| abstract |
The present invention relates to methods and agonist/antagonist compounds for modulating nuclear receptor activity, and nuclear receptor ligand binding. The invention includes a method for identifying residues comprising a ligand binding domain for a nuclear receptor of interest. Also included in a method of identifying agonists and/or antagonists that bind to the ligand binding domain of the nuclear receptors, and the estrogen receptor in particular. The invention is exemplified by identification and manipulation of the ligand binding domain of the estrogen receptor and compounds that bind to this site. The methods can be applied to other nuclear receptors including TR, GR and PR. |