Article

Glucocorticoid receptor mutants: man-made tools for functional research.

Laboratory of Eukaryotic Gene Expression and Signal Transduction (LEGEST), Department of Physiology, Ghent University, K.L. Ledeganckstraat 35, B-9000 Gent, Belgium.
Trends in Endocrinology and Metabolism (impact factor: 8.11). 05/2011; 22(8):295-310. DOI:10.1016/j.tem.2011.03.009 pp.295-310
Source: PubMed

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.

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Keywords

activation
 
artificial GR mutants
 
characteristics
 
glucocorticoid receptor
 
GR activity
 
ligand binding
 
ligand-dependent transcription factor
 
post-translational modifications
 
specific cofactors
 
transactivating
 
transrepressing specific gene promoters