Glucocorticoid receptors

Known as NR3C1, GCCR, GCR, GCRST, GR, GRL, nuclear receptor subfamily 3 group C member 1, Glucocorticoid Receptor

The glucocorticoid receptor also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor to which cortisol and other glucocorticoids bind.

It is the body’s stress hormone receptor.

It is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, and immune response.

When it interacts with endogenous stress hormones, it becomes a potent transcription factor that can turn gene expression on or off.

The receptor gene is expressed in several forms.

It has many different effects in different parts of the body.

Glucocorticoid receptor binding to glucocorticoids, results in the regulation of gene transcription.

Glucocorticoid receptor signaling promotes gene expression signatures reflecting reflecting T-cell dysfunction, associated with increased expression of inhibitory checkpoint receptors such as programmed cell death protein-1 and increased Interleukin-10 production.

The unbound receptor resides in the cytosol of the cell.

The receptor-glucorticoid activated complex up-regulates the expression of anti-inflammatory proteins in the nucleus or represses the expression of pro-inflammatory proteins in the cytosol.

It is encoded by NR3C1 gene which is located on chromosome 5 (5q31.

The glucocorticoid receptor (GR) resides in the cytosol complexed with a variety of proteins including heat shock protein 90 (hsp90), the heat shock protein 70 (hsp70) and the protein FKBP52 (FK506-binding protein 52).

When the endogenous glucocorticoid hormone cortisol diffuses through the cell membrane into the cytoplasm and binds to the glucocorticoid receptor (GR), it results in release of the heat shock proteins.

The activated form GR mechanisms of action include, transactivation and transrepression.

The glucocorticoid receptor functional activity appears to be highly context-dependent.

In central nervous system it functions as a major component of endocrine influence, especially the stress response on the brain.

It is implicated in both short and long-term adaptations seen in response to stressors and may be critical to the understanding of psychological disorders, including some or all subtypes of depression and post-traumatic stress disorder.

Dexamethasone and other corticosteroids are agonists to glucocorticoid receptor.

Mifepristone and ketoconazole are antagonists of the glucocorticoid receptor.

Glucocorticoids and glucocorticoid receptors can slow the proliferation of breast cancer cells in patients with estrogen receptor positive disease.

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