Community hub
Recent from talks
Knowledge base stats:
Talk channels stats:
Members stats:
Glucocorticoid receptor
The glucocorticoid receptor (GR or GCR) also known by its gene name NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the steroid receptor for glucocorticoids such as cortisol.
The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, inflammation, and immune response. Because the receptor gene is expressed in several forms, it has many different (pleiotropic) effects in different parts of the body and in the context of different diseases.
GR is a steroid receptor and thus its canonical action is similar to other steroid receptors. The unbound receptor resides in the cytosol of the cell. When glucocorticoids bind to the receptor, GR translocates to the nucleus of the cell where it acts as a transcription factor. The activated GR complex up-regulates the expression of anti-inflammatory proteins in the nucleus or represses the expression of pro-inflammatory proteins in the cytosol (by preventing the translocation of other transcription factors from the cytosol into the nucleus).
In humans, the GR protein is encoded by NR3C1 gene which is located on chromosome 5 (5q31).
Like the other steroid receptors, GR is modular in structure and contains the following domains (labeled A - F):
In the absence of hormone, 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 FKBP4 (FK506-binding protein 4). The endogenous glucocorticoid hormone cortisol diffuses through the cell membrane into the cytoplasm and binds to the glucocorticoid receptor (GR) resulting in the release of the heat shock proteins. The resulting activated form GR has two principal mechanisms of action, transactivation, and transrepression, described below.
A direct mechanism of action involves homodimerization of the receptor, translocation via active transport into the nucleus, and binding to specific DNA response elements activating gene transcription. This mechanism of action is referred to as transactivation. The biological response depends on the cell type.[citation needed]
In the absence of activated GR, other transcription factors such as NF-κB or AP-1 themselves are able to transactivate target genes. However activated GR can complex with these other transcription factors and prevent them from binding their target genes and hence repress the expression of genes that are normally upregulated by NF-κB or AP-1. This indirect mechanism of action is referred to as transrepression.[citation needed] GR transrepression via NF-κB and AP-1 is restricted only to certain cell types, and is not considered the universal mechanism for IκBα repression.
Hub AI
Glucocorticoid receptor AI simulator
(@Glucocorticoid receptor_simulator)
Glucocorticoid receptor
The glucocorticoid receptor (GR or GCR) also known by its gene name NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the steroid receptor for glucocorticoids such as cortisol.
The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, inflammation, and immune response. Because the receptor gene is expressed in several forms, it has many different (pleiotropic) effects in different parts of the body and in the context of different diseases.
GR is a steroid receptor and thus its canonical action is similar to other steroid receptors. The unbound receptor resides in the cytosol of the cell. When glucocorticoids bind to the receptor, GR translocates to the nucleus of the cell where it acts as a transcription factor. The activated GR complex up-regulates the expression of anti-inflammatory proteins in the nucleus or represses the expression of pro-inflammatory proteins in the cytosol (by preventing the translocation of other transcription factors from the cytosol into the nucleus).
In humans, the GR protein is encoded by NR3C1 gene which is located on chromosome 5 (5q31).
Like the other steroid receptors, GR is modular in structure and contains the following domains (labeled A - F):
In the absence of hormone, 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 FKBP4 (FK506-binding protein 4). The endogenous glucocorticoid hormone cortisol diffuses through the cell membrane into the cytoplasm and binds to the glucocorticoid receptor (GR) resulting in the release of the heat shock proteins. The resulting activated form GR has two principal mechanisms of action, transactivation, and transrepression, described below.
A direct mechanism of action involves homodimerization of the receptor, translocation via active transport into the nucleus, and binding to specific DNA response elements activating gene transcription. This mechanism of action is referred to as transactivation. The biological response depends on the cell type.[citation needed]
In the absence of activated GR, other transcription factors such as NF-κB or AP-1 themselves are able to transactivate target genes. However activated GR can complex with these other transcription factors and prevent them from binding their target genes and hence repress the expression of genes that are normally upregulated by NF-κB or AP-1. This indirect mechanism of action is referred to as transrepression.[citation needed] GR transrepression via NF-κB and AP-1 is restricted only to certain cell types, and is not considered the universal mechanism for IκBα repression.