Mixed agonists of the progesterone receptor and assays therefor

摘要

A third class of PR-ligand (i.e. mixed agonist) is identified which induces a progesterone receptor conformation distinct from that induced by a PR agonist or antagonist. PR mixed agonists exhibit partial agonist activity which is influenced by cell context. These compounds provide useful pharmacological profiles for treating progesterone related diseases and/or conditions. Assays are provided to screen for PR mixed agonists. Molecular designs are provided to convert a PR antagonist to a PR mixed agonist.