Molecular mechanisms of glucocorticoid action and resistance

The actions of glucocorticoid hormones are mediated by an intracellular receptor, the glucocorticoid receptor (GR). The mechanism of action of this ligand-inducible transcription factor is discussed, focusing on mechanisms of glucocorticoid resistance. Three mechanisms are highlighted: ligand-induce...

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Bibliographic Details
Published in:Journal of steroid biochemistry and molecular biology 2002-12, Vol.83 (1), p.37-48
Main Authors: Schaaf, Marcel J.M, Cidlowski, John A
Format: Article
Language:English
Subjects:
Active Transport, Cell Nucleus
Animals
Biological and medical sciences
DNA - metabolism
Down-Regulation
Glucocorticoid
Glucocorticoid receptor
Glucocorticoids - metabolism
Homologous down-regulation
Hormones. Endocrine system
Humans
Ligands
Medical sciences
Models, Biological
Models, Genetic
NF-kappa B - metabolism
NF-κB
Pharmacology. Drug treatments
Phosphorylation
Protein Binding
Protein Isoforms
Receptors, Glucocorticoid - chemistry
Receptors, Glucocorticoid - genetics
Receptors, Glucocorticoid - physiology
RNA, Messenger - metabolism
Transcriptional Activation
β-Isoform
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Summary:The actions of glucocorticoid hormones are mediated by an intracellular receptor, the glucocorticoid receptor (GR). The mechanism of action of this ligand-inducible transcription factor is discussed, focusing on mechanisms of glucocorticoid resistance. Three mechanisms are highlighted: ligand-induced down-regulation of the receptor, the dominant-negative inhibition by the β-isoform of the receptor, and repression by the transcription factor NF-κB. It has been shown that these mechanisms can significantly inhibit glucocorticoid signaling, and could therefore seriously decrease the efficacy of glucocorticoids used clinically.
ISSN:0960-0760
1879-1220
DOI:10.1016/S0960-0760(02)00263-7