Target intelligence / Profile preview

Glucocorticoid receptor ligand-binding domain (GR-LBD)

Target
GR-LBD
Molecular classification
Nuclear receptor, Transcription factor, Receptor
01

Overview

The glucocorticoid receptor ligand-binding domain (GR-LBD) is a critical component of the glucocorticoid receptor, a member of the nuclear receptor superfamily. Upon binding to glucocorticoid ligands, the GR undergoes conformational changes that facilitate its translocation into the nucleus and interaction with specific DNA sequences called glucocorticoid response elements (GREs). This interaction modulates the expression of genes involved in inflammation, metabolism, and immune response. The GR-LBD is crucial for the regulation of these biological processes and serves as a target for therapeutic interventions in conditions such as inflammatory diseases and metabolic disorders.

Other names
GR ligand-binding domainGR LBD
02

Mechanism of action

Modulation of gene expression via transcription activation or repression after ligand binding; interaction with coactivators or corepressors like PGC1α.

03

Biological functions

Signal transductionImmune responseInflammationMetabolismTranscription regulation
04

Disease associations

CancerInflammationNeurodegenerative diseaseStress responseMetabolic disorders
05

Safety considerations

Potential side effects from long-term glucocorticoid use, including osteoporosis, hyperglycemia, and mood changes.
06

Interacting drugs

Dexamethasone

3 more in the full profile.

07

Biomarkers

Cortisol levelsDexamethasone suppression test

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