Target intelligence / Profile preview

Retinoic acid receptor RXR-alpha (RXRA)

Target
RXRA
Molecular classification
Nuclear hormone receptor, Transcription factor
01

Overview

Retinoic acid receptor RXR-alpha (RXRA) is a nuclear receptor protein that functions as a ligand-dependent transcription factor. It mediates the biological effects of retinoids by regulating gene expression in response to its ligands, primarily 9-cis retinoic acid and all-trans retinoic acid. RXRA forms homodimers or heterodimers with other nuclear receptors such as RARs, PPARs, LXRs, and VDRs to regulate target gene transcription. It is involved in cell differentiation, apoptosis, lipid metabolism, and other biological processes. Dysregulation of RXRA is associated with various diseases.

Other names
Retinoid X receptor alphaNR2B1Nuclear receptor subfamily 2, group B, member 1
02

Mechanism of action

Ligand-dependent transcription factor; forms homo- or heterodimers with other nuclear receptors (RARs, PPARs, LXRs, VDRs) to regulate gene expression by binding to response elements in the promoter region of target genes. In the absence of ligand, RXR-RAR heterodimers recruit corepressors that induce histone deacetylation and chromatin condensation, leading to suppression of gene expression. Upon ligand binding, these corepressors are released and coactivators are recruited for activation of target genes.

03

Biological functions

Regulation of cell differentiationApoptosisLipid metabolismCytochrome P450 system regulationMicroRNA expression affecting vascular endothelial functionMyelin debris phagocytosisRemyelination
04

Disease associations

Bladder urothelial carcinomaPancreatic adenocarcinomaVitamin A deficiency syndromes (related to knockout studies)
05

Safety considerations

Developmental defects (based on knockout studies)Potential for off-target effects due to dimerization with multiple nuclear receptors
06

Interacting drugs

9-cis retinoic acid

1 more in the full profile.

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