Glucocorticoid receptor mutants: man-made tools for functional research

Abstract

The glucocorticoid receptor (GR) is a ligand-dependent transcription factor that can bind to glucocorticoids (GCs). Upon ligand binding, GR sheds its cytoplasmic chaperoning complex and translocates to the nucleus, where it can act as a ligand-dependent transcription factor, transactivating or transrepressing specific gene promoters. Often, GR interacts with specific cofactors to implement a variety of gene promoter effects. GR activity and function is further modulated by post-translational modifications. To assess the diverse aspects of GR mechanisms of activation and gene regulation, researchers continue to use a range of artificial GR mutants. In this review we analyze the characteristics of GR mutants with the aim of assisting the design and interpretation of GR mutant-based experiments.