ERalpha Human Estrogen NHR Functional Agonist & Antagonist Coactivator LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Estrogens, produced by ovaries and testis, affect growth and differentiation of many target tissues. These include the male and female reproductive tissues (mammary gland, uterus, ovary, and prostate). Estrogens have also been implicated in the physiology of the bone, cardiovascular tissues, and the brain. Two distinct estrogen receptors (ERα and ERß) bind estrogen as well as other agonists and antagonists. Estrogen receptor is a member of the super family of nuclear receptor that show a similar structure and mode of action.
No. of Assays on Panel:
2
Assays on Panel:
Family
NHR
Name
ERalpha Human Estrogen NHR Functional Agonist Coactivator LeadHunter Assay - TW
Item
311410-0
Protein
ERalpha
Organism
Human
Assay Sub Type
Protein-Protein Interaction
Family
NHR
Name
ERalpha Human Estrogen NHR Functional Antagonist Coactivator LeadHunter Assay - TW
Item
311410-1
Protein
ERalpha
Organism
Human
Assay Sub Type
Protein-Protein Interaction
Family:
NHR
Sub Family:
Estrogen
Class:
Steroid
Protein Name:
ERalpha
Uniprot Number:
P03372
Protein Aliases:
ER-alpha|Estradiol receptor|Nuclear receptor subfamily 3 group A member 1
Gene Name:
ESR1
Gene ID:
2099
Gene Aliases:
NR3A1|Era
Accession Number:
NM_001328100
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 estrogen receptor alpha (ERɑ)-LBD and coactivator peptide for 10 minutes at RT. Determination of the amount of complex formed is read spectrofluorimetrically at 520 nm/490 nm. Test compound-induced increase in fluorescence by 50 percent or more (≥50%) relative to the 1 μM Estriol response indicates possible ERɑ receptor agonist activity. Test compound-induced inhibition of 10 nM Estriol-induced fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
10 min at RT
Control Inhibitor:
Fulvestrant
Control Activator:
Estriol
Criteria For Significance:
≥ 50% decrease in fluorescence relative to estriol response, ≥ 50% Increase in fluorescence relative to estriol 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
Adverse / Beneficial Action:
Estrogen antagonists may be useful in improving the treatment of menopause and breast cancers.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
ERalpha Human Estrogen NHR Binding Agonist Radioligand LeadHunter Assay - TW
Item: 226010
ERalpha Human Estrogen NHR Functional Agonist Coactivator LeadHunter Assay - TW
Item: 311410-0
ERalpha Human Estrogen NHR Functional Antagonist Coactivator LeadHunter Assay - TW
Item: 311410-1
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