What is glucocorticoid receptor transactivation?
A direct mechanism of action involves homodimerization of the receptor, translocation via active transport into the nucleus, and binding to specific DNA responsive elements activating gene transcription. This mechanism of action is referred to as transactivation.
Which agonist does the glucocorticoid receptor bind to?
GRβ can also bind the glucocorticoid antagonist mifepristone (RU486) (70). In the presence of RU486, many of the GRβ-mediated changes in gene expression are abolished.
What is the meaning of transactivation?
In the context of gene regulation: transactivation is the increased rate of gene expression triggered either by biological processes or by artificial means, through the expression of an intermediate transactivator protein.
Is the glucocorticoid receptor a nuclear receptor?
The glucocorticoid receptor (GR) is an evolutionally conserved nuclear receptor superfamily protein that mediates the diverse actions of glucocorticoids as a ligand-dependent transcription factor.
What do nuclear receptors do?
Nuclear receptors are activated by lipid-soluble signals (e.g., steroid hormones) that cross the plasma membrane. Once activated, most function as transcription factors to control gene expression for numerous biological processes.
Is mifepristone a glucocorticoid receptor antagonist?
Mifepristone is the first and only available glucocorticoid receptor antagonist. It was initially mainly considered as a so-called ‘contragestive’ pill due to its antiprogestin activity. In this review, we summarize the results of mifepristone reported in the literature as a treatment of Cushing’s syndrome.
What is a cortisol antagonist?
Medications that stop the production or block the binding of cortisol to its receptor are sometimes referred to as cortisol blockers. These prescription drugs may be useful in the treatment of Cushing syndrome, a condition in which the body makes too much cortisol.
What is the function of the transactivation domain?
The transactivation domain or trans-activating domain (TAD) is a transcription factor scaffold domain which contains binding sites for other proteins such as transcription coregulators. These binding sites are frequently referred to as activation functions (AFs). TADs are named after their amino acid composition.
What is a transactivation assay?
The principle of in vitro androgen transactivation assay, based on stable transfection of a cell line with two plasmids; one encoding the androgen receptor and the other, the androgen response element (ARE) upstream of a reporter (REP) gene such as luciferase.
What is a glucocorticoid steroid?
What are glucocorticoids? Glucocorticoid drugs are man-made versions of glucocorticoids, steroids that occur naturally in your body. They have many functions. One is to interrupt inflammation by moving into cells and suppressing the proteins that go on to promote inflammation.