AR Human Androgen NHR Cell Based Antagonist Translocation LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Androgen receptor (AR) is the member of steroid nuclear hormone receptors that is involved in psychological physiology and pathological situation of prostate cancer. AR primarily resides in cytoplasm bound to chaperone in the absence of ligand stimulation. Upon ligand activation, AR translocates to nucleus and forms dimer to stimulate androgen responsive genes. Androgen receptor translocation assay is a cell-based phenotypic imaging method to measure nuclear translocation level of AR in response to testing substance. Cell-line expresses human full length AR and a fluorescent protein are used to test AR agonists and antagonists.
Family:
NHR
Sub Family:
3-Ketosteroid
Class:
Steroid
Protein Name:
AR
Uniprot Number:
P10275
Protein Aliases:
Dihydrotestosterone receptor|Nuclear receptor subfamily 3 group C member 6
Gene Name:
AR
Gene ID:
367
Gene Aliases:
AIS|NR3C4|SMAX1|HUMARA
Accession Number:
BC132975.1
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
High-content Imaging
Platform:
HCA
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
CHO-K1-hAR clone A2 cells expressing human full-length AR linked with red fluorescent protein (RFP) are seeded overnight. Test compound or vehicle is treated incubated with cells at 37°C, 5% CO2 for 6 hours. AR translocation is evaluated by nuclear redistribution of RFP-tagged AR with imaging acquisition and analysis. Test compound-induced increase in AR translocation response by 50 percent or more (≥50%) relative to 100 nM 5α-dihydrotestosterone indicates possible AR agonist activity. Test compound-induced inhibition of 300 pM 5α-dihydrotestosterone-induced AR translocation response by 50 percent or more (≥50%) indicates possible AR antagonist activity.
Incubation:
6 hr at 37°C
Control Inhibitor:
Enzalutamide
Criteria For Significance:
≥ 50% decrease in AR translocation relative to 5α-dihydrotestosterone 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:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Adverse / Beneficial Action:
Testosterone receptor agonists may promote prostate cancer and cause edema while antagonists may inhibit spermatogenesis and be useful in the treatment of prostate cancer.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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