrogen related receptor beta (ERRβ)-LBD and coactivator peptide for 1 hour at RT. Determination of the amount of complex formed is read spectrofluorimetrically at 520 nm/490 nm. Test compound-induced increase fluorescence by 50 percent or more (≥50%) relative to the 30 μM GSK4716 response indicates possible ERRβ receptor agonist activity. Test compound-induced inhibition of 10 μM GSK4716-induced fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
1 hr at RT
Control Inhibitor:
4-Hydroxytamoxifen
Control Activator:
GSK4716
Criteria For Significance:
≥ 50% decrease in fluorescence relative to GSK4716 response, ≥ 50% increase in fluorescence relative to GSK4716 response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
ERRbeta Human Estrogen-Related NHR Functional Agonist Coactivator LeadHunter Assay - TW
Item: 311530-0
ERRbeta Human Estrogen-Related NHR Functional Antagonist Coactivator LeadHunter Assay - TW
Item: 311530-1
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