Thermo Fisher Scientific LanthaScreen TR-FRET ER beta Coactivator Assay Kit

Thermo Fisher Scientific LanthaScreen™ TR-FRET ER beta Coactivator Assay Kit

The LanthaScreen™ TR-FRET ER beta Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential estrogen receptor (ER) beta ligands as agonists or antagonists of ligand-dependent coactivator recruitment.
This kit utilizes:

• ER beta ligand-binding domain (ERβ-LBD) tagged with glutathione-S-transferase (GST)
• Terbium (Tb)-labeled anti-GST antibody
• Fluorescein-labeled coactivator peptide
  in a homogeneous mix-and-read assay format.

Agonist Mode

To identify agonist compounds:

1. ERβ-LBD is added to ligand test compounds.
2. A mixture of fluorescein-coactivator peptide and Tb-anti-GST antibody is added.
3. After incubation at room temperature, the TR-FRET 520:495 emission ratio is calculated.
4. EC50 values are determined from dose-response curves.
   This EC50 represents the ligand concentration required to bind receptor, induce conformational change, and recruit coactivator peptide.

Antagonist Mode

To identify antagonist compounds:

1. ERβ-LBD is added to ligand test compounds.
2. A mixture containing agonist, fluorescein-coactivator peptide, and Tb-anti-GST antibody is added.
3. The agonist concentration used is the EC80, determined from the agonist mode assay.

사양 (Specifications)

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