Target intelligence / Profile preview

Nuclear hormone receptor (NHR)

Target
NHR
Molecular classification
Receptor, Transcription factor
01

Overview

Nuclear hormone receptors are a large family of intracellular transcription factors that directly bind DNA and regulate the expression of target genes in response to small, lipophilic ligands such as steroid hormones, thyroid hormones, retinoids, and certain vitamins[1][3][4][7][9]. They modulate critical physiological processes including metabolism, development, homeostasis, and cell differentiation[1][9][10]. In humans, there are 48 known nuclear hormone receptors, which are structurally characterized by distinct DNA-binding and ligand-binding domains[3][10]. Upon ligand binding, nuclear hormone receptors undergo a conformational change that promotes association with specific hormone response elements in DNA and recruitment of coactivators or corepressors to modulate transcription[4][8]. They are classified by sequence similarity and mechanism into several subfamilies, including steroid hormone receptors (e.g., estrogen, androgen, glucocorticoid), thyroid/retinoid/vitamin D receptor family, orphan receptors, and others[1][6][7].

Other names
Nuclear receptorNuclear receptor superfamilyNuclear receptor familyNR superfamily
02

Mechanism of action

Ligand-dependent gene transcription modulation Coactivator and corepressor recruitment Hormone response element (HRE) binding to DNA Chromatin remodeling

03

Biological functions

Regulation of gene expressionSignal transductionEmbryonic developmentCell differentiationMetabolism regulationHomeostasisReproductive developmentDetoxification
04

Disease associations

CancerMetabolic diseaseCardiovascular diseaseInflammationNeurodegenerative diseaseDiabetes mellitusInfertility
05

Safety considerations

Hormone-dependent tumor growth or resistanceMetabolic disturbances (e.g., diabetes risk, dyslipidemia)Cardiovascular effects (hypertension, fluid retention)Osteoporosis (some agents)Immunosuppression (glucocorticoid receptor agonists)Liver toxicity for some ligands (e.g., PPAR agonists)
06

Interacting drugs

Tamoxifen (Estrogen receptor modulator)

9 more in the full profile.

07

Biomarkers

ER (Estrogen receptor) status in breast cancerAR (Androgen receptor) in prostate cancerPR (Progesterone receptor) in breast cancerPPARγ expression in diabetes/metabolic syndromeGR (Glucocorticoid receptor) in some cancersVDR (Vitamin D receptor) in bone/immune disorders

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