Related Experiment Video
Updated: Jul 14, 2026

Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
Published on: September 21, 2011
Glucocorticoid receptor action in beneficial and side effects of steroid therapy: lessons from conditional knockout
Anna Kleiman1, Jan P Tuckermann
1Leibniz Institute for Age Research, Fritz Lipmann Institute, Group of Tissue specific Hormone Action, Beutenberg Str. 11, D-07745 Jena, Germany.
Abstract:
Glucocorticoids (GCs) are potent immune suppressive drugs with unfortunately severe side effects. Different molecular modes of actions of the GC receptor (GR) have been identified. Transcriptional transactivation by binding of a dimerized GR protein complex to the promoter of GC regulated genes or interference with activity of pro-inflammatory transcription factors by GR monomers are considered as the two major mechanisms. It has been hypothesized that selective GR agonists (SEGRAs) addressing dimer-independent function would reveal potent steroid therapeutic activity with reduced side effects. Recent studies of a mouse knock-in strain with a dimerization-deficient GR demonstrate that some inflammatory processes can be suppressed by GCs, while others cannot. Also side effects of GCs occur in these mice. Thus, depending on the process that is treated, SEGRA could be therapeutically more or less effective and not all side effects of steroid therapy may be reduced.
Related Concept Videos
Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids
Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids
ICS work through a multifaceted mechanism of action. They suppress the inflammatory response caused by the proliferation of TH cells. They also reduce the transcription of the IL-2 gene, which is involved in the...
Target Cell Response to Hormones
Notably, the cellular response can be regulated by altering the number of receptors expressed in the cell. For example, prolonged exposure to elevated hormone levels results in a gradual decline or down-regulation in the number of receptors for that specific hormone on the cell surface. Conversely, in response to low hormone levels, cells may use up-regulation, producing an...
Transducer Mechanism: Nuclear Receptors
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
Glucagon-like Receptor Agonists
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Cushing Syndrome I: Introduction
