Target intelligence / Profile preview

Nuclear Receptor (NR)

Target
NR
Molecular classification
Receptor, Transcription factor
01

Overview

Nuclear receptors are a superfamily of ligand-regulated transcription factors that play central roles in regulating gene expression in response to small, lipophilic molecules such as steroid hormones, thyroid hormones, retinoic acid, oxysterols, and vitamins A and D. They are essential for numerous physiological processes including metabolism, reproduction, development, inflammation control, circadian rhythm regulation, and cell differentiation. Upon binding their cognate ligands, they undergo conformational changes that enable them to regulate target gene expression by binding to specific DNA sequences and recruiting co-regulators.

Other names
Steroid hormone receptorIntracellular receptorLigand-activated transcription factor
02

Mechanism of action

Ligand binding induces conformational change, leading to DNA binding and regulation of gene transcription via recruitment of coactivators or corepressors.

03

Biological functions

Transcription regulationMetabolismDevelopmentReproductionInflammationImmune responseCell proliferationCell differentiationCircadian rhythm
04

Disease associations

CancerMetabolic disordersDiabetesObesityInflammatory conditionsHormonal imbalances
05

Safety considerations

Off-target effectsHormone-related side effectsDrug resistance
06

Interacting drugs

Tamoxifen

5 more in the full profile.

07

Biomarkers

ER expression in breast cancerAR expression in prostate cancer

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