Target intelligence / Profile preview

Mineralocorticoid Receptor, Androgen Receptor, Glucocorticoid Receptor (MR, AR, GR)

Target
MR, AR, GR
Molecular classification
Nuclear receptor, Intracellular receptor, Ligand-activated transcription factor, Steroid hormone receptor, nuclear receptor subfamily 3, group C, member 2 (NR3C2), nuclear receptor subfamily 3, group C, member 4 (NR3C4), nuclear receptor subfamily 3, group C, member 1 (NR3C1)
01

Overview

The mineralocorticoid receptor (MR), androgen receptor (AR), and glucocorticoid receptor (GR) are closely related members of the nuclear receptor superfamily, specifically the steroid hormone receptor subfamily. They function as ligand-activated transcription factors with a conserved domain structure: an N-terminal activation domain, a central DNA-binding domain, a hinge region, and a ligand-binding domain. Upon binding their respective steroid hormones—aldosterone (MR), androgens (AR), or glucocorticoids (GR)—these receptors translocate into the nucleus and regulate gene expression to control physiologic processes such as electrolyte balance (MR), development of male traits (AR), and stress responses (GR). They are key targets in diseases such as hypertension, prostate cancer, and inflammatory disorders, and are therapeutically modulated by numerous small molecules.

Other names
MRNR3C2ARNR3C4GRNR3C1
02

Mechanism of action

Ligand binding to the receptor induces conformational change, nuclear translocation, and gene transcription modulation (agonism or antagonism). Antagonists prevent receptor-mediated transcription of target genes. Some drugs function as partial agonists or selective modulators.

03

Biological functions

Regulation of gene transcriptionHormone-mediated signal transductionControl of diverse physiological processes (MR: salt and water homeostasis; AR: male sexual development, muscle and bone maintenance; GR: stress response, immune modulation, metabolism)
04

Disease associations

Cancer (especially prostate cancer for AR)Inflammation (GR modulation)Cardiovascular disease (MR involvement in hypertension and heart failure)Endocrine disordersNeurodegenerative disease (GR involvement)
05

Safety considerations

Hyperkalemia (MR)hypotension (MR)kidney dysfunction (MR)Hormonal imbalances (AR)metabolic effects (AR)cardiovascular risk in prostate cancer therapy (AR)Immunosuppression (GR)metabolic syndrome (GR)osteoporosis (GR)adrenal suppression (GR)
06

Interacting drugs

Spironolactone (MR)

10 more in the full profile.

07

Biomarkers

Aldosterone levels (for MR)sodium/potassium balance (for MR)Prostate-specific antigen (PSA) for prostate cancer (for AR)Cortisol levels (for GR)ACTH stimulation tests (for GR)

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