Insights on glucocorticoid receptor activity modulation through the binding of rigid steroids.

ABSTRACT:

Background

The glucocorticoid receptor (GR) is a transcription factor that regulates gene expression in a ligand-dependent fashion. This modular protein is one of the major pharmacological targets due to its involvement in both cause and treatment of many human diseases. Intense efforts have been made to get information about the molecular basis of GR activity.

Methodology/principal findings

Here, the behavior of four GR-ligand complexes with different glucocorticoid and antiglucocorticoid properties were evaluated. The ability of GR-ligand complexes to oligomerize in vivo was analyzed by performing the novel Number and Brightness assay. Results showed that most of GR molecules form homodimers inside the nucleus upon ligand binding. Additionally, in vitro GR-DNA binding anal

SUBMITTER: Presman DM 

PROVIDER: S-EPMC2952596 | biostudies-literature | 2010 Oct

REPOSITORIES: biostudies-literature