Back to results
US 6,218,128 B1Granted
Methods of identifying compounds having nuclear receptor negative hormone and/or antagonist activities
AssigneeAllergan Sales, Inc.
InventorsElliott S. Klein, Sunil Nagpal, Roshantha A. Chandraratna
Life of this patent
Estimating the term…
Abstract
Methods of characterizing and identifying negative hormones of nuclear receptors. Also disclosed are methods of making modulators of retinoid nuclear receptor transactivation activity, assays for agonists, antagonists, and negative hormones of the RAR receptor, and specific retinoid modulators of retinoid nuclear receptors.
Claims21
A method for determining whether a compound is an inverse agonist of a nuclear receptor comprising the steps:
- a) contacting a first polypeptide comprising a corepressor binding region and a ligand dependent transactivation region of said nuclear receptor with a test compound in the presence of a second polypeptide comprising at least a receptor-binding portion of a corepressor able to bind said nuclear receptor and
- b) detecting increased binding of said first polypeptide with said second polypeptide in a manner sensitive to the presence of said compound as an indication that said test compound is an inverse agonist of said receptor.
Dependencies are inferred from the claim text.