METHODS FOR SCREENING FOR REGULATORS OF INTRACELLULAR RECEPTOR TRANSCRIPTION AND COMPOUNDS REGULATING THE SAME.

摘要

Methods to screen for antagonists of steroid IR transcription as mediated by the PR-A useform of theed methods include a cell in which PR-A is transcriptionally inactive containing a steroid IR other than PR. PR-A and a reporter vector that includes a promoter which is transcriptionally active in the presence of the steroid IR and an activator of said steroid IR, but is substantially transcriptionally inactive in the presence of PR-A. This cell is contacted with the activator of the steroid IR and a compound to be assayed, and the level of reporter product produced in the cell is measured and compared to the level of reporter expressed in a similar cellular system absent PR-A as an indication of the potential antagonist activity of the compound being assayed. Also provided are an assay kit, a method of screening PR active compounds as ER antagonists and compounds that inhibit the transcriptional activity of a steroid IR in the presence ntially transcriptionally inactive.