University of California

Paul Webb

Peter J Kushner

C Anthony Hunt

Renee Williard

Gabriella Lopez

Thomas S Scanlan

John D Baxter

Rosalie M Uht

Robert J Fetterick

Sabine Borngraeber

This invention pertains to agonists that activate nuclear receptors. These agonists include an extension that contacts a region of the nuclear receptor outside the native ligand binding pocket. Methods for producing, identifying and designing such agonists are included along with nuclear receptor agonist complexes and libraries of agonists.

Method for creating specific, high affinity nuclear receptor pharmaceuticals

The present invention provides novel assay methods for identifying compounds that may have both estrogen agonist and antagonist properties. In particular, the assay use cells comprising promoters having an AP1 site linked to a reporter gene. Compounds capable of inducing or blocking expression of the reporter gene can thus be identified. The compounds may be further tested for the ability to modulate the standard estrogen response, as well.

Methods for screening compounds for estrogenic activity

Compositions comprising inhibitors of estrogen response

This invention provides methods for modulating gene expression at the transcriptional level. In particular, the methods involve tethering a transcriptional coactivator to a DNA binding domain that is specific for a target nucleic acid sequence and contacting the coactivator with a transcription factor. The transcription factor triggers or represses transcription mediated by the coactivator. Methods for identifying compounds that are able to modulate gene expression are also provided.

Methods to screen for transcription factor-coactivator interactions

Growing community of inventors

San Francisco, CA, United States of America

Paul Webb