Target intelligence / Profile preview

Retinoid X Receptor (RXR)

Target
RXR
Molecular classification
Nuclear receptor, Transcription factor
01

Overview

Retinoid X receptors (RXRs) are a subgroup of the nuclear receptor superfamily, functioning as ligand-activated transcription factors. They are primarily activated by 9-cis retinoic acid and play central roles in regulating gene expression related to development, metabolism, and cellular differentiation. RXRs form homodimers or heterodimers with other nuclear receptors like RARs, PPARs, and LXRs, modulating gene expression in various tissues. There are three main isoforms: RXR-alpha, RXR-beta, and RXR-gamma. RXRs regulate diverse physiological processes, including lipid, glucose, and cholesterol metabolism, and have been implicated in neurodegenerative diseases. Pharmacological targeting has shown protective effects against neuronal injury models. Bexarotene is an example of a synthetic ligand that has been used experimentally and clinically.

02

Mechanism of action

Ligand-dependent activation of transcription through recruitment of coactivators and release of corepressors.

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Biological functions

Lipid metabolism regulationGlucose homeostasisCholesterol metabolismBile acid homeostasisDevelopmentCellular differentiationTranscriptional regulation
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Disease associations

Metabolic disordersNeurodegenerative diseasesAlzheimer's diseaseParkinson's diseaseNeuroinflammationAllergies
05

Safety considerations

Hypothyroidism (via TR/RXR pathway crosstalk)
06

Interacting drugs

9-cis retinoic acid

1 more in the full profile.

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